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Tuesday, April 26
8:20 am Opening Keynote Remarks
Gregory A. Weiss, Ph.D., Professor, Departments of Chemistry, Molecular Biology & Biochemistry, University of California, Irvine
8:30 Chairperson’s Introduction
Frank L. Meyskens, Jr., M.D., Director, Chao Family Cancer Center, University of California, Irvine
8:40 How Do You Move Your Favorite Molecule from Lab to Clinic: Early Steps
James H. Doroshow, M.D., Director, Division of Cancer Treatment and Diagnosis, National Cancer Institute
9:15 Just Say NO to Neurodegenerative Diseases and Melanoma
Richard B. Silverman, Ph.D., Professor, Chemistry, Weinberg College of Arts & Sciences, Northwestern University
The importance of nitric oxide (NO) in neurodegenerative diseases and melanoma will be discussed. The design of potent and selective neuronal nitric oxide synthase inhibitors will be presented and their use in the treatment of neurodegenerative disease and melanoma described.
9:50 Revising the Biomarker Development Process for Oncology Drug Development
Samir N. Khleif, M.D., Head, Cancer Vaccine Section Investigator, National Cancer Institute
10:25 Refreshment Break, Poster Session & Exhibit Viewing
11:10 Chairperson’s Remarks
Hung Y. Fan, Ph.D., Professor, Molecular Biology and Biochemistry, School of Biological Sciences, University of California, Irvine
11:15 Optimization of Therapeutic Vaccines for Cancer and Their Use in the Preventative Setting
W. Martin Kast, Ph.D., Walter A. Richter Cancer Research Chair; Professor, Molecular Microbiology & Immunology, Obstetrics & Gynecology and Urology, Norris Comprehensive Cancer Center, University of Southern California
Therapeutic cancer vaccines still have to overcome significant hurdles in order to become truly effective. In this presentation evidence is provided on how therapeutic vaccines can be improved through enabling T cell homing into tumors as well as how they can be very effectively applied at a precancerous stage.
11:45 Gene Transfer-Mediated Induction of T Cells Resistant to Immune Inhibitory Mechanisms
Adrian Bot, M.D., Ph.D., Vice President, Scientific Management, MannKind Corp.
The ability of T cells to operate unhindered within tumors is essential to the success of cancer vaccines. Gene transfer by intra-lymph node plasmid injection elicits T cells lacking expression of inhibitory receptors. These and novel clinical data support the utilization of gene-transfer to optimize active immunotherapy for cancer.
12:15 pm Sponsored Presentation (Opportunity Available)
12:45 Luncheon Presentation (Sponsorship Opportunity Available)
2:00 Chairperson’s Remarks
Gregory A. Weiss, Ph.D., Professor, Departments of Chemistry, Molecular Biology & Biochemistry, University of California, Irvine
2:05 FEATURED SPEAKER
Ribonucleotide Reductases: Good Targets for Cancer Therapeutics?
 JoAnne Stubbe, Ph.D., Novartis Professor, Chemistry, Massachusetts Institute of Technology
Ribonucleotide reductases (RNR) catalyze the conversion of nucleotides to deoxynucleotides in all organisms. Recent studies on gemcitabine and clofarabine have suggested that the diphosphates are potent substoichiometric and stoichiometric RNR inhibitors, respectively. Our current understanding of the mechanisms by which these compounds target RNRs will be presented.
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2:35 FEATURED SPEAKER
Designing Transition State Analogues as Anticancer Agents
 Vernon L. Schramm, Ph.D., University Professor and Ruth Merns Chair, Biochemistry, Albert Einstein College of Medicine
Transition state structures of enzymes as anticancer targets are being solved by a combination of kinetic isotope effects and computational chemistry. Transition state analogues designed from this approach show promise in leukemia and solid tumors.
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3:05 Refreshment Break, Poster Session & Exhibit Viewing- Complimentary Access for UC Irvine Affiliates
3:45 Acquired Resistance to B-RAF Inhibitors in Melanoma
Roger Lo, M.D., Ph.D., Assistant Professor, Medicine; Dermatology Director, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine, UCLA
Recent clinical experience with B-RAF inhibitors has demonstrated in-human druggability of the B-RAF V600E mutation and a profound B-RAF oncogene addiction in human melanoma. Acquired drug resistance, however, is frequent and limits overall survival benefit from B-RAF targeting. Understanding the heterogeneous mechanisms of acquired resistance to B-RAF inhibitors is thus critical to augment the long-term efficacy of B-RAF inhibitors.
4:15 Chemo-Proteomic Interrogation of the Kinome in the Design of New Oncology Drugs
John Kozarich, Ph.D, Chairman, President, ActivX Biosciences, Inc.
We have developed chemical tools that permit the in situ identification and quantification of members of the kinome across species. The method will be highlighted with examples in the design and evaluation of specific, tissue selective kinase inhibitors for several important oncology targets.
4:45 Targeting the c-Myc Oncoprotein with Small Molecules
Edward Prochownik, Ph.D., Paul C. Gaffney Professor, Pediatrics; Professor, Microbiology & Molecular Genetics Section, Hematology/Oncology, Children’s Hospital, University of Pittsburgh Medical Center
Our laboratory has identified small molecules that bind to the bHLH-ZIP dimerization domain of c-Myc and inhibit the interaction with its obligate partner protein, Max. Recent studies have shown that that these small molecules bind to c-Myc with moderate affinity. A strategy whereby two such molecules are chemically linked to create a bi-valent c-Myc binder increases affinity by as much as 10,000-fold. Such molecules may be of general use in targeting a variety of tumors, nearly all of which are highly dependent upon fully functional c-Myc.
5:15 Reception Sponsored by Chao Family Comprehensive Cancer Center and Cambridge Healthtech Institute
6:30 Close of Day