Krzysztof Pankiewicz, PhD

Professor, Center for Drug Design (CDD)

Krzysztof Pankiewicz

Contact Info

panki001@umn.edu

Office Phone 612-624-2146

Office Address:
Nils Hasselmo Hall, Room 4-270
312 Church St. SE
Minneapolis, MN 55455

Mailing Address:
MMC 204
312 Church St. SE
Minneapolis, MN 55455

Postdoctoral Research Associate with Dr. Kyoichi Watanabe, Memorial Sloan-Kettering Cancer Center, 1980-1982

PhD, Polish Academy of Sciences (Medicinal Chemistry), 1979

Warsaw Polytechnic (Medicinal Chemistry), 1966

Summary

Awards & Recognition

  • Member of Bugs and Drugs Study Section, 2007 – 2011
  • Dept of Defense CML Research Program, 2005 and 2006
  • NIH-NIAID Special Emphasis Panel, Viral and Eukaryotic Pathogens Study Section, 2004, 2005, 2006
  • Special Review Committee of the Italian Ministry for University and Research, 2001 to 2003, and 2009
  • NIH-NIAID Special Emphasis Panel on Cooperative Research for Biodefense (VATID) and SARS , 2004

Professional Associations

Advisory Board Member, International Society for Nucleosides, Nucleotides, and Nucleic Acids

Editorial Board Member

  • Current Medicinal Chemistry
  • Mini-Reviews in Medicinal Chemistry
  • Medicinal Chemistry Reviews - Online

Scientific Societies

  • American Chemical Society
  • Polish Chemical Society
  • Harvey Society
  • The New York Academy of Sciences
  • American Association for the Advancement of Science
  • American Association for Cancer Research

Research

Research Summary/Interests

Treatment of Chronic Myelogenous Leukemia

Chronic myelogenous leukemia (CML) is a cancer which can be difficult to treat. The cancer cells require a protein called IMP-dehydrogenase (IMPDH) for their uncontrolled growth, but two slightly different forms of the protein are made by human cells. The Type II form is produced in large amounts by CML cancer cells, while the Type I form, a "housekeeping" protein, is the primary form found in normal cells. Both forms require a general helper molecule called nicotinamide adenine dinucleotide (NAD) to carry out their function, but they have subtle structural differences which should make it possible to specifically target the Type II protein.

Nicotinamide adenine dinucleotide (NAD), a small molecule cofactor, is crucial for IMPDH catalytic activity. We synthesized a number of cofactor analogues that bind at the IMP-dehydrogenase but cannot participate in the enzymatic activity, resulting in potent inhibition of the enzyme. Our mycophenolic adenine dinucleotide (MAD) analogues showed potent anti-CML activity in vitro and in a SCID mouse model but are not specific for either isoform. In collaboration with Dr. Barry Goldstein, we solved the crystal structure of the complex of IMP-MAD-IMPDH and found differences between the type I and type II isoforms at the cofactor binding domain. We now exploit these differences in structure-based design of the MAD analogue(s) that would be specific or highly selective against the type II of IMPDH by designing NAD analogs that take advantage of the structural differences between the two forms. We hope that these compounds bind and fill the NAD binding pocket on the Type II protein but not the Type I protein.

Antibiotics

We have two antibiotics projects. The first involves new treatments for tuberculosis, which is estimated to be present (usually in a dormant state) in one third of the global population. Activation of dormant tuberculosis infections can occur in patients with weakened immune systems, as in the case of AIDS.

Isoniazid (INH), an old "first line" treatment for tuberculosis, is a small molecule which reacts inside the bacteria, linking itself to the general helper molecule nicotinamide adenine dinucleotide (NAD). The INH-NAD complex inhibits synthesis of the bacterial cell wall, preventing bacterial growth. Recent studies have shown that drug resistant tuberculosis does not carry out the reaction which links INH to NAD, and therefore cell wall growth is not blocked. We are preparing NAD analogs that mimic the properties of INH-NAD, which would bypass the need for the linking step inside cells. These molecules may be active against drug resistant tuberculosis.

Our second project is similar to the leukemia research described above. Substantial differences exist between the NAD binding site of human IMPDH and IMPDH enzymes from other organisms. We are using these differences to design inhibitors that will block activity of the IMPDH protein in disease-causing organisms without affecting human IMPDH. Target organisms include bacteria, fungi, and protozoa.

Antiviral Agents

We continue our search for drugs, including nucleoside phosphonates, which prevent certain types of viruses from making copies of their genetic material. We are also synthesizing analogs of mycophenolic acid (MPA) as potential anti-viral drugs. MPA is one of the most effective agents against the West Nile virus, but we hope to improve its properties.

Inhibitors of IMP-Dehydrogenase for Treatment of Chronic Myelogenous Leukemia (CML)

Cancer cells, including CML cells, require IMP-dehydrogenase (IMPDH) for their uncontrolled growth and overexpress the type II isoform of the enzyme. The type I isoform, a "housekeeping" enzyme, is dominant in normal cells. We focus on synthesis of specific inhibitors of the type II isoform. Such compounds should show antileukemic effects without affecting normal cells that use the type I isoform.

Nicotinamide adenine dinucleotide (NAD), a small molecule cofactor, is crucial for IMPDH catalytic activity. We synthesized a number of cofactor analogues that bind at the IMP-dehydrogenase but cannot participate in the enzymatic activity, resulting in potent inhibition of the enzyme. Our mycophenolic adenine dinucleotide (MAD) analogues showed potent anti-CML activity in vitro and in a SCID mouse model but are not specific for either isoform. In collaboration with Dr. Barry Goldstein, we solved the crystal structure of the complex of IMP-MAD-IMPDH and found differences between the type I and type II isoforms at the cofactor binding domain. We now exploit these differences in structure-based design of the MAD analogue(s) that would be specific or highly selective against the type II of IMPDH.

CDD Pankiewicz, Krzysztof illustration

Shown on the right is the crystal structure of the Type II enzyme with C2-MAD and RMP bound, with an overlay of MPA and IMP from the structure of the hamster enzyme. The active site loop is shown in yellow. Key differences between Type I and Type II include the substitution of the three residues shown in light blue at the bottom left of the figure. In Type I IMPDH, His253 becomes Arg, Phe282 becomes Tyr, and Thr458 becomes Ile.

NAD Analogues as Potential Antibiotics

Isoniazid (INH), an old "first line" antibiotic against tuberculosis (TB), needs metabolic activation to form a covalent complex with NAD. This complex inhibits the enoyl-reductase, an enzyme involved in mycolic acid synthesis crucial for the growth of Mycobacterium tuberculosis. Recent studies have shown that multi-drug resistant TB strains (MDR-TB) do not activate INH to form such a complex. We are preparing NAD analogues that mimic the complex properties but do not require metabolic activation and therefore are expected to have therapeutic potential against MDR-TB.

Substantial differences between the NAD binding site of human IMPDH and IMPDH enzymes from other sources have been demonstrated. We are targeting these differences for designing inhibitors that will not affect the human enzyme. We design potential inhibitors against bacterial, fungal, and protozoan pathogens including S. pyogenes, P. carinii, C. parvum, and C. albicans.

Nucleosides, Nucleotides, and Mycophenolic Acid Analogues as Antiviral Agents

We continue our search for inhibitors of viral RNA-dependent RNA polymerases and Flaviviridae virus replication by synthesis of nucleosides and nucleotide analogues (such as phosphonates). We are also synthesizing analogs of mycophenolic acid (MPA) as potential inhibitors of RNA virus replication. MPA is one of the most potent agents against WNV.

Patents

  •  Pankiewicz KW, Kamerdyniak B, Chachula S. Synthesis of steroid 21-ester 9(11)-dehydro compounds from pregnane series of steroid 21-alcohols containing 11-?-hydroxyl group. Pol. 104189 (1979).
  • Pankiewicz KW, Kamerdyniak B. Sposob wytwarzania 9-?-fluoroprednisolonu octanu wysokiej czystosci. Pol.104190 (1979)
  • Stec WJ, Kinas R, Pankiewicz KW. Sposob wytwarzania 2-tlenku-2-[bis(2-chloroetylo)amino]-1-oksa-3-aza-3-fosfacykloheksanu (cyklofosfamidu) o czystosci optycznej. Pol. 100390 (1975)
  • Kinas R, Stec WJ, Pankiewicz KW. Verfarhen zur Herstellung von optisch aktivem 2-[bis(2-chloroethyl)amino]-1-oxa-2-aza-3-phospha-cyclo-hexanoxid-2. BRD Deutches Patentamt, Auslegesschrift DE 2644905 (1975)
  • Kinas R, Stec WJ, Pankiewicz KW. A method of preparing optically active 2-[bis(2-chlorethyl)amino]-1-oxa-2-aza-3-phosphahexane-2-oxide. Brit. Patent 1.553.984 (1976).
  • Kinas R, Pankiewicz KW, Stec WJ. Sposob wytwarzania optycznie czynnego 2-tleno-3-(2-chloroetylo)-2-[(2-chloroetylo)amino]-tetra-hydro-2H-1,2,3-oxazafosforinanu. Pol. 109108 (1977).
  • Pankiewicz KW, Kinas R, Boryczka S, Stec WJ. Sposob wytwarzania N.N',N"-trojetylenetiofosforamidu (THIO-TEPA). Pol. 116803 (1978)
  • Stec WJ, Kinas R, Pankiewicz KW. Sposob wytwarzania optycznie czynnych pochodnych 1,3,2-oksazafosforinanu. Pol. 119971 (1980)
  • Watanabe KA, Pankiewicz KW, Krzeminski J, Nawrot B. Synthesis of 2'-"up" fluorinated 2'-deoxy-arabinofuranosyl purines. US 5,525,720 (1996).
  • Watanabe KA, Pankiewicz KW, Goldstein BM, J.Ellis Bell. C-Nucleoside isosters of analogs thereof and pharmaceutical compositions. US 5,569,650 (1996).
  • Pankiewicz KW, Watanabe KA, Zatorski A. C-Nucleoside isostere of nicotinamide adenine dinucleotide, analogs thereof and use as anticancer agent. US 5,658,890 (1997).
  • Watanabe KA, Pankiewicz KW, Goldstein BM, J. Ellis Bell. Analogues of adenosine 5'-diphosphate and pharmaceutical compositions thereof. US 5,700,786 (1977).
  • Watanabe KA, Pankiewicz KW, Krzeminski J, Nawrot B. 2'-"Up" fluorinated 2'-deoxy-arabinofuranosylpurines. US 5,750,675 (1998)
  • Pankiewicz KW, Lesiak K, Watanabe KA. Tetraphosphonate bicyclic trisanhydrides. US6,326,490 (2001)
  • Stuyver L, Pankiewicz KW, Patterson K, Otto MJ, Watanabe KA. Antiviral agents for treatment of Flaviviridae Infection. WO 02/48165 A2
  • Pankiewicz KW, Lesiak K, Watanabe KA. Tetraphosphonate bicyclic trisanhydrides. US 6,713,623 (2004)
  • Pankiewicz KW, Chen L. Potent differentiation/apoptosis inducers as dual inhibitors of IMP dehydrogenase and histone deacetylases. US 60/952,800 (2007).
  • Pankiewicz KW, Felczak K, Chen L. Novel potent inhibitors of IMP-dehydrogenase, US60/956,730 (2007)
  • Mansky L, Patterson S, Pankiewicz KW. Novel combination therapy for viral infection. Docket Z08018 (2008)
  • Shi P-Y, Pankiewicz KW, Chen L, Felczak K. Methods and Compositions for Treating Flavivirus Infection, US 2011/212698 (2011)

Publications

  • Pankiewicz KW, Kamerdyniak B, Pieta S. Aromatyzacja pierscienia A prednisolonu w procesie mikrobiologicznej 1, 2-dehydratacji cortico-steronu. Aromatization of the A-ring of prednisolone during microbiological 1, 2-dehydration of corticosterone. Bull. Pharm. Inst. 1973, 12-15.
  • Kinas R, Pankiewicz K, Stec WJ. The synthesis of enantiomeric cyclophosphamides. Bull. Acad. Polon. Sci., Ser. Sci. Chim. 1975, 23, 981-984.
  • Kinas R, Pankiewicz K, Stec WJ, Farmer PB, Foster AB, Jarman M. Synthesis and absolute configuration of the optically active forms of 2-[bis(2-chloroethyl)amino]-4-methyl- tetrahydro-2H-1,3,2-oxaza-phosphorine 2-oxide. J. Org. Chem. 1977,42, 1650-1652.
  • Farmer PB, Jarman M, Facchinetti T, Pankiewicz K, Stec WJ. The metabolism and antitumor activity of the enantiomers of cis and trans 4-methylcyclophosphamide. Chem-Biol Interactions. 1977, 18, 47-57.
  • Cox PJ, Farmer PB, Foster AB, Griggs LJ, Jarman M, Kinas R, Pankiewicz K, Stec WJ. Application of deuterium labeling mass spectrometry in a study of the metabolism of the enantiomers of cyclophosphamide. Biomed Mass Spectrom. 1977, 4, 371-375.
  • Kinas R, Pankiewicz K, Stec WJ, Farmer PB, Foster AB, Jarman M. The synthesis of the optical isomers of 2-(2-chloroethylamino)-3-(2-chloroethyl)tetrahydro-2H-1,3,2-oxaza-phosphorine-2-oxide (isophosphamide). Bull Acad. Polon. Sci., Ser. Sci. Chim. 1978, 26, 39-42.
  • Milsted RA, Jarman M, Smyth JF, Kinas R, Pankiewicz K, Stec WJ. Comparative metabolism of cyclophosphamide and its enantiomers in humans. Proc. Am. Assoc. Cancer Res. 1978, 19, 50.
  • Stec WJ, Kinas R, Pankiewicz KW. Sposob wytwarzania optycznie czynnej pochodnej 1,2,3-oxazafosorinanu. Rocz. Chem.1978, 52, 659.
  • Jarman M, Milsted RA, Smyth JF, Kinas R, Pankiewicz K, Stec WJ. Comparative metabolism of 2-[bis(2-chloroethyl)amino]tetrahydro-2H-1,3,2-oxazaphosphorine-2-oxide (cyclophosphamide) and its enantiomers in humans. Cancer Res. 1979, 39, 2762-2767.
  • Pankiewicz K, Kinas R, Stec WJ, Foster AB, Jarman M, Van Maanen JMS. Synthesis and absolute configuration assignments of enantiomeric forms of ifosphamide, sulfosphamide, and trofosphamide. J. Am. Chem. Soc. 1979, 101, 7712-7718.
  • Adamiak DA, Gdaniec M, Pankiewicz K, Stec WJ. Absolute configuration of cancerostatic S(-)-isophosphamide. Angew. Chem. Int. Ed. Engl. 1980, 19, 549-550.
  • Misiura K, Pankiewicz K, Stec WJ, Jarman M. The synthesis of enantiomers of 4-ketocyclophosphamide. Experientia 1981, 37, 216-217.
  • Matsuda A, Chu CK, Reichman U, Pankiewicz K, Watanabe KA, Fox JJ. Nucleosides. 120. Synthesis of 2'-deoxypseudoisocytidine and 2'-deoxy-1-methyl pseudouridine from pseudouridine. J. Org. Chem. 1981, 46, 3603-3609.
  • Pankiewicz K, Matsuda A, Watanabe KA. Improved and general synthesis of 2'-deoxy-C-nucleosides. Synthesis of 5-(2-deoxy-D-erythropento-furanosyl)uracil, -1-methyluracil, -1,3-dimethyl-uracil, and -isocytosine. J. Org. Chem.1982, 47, 485-488.
  • Matsuda A, Pankiewicz K, Marcus BK, Watanabe KA, Fox JJ. Synthesis of 3-methylpseudouridine and 2'-deoxy-3-methylpseudouridine. Carbohydr. Res. 1982, 100, 297-302.
  • Pankiewicz KW, Watanabe KA. Nucleosides. 125. Synthesis of 5'-deoxy-5'-substituted-1,3-dimethylpseudouridines from 3',5'-O-(1,1,3,3-tetraisopropyldisiloxanyl)-1,3-dimethylpseudo-uridine. A novel isomerization reaction. Nucleic Acids Res. Symp. Series. 1982, 11, 9-12.
  • Misiura K, Okruszek A, Pankiewicz KW, Stec WJ, Czownicki Z, Utracka B. Stereospecific synthesis of chiral metabolites of ifosfamide and their determination in the urine. J. Med. Chem. 1982,26, 674-679.
  • Kinas R, Pankiewicz KW, Stec WJ. Sposob wytwarznia optycznie czynnych pochodnych 1,2,3-oksazafosforinanu. PT Chem. 1982, 12-15.
  • Tchorzewski H, Soszyniska W, Andrejewski W, Pankiewicz K, Stec WJ. Comparative study on immunosuppressive and lympholytic activity of optical isomers of cyclophosphamide. Arch. Immunol. Ther. Exp. 1983, 31, 329-333.
  • Pankiewicz KW, Matsuda A, Watanabe KA, Fox JJ. Selective methylation of the C-nucleoside, pseudoisocytidine and its 2'-deoxy analog. Synthesis of 1-methyl, 3-methyl, and 4-O-methyl derivatives. Tetrahedron 1984, 40, 33-38.
  • Pankiewicz KW, Hirota K, Matsuda A, Watanabe KA. Synthesis of pseudocytidine. Carbohydr. Res. 1984, 127, 227-233.
  • Watanabe KA, Su T-L, Pankiewicz KW, Harada K. Novel ring transformation reactions and their applications to the synthesis of potential anticancer heterocyclic compounds. Heterocycles 1984, 21, 289-307.
  • Pankiewicz KW, Watanabe KA, Takayanagi H, Itoh T, Ogura H. Synthesis of 2'-deoxy-2'-substituted- and 5'-deoxy-5'-substituted-pseudouridine derivatives. Crystalline and molecular structure of 2'-chloro-2'-deoxy-1,3-dimethyl-pseudouridine. Studies directed toward the synthesis of 2'-deoxy-2'-substituted-arabino nucleosides. 1. J. Heterocycl. Chem. 1985, 22, 1703-1710.
  • Pankiewicz KW, Watanabe KA. The synthesis of 5-(2-chloro-2-deoxy-ß-D-arabinofuranosyl)uracil. Reinterpretation of reaction of pseudouridine with ?-acetoxy-isobutyryl chloride. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. 2. Nucleosides Nucleotides 1985, 4, 613-624.
  • Pankiewicz KW, Kim J_H, Watanabe KA. Synthesis of 5-(2'-substituted-2'-deoxy-ß-D-arabinofuranosyl)-1-methyluracils from 1-methylpseudouridine. The first direct introduction of the 2'-substituent to C2' in the ''up'' configuration by nucleophilic reactions. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. 3. J. Org. Chem. 1985, 50, 3319-3322.
  • Pankiewicz KW, Nawrot BC, Watanabe KA. (Trifluoromethyl)sulfonyl (Triflyl) migration. Synthesis of 6,3'-anhydro-3-benzyl-1-(5-chloro-5-deoxy-ß-D-xylofuranosyl)barbituric acid from the 2'-trifluoro-methanesulfonate (triflate) of 6,5'-anhydro-3-benzyl-1-ß-D-ribo-furanosylbarbituric acid. J. Org. Chem. 1986, 51, 1525-1529.
  • Pankiewicz K, Matsuda A, Watanabe KA. 5-(1-ß-D-Ribofuranosyl) isocytosine. A large scale preparation of pseudoisocytidine, an antileukemic C-nucleoside from pseudouridine. In: Townsend, Tipson, eds. Nucleic Acid Chemistry: Improved and New Synthetic Procedures, Methods and Techniques. New York: Wiley and Sons, Inc,1986, 3, 89-90.
  • Kabat MM, Pankiewicz KW, Watanabe KA. Synthesis of 5-(ß-D-ribofuranosyl) nicotinamide and its N-methyl derivative. The isosteric and isoelectronic analogues of nicotinamide nucleoside. J. Med. Chem. 1987, 30, 924-927.
  • Heston WDW, Watanabe KA, Pankiewicz KW, Covey DF. Cytotoxic and non-cytotoxic N-alkyl derivatives of putrescine: effect on polyamine uptake and growth of prostatic cancer cells in vitro. Biochem. Pharmacol. 1987, 36, 1849-1852.
  • Pankiewicz KW, Nawrot B, Sochacka E, Watanabe KA. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. Nucleic Acids Res. Symp. Ser. 1987, 18, 257-260.
  • Pankiewicz KW, Watanabe KA. Synthesis of 5'- deoxy-5'-substituted-2,2'-anhydro-1-(ß-D-arabinofuranosyl)uracils. A new 2,5'- to 2,2'-anhydro-nucleoside transformation. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. (4). Chem. Pharm. Bull. 1987, 35, 4494-4497.
  • Pankiewicz KW, Watanabe KA. Some reactions of 2'-O-triflyl-2,3'-anhydroxylosyluracil with nucleophilic reagents. Synthesis of 2'-chloro-2',3'-dideoxy-uridinene. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. (5). Chem. Pharm. Bull. 1987, 35, 4498-4502.
  • Pankiewicz KW, Nawrot B, Gadler H, Price RW, Watanabe KA. 1-Methyl-5-(2-deoxy-2-fluoro-ß-D-arabino-furanosyl)-uracil, the C-nucleoside isostere of the potent antiviral agent 1-(2-deoxy-2-fluoro-ß-D-arabinofuranosyl)thymine (FMAU). Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. 6. J. Med. Chem. 1987, 30, 2314-2316.
  • Kabat MM, Pankiewicz KW, Sochacka E, Watanabe KA. Synthesis of 6-(ß-D-ribofuranosyl)picolinamide. A novel C-nucleoside from D-ribonolactone. Chem. Pharm. Bull. 1988, 36, 634-640.
  • Pankiewicz KW, Sochacka E, Kabat MM, Ciszewski LA, Watanabe KA. Efficient synthesis of 5-(ß-D-ribofuranosyl)nicotinamide and its ?-isomer. J. Org. Chem. 1988, 53, 3473-3479.
  • Nawrot B, Pankiewicz KW, Zepf RA, Watanabe KA. Synthesis and reactivity of benzyl 2-O-trifluoromethylsulfonyl- and benzyl 3-O-trifluoromethylsulfonyl-ß-D-ribofuranoside. The first evidence of trifluoromethylsulfonyl (triflyl) migration in carbohydrates. J. Carbohydr. Chem. 1988, 7, 95-114.
  • Pankiewicz KW, Kabat MM, Sochacka E, Ciszewski L, Zeidler J, Watanabe KA. C-Nucleoside analogues of nicotinamide mononucleotide (NMN). Nucleosides Nucleotides 1988, 7, 589-593.
  • Chen L-C, Su T-L, Pankiewicz KW, Watanabe KA. Synthesis of 2,5'-anhydro-2-thiouridine and its conversion to 3'-O- acetyl-2,2-anhydro-5'-chloro-5'-deoxy-2-thiouridine. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides (7). Nucleosides Nucleotides 1989, 8, 1179-1188.
  • Watanabe KA, Su T-L, Pankiewicz KW. Design and development of chemotherapeutic drugs. In: Yoshida Z, Shiba T, Ohshiro Y, eds. New Aspects of Organic Chemistry I. 1988 November 14-18; Kyoto, Japan. Tokyo: Kodansha, 1989, 453-497.
  • Sochacka E, Nawrot B, Pankiewicz KW, Watanabe KA. Synthesis of 1-methyl-5-(3-azido-2,3-dideoxy-ß-D-erythro pentofuranosyl)uracil and 1-methyl-5-(3-azido-2,3-dideoxy-2-fluoro-ß-D-arabinofuranosyl)uracil. The C-nucleoside isostere of 3'-azido-3'-deoxythymidine and its 2'-"up"-fluoro analogue. J. Med. Chem. 1990, 33, 1995-1999.
  • Krzeminski J, Nawrot B, Pankiewicz KW, Watanabe KA. Synthesis of 9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)hypoxanthine. The first direct introduction of a 2'-?-fluoro substituent in preformed purine nucleosides. Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. 8. Nucleosides Nucleotides 1991,10, 781-798.
  • Pankiewicz KW, Ciszewski LA, Ptak AT. Synthesis of 2,2'-anhydro-2-hydroxy- and 6,2'-anhydro-6-hydroxy-1-?-D-arabinofuranosylnicotinamide as conformationally restricted nicotinamide nucleoside analogs. Nucleosides Nucleotides 1991,10, 1333-1344.
  • Pankiewicz KW, Krzeminski J, Ciszewski LA, Ren W-Y, Watanabe KA. A synthesis of 9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)adenine and -hypoxanthine. An effect of C3'-endo to C2'-endo conformational shift on the reaction course of 2'-hydroxyl group with DAST. J. Org. Chem. 1992, 57, 553-559.
  • Pankiewicz KW, Krzeminski J, Watanabe KA. Synthesis of 2'-?-fluoro- and 3'-?-fluoro-substituted guanine nucleosides. Effects of sugar conformational shifts on nucleophilic displacement of the 2'-hydroxy and 3'-hydroxy group with DAST. J. Org. Chem. 1992, 57, 7315-7321.
  • Pankiewicz KW, Watanabe KA. 2'-?-Fluoro-substituted nucleosides via direct approach. J. Fluorine Chem. 1993, 64, 15-36.
  • Rosenberg I, Farras Soler J, Tocik Z, Ren W-Y, Ciszewski LA, Kois P, Pankiewicz KW, Spassova MK, Watanabe KA. Synthesis of oligo-nucleotides containing the C-nucleoside and 2'-deoxy-2'-fluoro nucleoside moieties by the H-phosphonate method. Nucleosides Nucleotides 1993, 12, 381-401.
  • Pankiewicz KW, Zeidler JM, Ciszewski LA, Bell JE, Goldstein BM, Jayaram HN, Watanabe KA. Synthesis of isosteric analogues of nicotinamide adenine dinucleotide (NAD) containing C-nucleotide nicotinamide and picolinamide. NAD analogues 1. J. Med. Chem. 1993,36, 1855-1859.
  • Zatorski A, Lipka P, Mollova N, Schram KH, Goldstein BM, Watanabe KA, Pankiewicz KW. Synthesis of thiazole-4-carboxamide adenine difluoromethylene diphosphonates substituted with fluorine at C2' of the adenosine. NAD analogues 2. Crabohydr. Res. 1993, 249, 95-108.
  • Pankiewicz KW, Watanabe, KA. A Synthesis of 2'-fluoro- and 3'-fluoro-substituted purine nucleosides by a direct approach. In: Nucleosides as Antitumor and Antiviral Agents, Chu CK, Baker DC. Eds. Plenum Press, New York, 1993, pp 55-71.
  • Zatorski A, Lipka P, Pankiewicz KW. Synthesis of thiazole-4-carboxamide adenine dinucleotide (TAD) analogues with an altered anhydride bridge. NAD analogues 3. Coll. Czech. Chem. Commun. 1993, 58, 122-126.
  • Goldstein BM, Li H, Jones JP, Bell JE, Zeidler JM, Pankiewicz KW, Watanabe KA. C-NAD: A Potent and specific inhibitor of alcohol dehydrogenase. J. Med. Chem.1994, 37, 392-399.
  • Li H, Hallows WA, Punzi JS, Marquez VE, Carrell HL, Pankiewicz KW, Watanabe KA, Goldstein BM. Crystallographic studies of two alcohol dehydrogenase bound analogues of thiazole-4-carboxamide adenine dinucleotide (TAD), the active anabolite of the antitumor agent tiazofurin. Biochemistry 1994, 33, 23-32.
  • Li H, Hallows WH, Punzi JS, Pankiewicz KW, Watanabe KA, Goldstein BM. Crystallographic studies of isosteric NAD analogues bound to alcohol dehydrogenase: Specificity and substrate binding in two ternary complexes. Biochemistry 1994,33, 11734-11744.
  • Pankiewicz KW, Zatorski A, Watanabe KA. The chemistry of NAD analogues. NAD analogues 6. Nucleic Acid Symp. Ser. 1994,31, 139-142.
  • Zatorski A, Goldstein BM, Colby TD. Jones JP, Pankiewicz KW. Potent inhibitors of human inosine monophosphate dehydrogenase type II; Fluorine-substituted analogues of thiazole-4-carboxamide adenine dinucleotide. NAD analogues 4. J. Med. Chem. 1995,38, 1098-1105.
  • Lipka P, Zatorski A, Watanabe KA, Pankiewicz KW. Synthesis of methylene-bridged analogues of nicotinamide riboside, nicotinamide mononucleotide, and nicotinamide adenine dinucleotide. NAD analogues 5. Nucleosides Nucleotides 1996, 15, 149-167.
  • Pankiewicz KW, Zatorski A, Watanabe KA. NAD analogues as potential anticancer agents: Conformational restrictions as basis for selectivity. NAD analogues 9. Acta. Biochimca. Polonica.1996,43, 183-193.
  • Zatorski A, Watanabe KA, Carr, SF, Goldstein, BM, Pankiewicz KW. The chemical synthesis of benzamide adenine dinucleotide: Inhibition of inosine monophosphate dehydrogenase (type I and II). NAD analogues 7. J. Med. Chem.1996, 39, 2422-2426.
  • Pankiewicz KW, Lesiak K, Zatorski A, Watanabe KA. Synthesis of methylenebis-phosphonate analogues of ADP-ribose. NAD analogues 8. Coll. Czech. Chem. Commun.1996, 61, 92-95.
  • Pankiewicz KW, Lesiak K, Zatorski A, Goldstein BM,. Carr, SF, Sochacki M, Majumdar A, Seidman M, and Watanabe KA. The practical synthesis of methylenebisphosphonate analogue of benzamide adenine dinucleotide. Inhibition of human inosine monophosphate dehydrogenase (type I and II). NAD analogues 10. J. Med. Chem. 1997,40, 1287-1291.
  • Pankiewicz KW, Lesiak K, Watanabe KA. Efficient synthesis of methylenebis(phosphonate) analogues of P1, P2-disubstituted pyro-phosphates of biological interest. A novel plausible mechanism. J. Am. Chem. Soc. 1997, 119, 3691-3695.
  • Lesiak K, Watanabe KA, Majumdar A, Seidman M, Goldstein BM, Pankiewicz KW. Synthesis of non-hydrolyzable analogues of thiazole-4-carboxamide- and benzamide-adenine dinucleotide containing fluorine atom at the C2' of adenine nucleoside. Induction of K562 differentiation and IMPDH inhibitory activity. NAD analogues 11. J. Med Chem. 1997, 40, 2533-2538.
  • Pankiewicz KW. NAD analogues designed as potential anticancer agents. Quest for selective inhibition of inosine monophosphate dehydrogenase (IMPDH). NAD analogues12. Pharmacol. Ther. 1997, 76, 89-100.
  • Luyten I, Pankiewicz KW, Watanabe KA, Chattopadhyaya J. The determination of the tautomeric equlibrium of pseudouridine in the basic solution. J. Org. Chem. 1998, 63, 1033-1040.
  • Lesiak K, Watanabe KA, George J, Pankiewicz KW. 2-(4-Nitrophenyl)ethyl methylene-bis(phosphonate): A Versatile reagent for the synthesis of nucleoside 5'-methylene-bis(phosphonate)s. J. Org. Chem.1998, 63, 1906-1909.
  • Lesiak K, Watanabe KA, Pankiewicz KW. Synthesis of 2'-deoxy-nucleoside 5'-methylenebis(phosphonate)s using 2-(4-nitrophenyl)ethylmethylenebis(phosphonate) as the phosphonylating agent. Nucleosides Nucleotides1998, 17, 1857-1860.
  • Lesiak K, Watanabe KA, Majumdar A, Powell J, Seidman M, Vanderveen K, Goldstein BM, Pankiewicz KW. The Synthesis of methylenebis(phosphonate) analogue of mycophenolic adenine dinucleotide. A Glucuronidation resistant MAD analogue of NAD. NAD analogues 13. J. Med. Chem. 1998, 41, 618-622.
  • Pankiewicz KW, Lesiak K. Novel mycophenolic adenine bis(phosphonate)s as potent anticancer agents and inducers of cells differentiation. NAD analogues16. Nucleosides Nucleotides 1988, 18, 927-932.
  • Gibson ES, Lesiak K, Watanabe KA, Gudas LJ, Pankiewicz KW. Synthesis of a novel C-nucleoside,2-amino-7-(2-deoxy-?-D-erythro-pentofurano-syl)-3H,5H-pyrrolo-[3,2-d]-pyrimidin-4-one.(2'-deoxy-9-deazaguanosine). Nucleosides Nucleotides 1999, 18, 363-376.
  • Lesiak K, Pankiewicz KW. Synthesis of methylenebis(phosphonate) analogues of nucleotide coenzymes and other biologically important pyrophosphates. A novel coupling mechanism. NAD analogues 14. Phosphorus, Sulfur Silicon Relat. Elem. 1999, 671-674.
  • Pankiewicz KW. Inhibitors of inosine monophosphate dehydrogenase as potential chemo-therapeutic agents. NAD analogues 15. Expert Opin. Ther. Pat. 1999, 9, 55-65.
  • Stivers JT, Pankiewicz KW, Watanabe KA. Kinetic mechanism of damage site ecognition and uracil flipping by Escherichia coli uracil DNA glycosylase. Biochemistry 1999, 38, 952-963.
  • Pankiewicz KW. Inosine monophosphate dehydrogenase as a target for structure- and mechanism-based drug design. Current Med. Chem. 1999, 6, 578
  • Pankiewicz KW, Malinowski K, Jayaram, HN, Lesiak-Watanabe K, Watanabe KA. Novel mycophenolic adenine bis(phosphonate)s as potential immunosuppressants. NAD analogues 17. Current Med. Chem. 1999, 6, 629.
  • Drohat A, Xiao G, Tordova M, Jagadesh J, Pankiewicz KW, Watanabe KA, Gilliland GL, Stivers J.T. Heteronuclear NMR and crystallographic studies of wild-type and H187Q Escherichia coli uracil DNA glycosylase: Electrophylic catalysis of uracil expulsion by a neutral histidine 187. Biochemistry 1999, 38, 11876-11886.
  • Pankiewicz KW. Fluorinated nucleosides. Carbohydr. Res. 2000, 327, 87-99.
  • Dong J, Drohat AC, Stivers, JT, Pankiewicz KW, Carey PR. Raman spectroscopy of uracil DNA glycosylase-DNA complexes: Insights into DNA damage recognition and catalysis. Biochemistry 2000, 39, 13241-13250.
  • Pankiewicz KW. Inhibitors of inosine monophopshate dehydrogenase as potential chemotherapeutic agents. Update Expert Opin. Ther. Pat. 2001, 11, 1061-1070.
  • Pankiewicz KW, Goldstein BM. The chemistry of nucleoside and dinucleotide inhibitors of Inosine Monophosphate Dehydrogenase (IMPDH). NAD analogues 18 – Recent Advances in Nucleosides: Chemistry and Chemotherapy, Chu, C.K. Ed., Elsevier Science 2002, 71-90.
  • Pankiewicz KW, Lesiak-Watanabe KB, Watanabe, Patterson S, KA, Jayaram HN, Yalowitz JA, Miller MD, Seidman M, Majumdar A, Prehna G, Goldstein BM. Novel mycophenolic adenine bis(phosphonate) analogues as potential differentiation agents against human leukemias. NAD analogues 20. J. Med. Chem. 2002, 45, 703-712.
  • Pankiewicz KW, Watanabe KA, Lesiak-Watanabe K, Goldstein BM, Jayaram HN. The Chemistry of nicotinamide adenine dinucleotide (NAD) analogues containing C-nucleosides related to nicotinamide riboside. NAD analogues 21. Curr. Med. Chem. 2002, 9, 733-741.
  • Yalowitz JA, Pankiewicz KW, Patterson SE, and Jayaram HN. Cytotoxicity and Cellular Differentiation Activity of Methylenebis(phosphonate) Analogs of Mycophenolic Acid Adenine Dinucleotide in Human Cell Lines. Cancer Lett. 2002, 181, 31-38
  • Clark JL, Patterson SE, Mason JC, Otto MJ, Schinazi RF, Watanabe KA, Risal D, Goldstein BM, Pankiewicz KW. Novel inhibitors of inosine monophosphate dehydrogenase (IMPDH). Collect. Czech Chem. Commun. Symp. Ser. 2002, 5, 256-260
  • Pankiewicz KW, Goldstein BM. Inosine monophosphate dehydrogenase and its inhibitors. An overview. NAD analogues 19. Inosine Monophosphate Dehydrogenase A Major Therapeutic Target, Pankiewicz KW, Goldstein BM Eds., ACS Symposium Series No. 839, 2003, 1- 20.
  • Jayaram HN, Yalowitz, JA. Krupitza G, Szekeres T, Krohn K, Pankiewicz KW. Studies with benzamide riboside, a recent inhibitor of inosine 5’-monophosphate dehydrogenase. Inosine Monophosphate Dehydrogenase A Major Therapeutic Target. Pankiewicz KW, Goldstein BM, Eds., ACS Symposium Series No. 839, 2003, 231-247.
  • Pankiewicz KW, Patterson SE, Jayaram, HN, Goldstein. Cofactor analogues as inhibitors of IMP dehydrogenase; design and new synthetic approaches. Inosine Monophosphate Dehydrogenase A Major Therapeutic Target, Pankiewicz KW, Goldstein BM Eds., ACS Symposium Series No. 839, 2003, p.247-282.
  • Stuyver LJ, Lostia S, Patterson SE, Watanabe KA, Otto MJ, Pankiewicz KW. Inhibitors of the IMPDH enzyme as potential anti-bovine viral diarrhea virus agents. Antiviral Chem. Chemother. 2003,13, 345-352.
  • Hollecker L, Du J, Hassan A, Shi J, Wang P, Patterson SE, Khan N, Hobs A, Clark J, Rachakonda S, Chun BK, Pinar I, Lostia S, McBrayer T, Stuyver LJ, Otto MJ, Pankiewicz KW. Synthesis and antiviral activity of a mutagenic N4-hydoxycytidine and its analogues. Developments in Nucleic Acids, Schinazi RF, Liotta D. eds. IHL Press, 2004, p.319-337.
  • Patterson SE, Black PL, Clark JL, Risal D, Goldstein BM, Jayaram HN, Schinazi RF, Pankiewicz KW. The mechanism of action and antileukemic activity of bis(phosphonate) analogue of mycophenolic adenine dinucleotide (C2-MAD); An alternative for tiazofurin? Developments in Nucleic Acids, Schinazi RF, Liotta D. eds. IHL Press, 2004, p.447-456.
  • Patterson SE, Clark JL, Mason JC, Pankiewicz KW The reaction of alcohols and nucleosides with methylenebis(phosphonic acid dichloride): Facile synthesis of methylenebis-(phosphonic acid) monoesters. Developments in Nucleic Acids Acids, Schinazi RF, Liotta D. eds. IHL Press, 2004, p.
  • Pankiewicz KW, Patterson SE, Black PL, Jayaram HN, Risal D, Goldstein BM, Stuyver LJ, Schinazi RF., Cofactor Mimics as Selective Inhibitors of NAD-dependent Inosine Monophosphate Dehydrogenase (IMPDH). Curr. Med. Chem. 2004, 11, 887-900
  • Stuyver LJ, McBrayer TR, Tharnish PM, Hassan AEA, Chu CK, Pankiewicz KW, Watanabe KA, Schinazi RF, Otto MJ. Dynamics of subgenomic HCV levels in Huh-7 cells after exposure to nucleotide antimetabolites. J. Virol. 2003, 77, 10689-10694
  • Wang P, Hollecker L, Pankiewicz KW, Patterson SE, Whitaker T, McBrayer TR, Tharnish PM, Sidwell RW, Stuyver LJ, Otto MJ, Schinazi RF, Watanabe KA. Synthesis of N3,5’-cyclo-4-(?-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one, a novel compound with potential anti-hepatitis C virus activity. J. Med. Chem. 2004, 47, 6100.
  • Shi J, Du J, Ma T, Pankiewicz KW, Patterson SE, Tharnish PM, McBrayer TR, Stuyver LJ, Otto MJ, Chu CK, Schinazi RF, Watanabe KA. Synthesis and anti-viral activity of a series of D- and L-2’-deoxy-2’-fluororibonucleosides in the subgenomic HCV replicon system. Bioorg. Med. Chem. 2005, 13, 1641–1652.
  • Clark JL, Hollecker L, Mason JC, Stuyver LJ, Tharnish PM, Lostia S, McBrayer TR, Schinazi RF, Watanabe KA, Otto MJ, Furman PA, Stec WJ, Patterson SE, Pankiewicz KW. Design, synthesis, and antiviral Activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. J. Med. Chem. 2005, 48, 5504-5508.
  • Chun B-K, Clark J, Du J, Furman PA, Hassan AE, Hollecker L, McMrayer T, Otto ME, Pankiewicz, KW, Patterson SE, Rachakonda S, Schinazi RF, Stuyver J, Wang PW, Watanabe KA, Whitaker T. 5’,9-Anhydro-3-(?-D-ribofuranosyl)purine nucleoside analogues as potential anti-HCV agents. Coll. Czech. Chem. Commun. Symp. Ser. 2005, 7, 319-327.
  • Wang P, Hollecker L, Pankiewicz KW, Patterson SE, Whitaker T, McBrayer TR, Tharnish PM, Stuyver LJ, Schinazi RF, Otto MJ, Watanabe KA. Synthesis of N3,5'-cyclo-4-(?-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one and its 3'-deoxysugar analogue as potential anti-hepatitis C virus agents. Nucleosides Nucleotides Nucleic Acids 2005, 24, 957-60.
  • Shi J, Du J, Ma T, Pankiewicz KW, Patterson SE, Hassan AE, Tharnish PM, McBrayer TR, Lostia S, Stuyver LJ, Watanabe KA, Chu CK, Schinazi RF, Otto MJ. Synthesis and in vitro anti-HCV activity of ?-D- and 1-2'-deoxy-2'-fluororibonucleosides. Nucleosides, Nucleotides Nucleic Acids 2005, 24, 875-879.
  • Chen L, Rejman D, Bonnac L, Pankiewicz K, Patterson SE. Nucleoside-5'-phosphoimidazolides: Reagents for facile synthesis of dinucleotide pyrophosphates. Current Protocols in Nucleic Acid Chemistry, Beaucage SL, Bergstrom DE, Herdewijn P, Matsuda A, eds. Wiley & Sons, 2005, p.13.4.1 -13.4.10
  • Pankiewicz KW, Gao G, Patterson SE. Synthesis of methylenebis(phosphonate) analogues of dinucleotide pyrophosphates and other P1 , P2- methylenebis(phosphonate) diesters from methylenebis-(phosphonate) monoesters. Current Protocols in Nucleic Acid Chemistry Beaucage SL, Bergstrom DE, Herdewijn P, Matsuda A, eds. Wiley & Sons, 2006, p. 13.5.1 -13.5.13
  • Rejman D, Olesiak M, Chen L, Patterson SE, Wilson D, Jayaram HN, Hedstrom L, Pankiewicz KW. Novel methylenephosphophosphonate analogues of mycophenolic adenine dinucleotide Inhibition of Inosine Monophosphate Dehydrogenase. J. Med. Chem. 2006, 49, 5018-22
  • Bonnac LF, Gao G, Chen L, Patterson, SE, Jayaram HN, Pankiewicz KW. Efficient synthesis of benzamide riboside, a potential anticancer agent. Nucleosides, Nucleotides Nucleic Acids 2007, 26, 1249-53
  • Suk D-H, Bonnac LF, Dykstra CC, Pankiewicz, KW, Patterson SE. Rational design and synthesis of novel ant-Girardia agents. Bioorg. Med. Chem. Lett. 2007, 17, 2064-67.
  • Suk D-H, Rejman D, Dykstra CC, Pohl R, Pankiewicz KW, Patterson SE. Phosphonoxins: Rational Design and Discovery of a Potent Nucleotide Anti-Giardia Agent. Bioorg. Med. Chem. Lett. 2007, 17, 2811-2816.
  • Bonnac LF, Chen L, Pathak R, Gao G, Ming Q, Bennet E, Felczak K, Kullberg M, Patterson SE, Mazzola F, Magni G, Pankiewicz KW. Probing binding requirements of NAD kinase with modified substrate (NAD) analogues. Bioorg. Med. Chem. Lett. 2007, 17, 1512-1515.
  • Chen L, Gao G, Bonnac L, Wilson D, Bennett E, Jayaram HN, Pankiewicz KW. Methylenebis(sulfonamide) linked Nicotinamide Adenine Dinucleotide analogue as an IMP-dehydrogenase inhibitor. Bioorg. Med. Chem. Lett. 2007, 17, 3152-55.
  • Bonnac L, Gao G, Chen L, Felczak K, Bennett EM, Tonge P, Tonge, Pankiewicz KW. Synthesis of 4-phenoxybenzamide adenine dinucleotide as NAD analogue with inhibitory activity against enoyl-ACP reductase (InhA) of Mycobacterium tuberculosis. Bioorg. Med. Chem. Lett. 2007,17, 4588-91.
  • Pankiewicz KW, Chen L. Recent development of IMP-dehydrogenase inhibitors for the treatment of cancer. Curr. Opin. Drug Disc. Develop. 2007, 10, 403-12.
  • Chen L, Gao G, Felczak K, Bonnac L, Patterson SE, Wilson D, Jayaram HN, Hedstrom L, Pankiewicz KW. Probing binding requirements of type I and type II isoforms of IMP-dehydrogenase with adenine modified NAD analogues. J. Med. Chem. 2007, 50, 5743-51
  • Chen L, Wilson D, Jayaram HN, Pankiewicz KW. Dual inhibitors of Inosine Monophosphate Dehydrogenase and Histone Deacetylases for cancer treatment. J. Med. Chem. 2007, 50, 6685-91.
  • Chen L, Petrelli R, Felczak K, Gao G, Bonnac L, Yu JS, Bennett EM, Pankiewicz KW. Nicotinamide adenine dinucleotide based therapeutics. Curr. Med. Chem. 2008, 15, 650-670.
  • Chen L, Petrelli R, Felczak K, Olesiak M, Bennet EM, Magni G, Pankiewicz KW. Novel cofactor-type inhibitors of NAD-dependent enzymes. NAD-based therapeutics. Coll. Czech Chem. Commun. Symp. Series. 2008, 10, 71-79.
  • Chen L, Petrelli R, Olesiak M, Wilson DJ, Labello NP, Pankiewicz KW. Bis(sulfonamide) Isosters of Mycophenolic Adenine Dinucleotide Analogues. Inhibition of Inosine Monophosphate Dehydrogenase. Bioorg. Med. Chem. 2008, 16, 462-9
  • Chen L, Wilson DJ, Labello NP, Jayaram HN, Pankiewicz KW. Mycophenolic acid analogues with a modified metabolic profile. Bioorg. Med. Chem. 2008, 16, 9340-45
  • Zou G, Puig-Basagoiti F, Zhang B, Qing M, Chen L, Pankiewicz KW, Felczak K, Yuan Z, and Shi P-Y. A single-amino acid substitution in West Nile virus 2K peptide between NS4A and NS4B confers resistance to lycorine, a flavivirus inhibitor. Virology 2009,384, 242-252
  • Ju S, McLennan G, Bennett SL, Liang Y, Bonnac L, Pankiewicz KW, Jayaram HN. Technical aspects of imaging and transfemoral arterial treatment of N1-S1 tumors in rats: an appropriate model to test the biology and therapeutic response to transarterial treatments of liver cancers. J. Vasc. Interv. Radiol. 2009, 20, 410-4.
  • Petrelli R, Liqiang Chen L, Felczak K, Sham Y, Bennett EM, Cappellacci L, Franchetti P, Grifantini M, Mazzola F, Di Stefano M, Magni G, and Pankiewicz KW. Selective inhibition of nicotinamide adenine dinucleotide kinases by dinucleoside disulfide mimics of nicotinamide adenine dinucleotide analogues. Bioorg. Med. Chem. 2009, 17, 5656-64.
  • Sun XE, Sharling L, Muthalagi M, Mudeppa DG, Pankiewicz KW, Felczak K, Rathod PK, Mead J, Striepen B, Hedstrom L. Prodrug activation by Cryptosporidium thymidine kinase. J. Biol. Chem. 2010, 285, 15916-22.
  • Chen L, Wilson DJ, Xu Y, Aldrich CC, Felczak K, Sham YY, Pankiewicz KW. Triazole-linked inhibitors of inosine monophosphate dehydrogenase from human and Mycobacterium tuberculosis. J. Med. Chem. 2010, 53, 4768-78.
  • Chen L, Petrelli R, Gao G, Wilson DJ, McLean GT, Jayaram HN, Sham YY, Pankiewicz KW. Dual Inhibitors of Inosine Monophosphate Dehydrogenase and Histone Deacetylases Based on a Cinnamic Hydroxamic Acid Core Structure.Bioorg. Med. Chem. 2010, 18,5950-64.
  • Pankiewicz KW. NAD and its Role in Biology and Medicine. Curr. Med. Chem. 2011, 18, 1890.
  • Felczak K, Chen L, Wilson D, Williams J, Vince R, Petrelli R, Jayaram HN, Kusumanchi P, Kumar M, Pankiewicz KW. Cofactor-type inhibitors of inosine monophosphate dehydrogenase via modular approach: targeting the pyrophosphate binding sub-domain. Bioorg. Med. Chem. 2011, 19, 1594-605.
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  • Pankiewicz KW, Felczak K. Rehab of NAD(P)-Dependent Enzymes with NAD(P)-Based Inhibitors. Curr. Med. Chem.2011, 18, 1891-908.
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  • Felczak K and Pankiewicz KW. Rehab of NAD-dependent enzymes with NAD-based inhibitors; synthesis of methylene-bis(phosphonate) analogues of pyridone-3-carboxamide adenine dinucleotides. Coll. Czech Chem. Commun. Symp. Ser. 2011, 11, 71-79.
  • Felczak K, Chen L, Wilson D, Williams J, Vince R, Petrelli R, Jayaram HN, Kusumanchi P, Kumar M, Pankiewicz KW. Cofactor-type inhibitors of inosine monophosphate dehydrogenase via modular approach: targeting the pyrophosphate binding sub-domain. Bioorg. Med. Chem. 2011, 19, 1594-605.
  • Pankiewicz KW, Felczak K. Rehab of NAD(P)-Dependent Enzymes with NAD(P)-Based Inhibitors. Curr. Med. Chem.2011, 18, 1891-908.
  • Felczak K and Pankiewicz KW. Synthesis of methylenebis(phosphonate) analogues of 2,4,6, -pyridones of NAD.Nucleosides Nucleotides Nucleic Acids 2011, 7-8, 512-23.
  • MacPherson I, Temme J, Habeshian S, Felczak K, Pankiewicz KW, Hedstrom L, Krauss Isaac.A Tool for the Evolution of Modified DNA Aptamers: Application to HIV Glycocluster Antigen Design. Angew. Chem. Int. Ed. 2011, 50, 11238-42.
  • Roussel B, Johnson-Farley N, Kerrigan JE, Scotto KW, Banerjee D, Felczak K, Pankiewicz KW, Gounder M, Lin HX, Abali EE, et al A Second Target of Benzamide Riboside: Dihydrofolate Reductase. Cancer Biol. Therap. 2012, 13, 1290-98.