Director

CURRICULUM VITAE

VALERY V. ANTONENKO, PH.D.

***** *** ***** *****, *********, CA 95014

408-***-**** (home), 650-***-**** (cell)

***@***.***

EDUCATION

**** **.*. ********** *********. Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry (“Ivy League” of the Soviet Union), Russian Academy of Sciences, Moscow, Russia

1983 M. S. (Summa Cum Laude) in Chemistry of Natural Products and Pharmaceutical Chemistry. Mechnikov University, Odessa, USSR

PROFESSIONAL EXPERIENCE

2/2010–08/2011 Threshold Pharmaceuticals, Inc. Redwood City, CA. Research Fellow, Anti-cancer Drug Discovery. Regulatory Affairs Trainee.

2006 – 09/2009 NovoStem Therapeutics, Inc. Memphis TN, Cupertino, CA. Director, Cancer Stem Cells Pan Pharma Drug Discovery Platform.

2003 – 2006 Johnson & Johnson Pharmaceuticals, Mountain View, CA. Senior Research Fellow/Director.

2001 – 2003 ArQule, Inc., Woburn, Massachusetts. Director of Medicinal Chemistry.

1992 – 2001 GlaxoSmithKline (Affymax Research Institute), Palo Alto, California. Research Fellow/Associate Director, Head of High-Throughput Medicinal Chemistry.

1990 - 1992 University of California at San Diego, Laboratories of Professor Murray Goodman, La Jolla, California. Senior Visiting Scientist. Scientific Advisor to Affymax Research Institute.

1983 - 1990 Shemyakin Institute of Bioorganic Chemistry, National Academy of Sciences, Moscow, Russia

1988-90 – Project Leader, Chemistry of Immunomodulators

1987-88 – Research Scientist. Laboratory of Natural Products and Peptide Chemistry.

1983-87 – Graduate Student. Laboratory of Natural Products and Peptide Chemistry. Scientific advisor: Professor Vadim T. Ivanov, D. Sc., Member of the Russian Academy of Sciences, Director, Chairman, Department of Physico-Chemical Biology of the Russian Academy of Sciences

1979 - 1983 A. V. Bogatsky Physico-Chemical Institute, Department of CNS-Active Compounds, National Academy of Sciences, Odessa, USSR, RA (part time)

VALERY V. ANTONENKO

PROFESSIONAL ACTIVITIES

Member New Product Development Committee, JNJ (ALZA Corporation) (2003-2006)

Member, ArQule Portfolio Management Committee (2001-2002)

Chairman, GlaxoWellcome Lead Discovery 2000 Automation Committee (1998-2000)

Member, Editorial Board of the Series “Solid Phase Organic Syntheses” (1998-present)

Member, GW-ARI Technology Evaluation Committee (1998-2000)

Member, GW-ARI Chemistry Coordination Committee (1998-2000)

Member, Glaxo-Wellcome International Committee on Combinatorial Technologies (1997-2000)

RESEARCH SUMMARY

Threshold Pharmaceuticals, Inc.

• Design and synthesis of hypoxia-activated anti cancer drugs and pro-drugs

• Prepare for RAC certification exam

• Assist in SOP development, review and initiation

• Assist in monitoring and reporting project timelines

• Organize materials from preclinical and clinical studies for review and assist in review process

• Compile and organize materials for pre submission reports

• Assist in the preparation of routine reports and regulatory agency communications

• Assist in the preparation of postmarket reports and submissions

• Design and synthesis of hypoxia-activated anti cancer drugs and pro-drugs

NovoStem Therapeutics, Inc.

• Fund-raising for the company

• Established drug discovery programs in the area of cancer stem cells

• Designed compounds with anti cancer stem cell activity

Johnson & Johnson Pharmaceuticals

• Created new pharmaceutical product concepts for commercialized small molecule drugs based on ALZA drug delivery and formulation technologies overcoming drug resistance, enhancing intestinal absorption, bioavailability and a PK-profile.

• Selected early-stage J&J molecules (pre-GLP-Tox through Phase 2) as candidates for drug delivery based products.

• Carried out research in the area of colonic absorption of drugs (inter-species correlations, influence of structure and physico-chemical properties).

• Studied potential benefits of targeting drug-delivery options at earlier stages of drug discovery and development.

• Established a prodrug program aimed at enhancing colonic and intestinal absorption of known drugs utilizing active transport mediated by transporters expressed in human intestinal tissue.

ArQule, Inc.

• Initiated and carried out drug discovery programs in inflammation based on high-throughput combinatorial synthesis.

VALERY V. ANTONENKO

• Co-lead drug rescue initiative (application of combinatorial synthesis and predictive ADME technologies to overcome deficiencies in known drugs and to identify early potential problems with compounds in different stages of the discovery process).

• Co-managed ArQule’s drug discovery portfolio and combinatorial synthesis collaborations.

Affymax Research Institute.

• Created high-throughput medicinal chemistry program.

• Developed and applied novel technologies for improving the pace of hit identification and lead optimization. Primary drug discovery targets: SERMs, nuclear receptors. Exploratory discovery programs: antimicrobial, inhibitors of MMPs, Collagenase 1 and PTPs.

• Developed chemical aspects (i.e., highest-yielding reaction conditions, orthogonal side-chain protection strategies, required for UV-induced deprotection, novel photo-cleavable protecting groups, reproducible methods of surface derivatization to achieve optimal loading, surface density and detection using confocal microscopy) of light-directed synthesis of high-density peptide and peptidomimetic microarrays on UV-transparent flat surfaces. Applied the technology to discover sub-nanomolar inhibitors of IL-I.

• Developed novel technologies for high-speed solid- and solution-phase parallel and combinatorial synthesis: HiTOPS, GNOME, PHOENIX, CAS.

• Licensed high-throughput synthesis technologies to Yamato Corporation, Japan.

UCSD. Laboratories of Professor Murray Goodman

• Focused on rational drug design and synthesis of peptidomimetics with enhanced stability toward proteolytic enzymes.

• Synthesized novel unnatural amino acids (pyroglutamate and proline mimetics) and peptide analogs (morphiceptin, enkephalin, and TRH) with amide bond surrogates.

Shemyakin Institute of Bioorganic Chemistry

• Synthesized immunoactive compounds derived from natural sources (bone marrow extract) and their analogs.

• Synthesized agonists and antagonists of Transforming Growth Factor α and Epidermal Growth Factor.

• Carried out solid-phase synthesis of magainin and its analogs with enhanced enzymatic stability and antimicrobial activity.

• Studied the shelf-stability of delta sleep inducing peptide (DSIP).

• Developed formulations of DSIP for intranasal administration.

Ph. D. Program (Shemyakin Institute of Bioorganic Chemistry USSR Academy of Sciences)

• Synthesized in solution linear and cyclic fragments of oncoproteins sis, fos, and myc.

• Developed synthetic methodology for a loading-controlled site-specific conjugation of the oncoprotein fragments to carrier-proteins such as KLH and albumins.

• Prepared synthetic immuno-constructs of oncoprotein fragments with N-acetyl muramyl dipeptides and N-acetylglucosaminyl-N-acetylmuramyl dipeptide (GMDP).

• Studied levels of expression (and their prognostic value) of the oncoproteins sis, fos, and myc in human normal and primary cancer tissues, and metastases

Physico-Chemical Institute

• Carried out enzymatic peptide synthesis of TRH.

• Synthesized unnatural amino acids, membrane-active aza-crown ether-containing peptide and amino acid analogs, and analogs of TRH.

VALERY V. ANTONENKO

• Synthesized derivatives of amphetamines, anxiolytics of the 1,4-benzodiazepine family, and 1,4,5-benzotriazocines.

• Participated in the development of Phenazepam, new and approved by the USSR equivalent of the US’ FDA 1,4-benzodiazepine tranquilizer.

MAJOR PUBLICATIONS AND PATENTS

Antonenko, V., Ashwell, M., Ali, S., Liu, J., Liu, Y., Lohse, P., Mekonnen, B., Selliah, R., Tandon, M., Wrona, W. Inibitors of p38 and methods of using the same PCT WO 2004

Antonenko, V. Parallel Synthesis. In Houben-Weil Methods of Organic Chemistry, v. E 22 a, Ed. Board Büchel, K. H. …; Georg Thieme Verlag : Stuttgart, 2002

Campbell, D. A.; Antonenko, V. V.; Selick, H. E.; Gavin, R. M.; Ida, S.; Muir, A. H. Systems and Methods for Solid-Phase Parallel Synthesis of a Combinatorial Collection of Compounds. U.S. Patent 6168914, 2001.

Antonenko, V. V.; Kulikov, N. V. Chemical Synthesizers. U.S. Patent 6149869, 2000.

Antonenko, V. V.; Kulikov, N. V.; Jacobs, J. W. Systems and Methods for Parallel Synthesis of Organic Compounds. U.S. Patent 6117397, 2000.

Campbell, D. A.; Antonenko, V. V.; Selick, H. E. System and Method for Solid-Phase Synthesis of a Combinatorial Collection of Compounds. U.S. Patent 6083682, 2000.

Antonenko, V. V.; Kulikov, N. V. Methods for Parallel Synthesis of Organic Compounds.

U.S. Patent 6051439, 2000.

Antonenko, V. V.; Kulikov, N. V.; Jacobs, J. W. System for Parallel Synthesis of Organic Compounds. U.S. Patent 6042789, 2000.

Antonenko, V. V.; Mortezaei, R.; Kulikov, N. V. In New Trends in Synthetic Medicinal Chemistry; Gualtiery, F., Ed.; Methods and Principles in Medicinal Chemistry; Wiley-VCH: Weinheim, 2000; Vol. 7, Chapter 3, Combinatorial Chemistry.

Antonenko, V. V. In Combinatorial Chemistry and Technology: Principles, Methods, and Applications; Mierus, G.; Fassina, G., Eds; Marcel Dekker, Inc.: Basel, New York, 1999; Chapter 9, Automation in combinatorial chemistry.

Antonenko, V. V.; Kulikov, N. V. Systems and Methods for the Synthesis of Organic Compounds. U.S. Patent 5866342, 1999.

Campbell, D. A.; Antonenko, V. V.; Selick, H. E.; Gavin, R. M.; Ida, S. Solid Phase Parallel Synthesis Systems and Methods. PCT Int. Appl. WO 9932219, 1999.

Szardenings, A. K.; Antonenko, V. V.; Campbell, D. A.; DeFrancisco, N.; Ida, S.; Shi, L.; Sharkov, N.; Tien, D.; Wang, Y.; Navre, M. Identification of Highly Selective Inhibitors of Collagenase-1 from Combinatorial Libraries of Diketopiperazines. J. Med. Chem. 1999, 42(8), 1348-1357.

VALERY V. ANTONENKO

Antonenko, V. V.; Kulikov, N. V. Reaction Block Systems and Methods for Synthesis of Organic Compounds on Solid Support. PCT Int. Appl. WO 9813137, 1998.

Antonenko, V. V.; Kulikov, N. V.; Jacobs, J. W. System and Methods for Parallel Synthesis of Organic Compounds. PCT Int. Appl. WO 9817382, 1998.

Jacobs, J. W.; Antonenko, V. V.; Patel, D. V.; Yuan, Z.; Holmes, C. P.; Schullek, J.; Grove, J. R.; Kulikov, N. V.; Maclean, D.; Navre, M.; Nguyen, C.; Shi, L.; Sundaram, A.; Sundberg, S. A. In Combinatorial Chemistry and Molecular Diversity in Drug Discovery; Gordon, E. M.; Kerwin, J. F., Jr., Eds.; Wiley-Liss, A John Wiley & Sons, Inc.: New York, 1998; Chapter 111, Light-Directed Chemical Synthesis of Positionally Encoded Arrays.

Tumelty, D.; Needels, M. C.; Antonenko, V. V.; Bovy, P. R. Synthesis of Head-to-Tail and Lactam Cyclized Libraries. In Peptides: Chemistry, Structure, Biology, Proceedings of the 14th American Peptide Symposium; Kaumaya, P. T. P.; Hodges, R. S., Eds.; Mayflower Scientific, Kingswinford, UK, 1996, 121-122.

Vetter, D., Tumelty, D. A., Antonenko, V. Methods for the Solid Phase Synthesis of Glycoconjugates. WO 9518971, 1995.

Antonenko, V. V.; Kulikov, N. V.; Tumelty, D.; Sundaram, A.; Jacobs, J. W. Combinatorial Libraries bi Light-Directed, Spatially Addressable Chemical Synthesis: Fidelity of the Method and Application to Drug Discovery. In Peptides 1994, Proceedings of the 23d European Peptide Symposium; Maia, Hernani L. S., Ed.; ESCOM, Leiden, Netherlands, 1995, 451-452.

Tumelty, D.; Vetter, D.; Antonenko, V. V. Immobilized Activated Peptides as Reagents for Cyclic and Derivatized Libraries. J. Chem. Soc., Chem. Commun. 1994, 9, 1067-1968.

Spencer, J. R.; Delaet, N. G. J.; Toy-Palmer, A.; Antonenko, V. V.; Goodman, M. Unusual Amide Bond Cleavage Reactions during Acidolytic Deprotection Reaction. J. Org. Chem. 1993, 58, 1635-1638.

Spencer, J. R.; Antonenko, V. V.; Delaet, N. G. J.; Goodman, M. Comparative Study of Methods to Couple Hindered Compounds. Int. J. Pept. Protein Res. 1992, 40, 282-293.

Mazurenko, N. N.; Kiseleva, N. P.; Kudryavets, Yu. I.; Mikhaleva, I. I.; Antonenko, V. V.; Kiselev, F. L. Tumor Cell Proteins Detected with Antibodies to C- and N-Terminal Fragments of the c-fos Protooncogene Product. Mol. Biol. (Engl. Transl.) 1990, 24, 1078-1088.

Antonenko, V. V.; Prudchenko, I. A.; Mikhaleva, I. I.; Mazurenko, N. N.; Kiseljoff, F. L. Detection of Cellular Proteins by Sequence-Specific Antisera. J. Cell. Biochem., Suppl 14C, 1990, 234.

Antonenko, V. V.; Prudchenko, I. A.; Mikhaleva, I. I.; Mazurenko, N. N.; Kiselev, F. L. Synthesis and Biological Properties of Antigenic Fragments of p28sis and p55fos Oncoproteins. J. Cell. Biochem., Suppl 12B, 1988, 61.

Antonenko, V. V.; Prudchenko, I. A.; Mikhaleva, I. I.; Mazurenko, N. N.; Kiselev, F. L. Synthesis and Immunogenic Properties of Peptides Corresponding to the 200-210 Sequence of p28sis Oncoprotein. Bioorg. Khim. 1987, 13, 1301-1312.

Mazurenko, N. N.; Gladkova, T. I.; Mikhaleva, I. I.; Antonenko, V. V.; Prudchenko, I. A.; Kiselev,

VALERY V. ANTONENKO

F. L. Preparation and Characterization of Antibodies to Synthetic Oncoprotein Fragments. I. Antiserum to Transforming Protein from Simian Sarcoma Virus p28sis. Mol. Biol. (Engl. Transl.) 1987, 21, 806-813.

Antonenko, V. V.; Mazurov, A. A.; Andronati, S. A. Isomeric 2-Methyl-4-(o-nitrobenzylidene)-oxazol-5-ones. Chemistry of Heterocyclic Compounds (Engl. Transl.) 1985, 21, 514-516.

Mazurov, A. A.; Antonenko, V. V.; Andronati, S. A. Properties of 1,4,5-Benzotriazocines. Chemistry of Heterocyclic Compounds (Engl. Transl.) 1983, 19, 337-340.

REFERENCES

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