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薬剤標的としてのキナーゼ阻害剤は研究開発の絶頂期にあります。医薬品業界では現在、癌以外の治療分野に矛先を向け始めています。既存の阻害剤に関する新規の応用分野について研究されており、癌治療薬開発のための新たな標的が探求されています。製薬会社のプロジェクトの40％以上が癌以外の分野であることを考えると、この分野の開発や課題について解決する必要性があるのは明らかです。 11月2日（水） 7:00 am Conference Registration and Morning Coffee 阻害剤の設計と最適化 8:30 Chairperson’s Opening Remarks 8:40 Discovery of CX-4945, the First Clinical Stage Inhibitor of Protein Kinase CK2 for the Treatment of Cancer Fabrice Pierre, Ph.D., Associate Director, Medicinal Chemistry, Cylene Pharmaceuticals, Inc. Protein kinase CK2 expression and activity are elevated in many cancers, and the enzyme is known to regulate many oncogenic pathways, notably EGFR regulated pathways, PI3K-Akt-mTOR, WNT and NF-kB cascades, angiogenesis and the DNA damage response. These properties make CK2 an attractive oncology target for single-agents or combination therapies. This talk will discuss the design, SAR and latest characterization of CX-4945, the first ATP-competitive inhibitor of CK2 currently in clinical trials. 9:10 Structure-Based Design of VEGFR-2 Inhibitors Matthew Martin, Ph.D., Senior Scientist, Amgen, Inc. Using the available structures of VEGFR-2 small molecule complexes, a novel series of inhibitors was identified. This talk will describe the design, optimization, and biological activity of a second generation VEGFR-2 inhibitor. 9:40 Structure-Based Identification of ATP-Competitive MK2 Inhibitors Anthony Oubrie, CSO, Lead Pharma MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. In this talk, I will present the structure-based discovery of a novel MK2 inhibitor that exhibited in vivo efficacy in a short-term pre-clinical model. Optimization of this compound led to the identification of inhibitors with improved cellular potency and oral availability. 10:10 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing 肺疾患の標的化 10:40 Inhibition of a Novel Serine/Threonine Kinase Over-Expressed in Chronic Obstructive Pulmonary Disorder Stefen Boehme, Ph.D., Director, Immunology, Axikin Pharmaceuticals, Inc. We have identified a novel serine/threonine kinase that is upregulated in the lung tissue of COPD patients. siRNA-mediated knock-down of this kinase decreases the secretion of inflammatory cytokines in in vitro experiments and strongly inhibits multiple aspects of the inflammatory response observed in various animal models of COPD. Using the crystal structure of the kinase to guide our screening and SAR efforts, we have identified multiple lead compounds. We will discuss our ongoing pre-clinical development of antagonists against this novel kinase and as a possible treatment for COPD. Sponsored by Jabe Wilson, MBA, Ph.D., Senior Product Development Manager, Elsevier (Pharma & Biotech Group) In target identification/validation the fundamental questions are how is a target identified, and the hypothesis developed using the scientific literature? Reducing time & money investments in literature searching to get to a go-no go decision is crucial. Target Insights from Elsevier is a new online decision support tool for biologists dealing with these issues. Sponsored by
Dirk Leysen, Ph.D., Founder & CSO, Amakem NV Kinases are powerful biochemical targets with great potential to treat and modify many diseases. However most kinase inhibitors do not reach the market: systemic side effects limit the dose that can be applied and lead to narrow therapeutic windows and sub-therapeutic treatment regimens. Amakem developed a platform to circumvent these basic problems. Two cases will be presented in the field of ophthalmology and lung diseases that prove the validity of the concept and future value. 12:10 pm Panel Discussion Sponsored by From cDNA Clones to Assays, A Genomic Approach Xuan Liu, PhD, Senior Director, Marketing, OriGene Technologies, Inc. Biomedical research demand quality tools for detection, measurement and perturbation of specific gene/protein targets. Built upon a solid foundation of genome wide full-length cDNA clone clones, OriGene has been developing products and service focusing on system biology approaches to gene function analysis. In this talk, we will showcase some of our novel technology platforms for analyze individual proteins as well as proteome in general. 癌標的戦略 2:20 Chairperson’s Remarks 2:25 Epithelial-Mesenchymal Transition (EMT) as a Framework for Selection of Kinase Targets and Therapeutic Combinations for Oncology Jonathan Pachter, Ph.D., Senior Research Director, Translational Research, OSI Pharmaceuticals The activity of various Molecular Targeted Therapies, including the IGF-1R/IR kinase inhibitor OSI-906 and the mTORC1/2 kinase inhibitor OSI-027 to inhibit tumor cell proliferation as a function of epithelial vs. mesenchymal phenotype will be discussed. A strategy to select and validate novel kinase targets that influence the EMT transition or survival/proliferation of mesenchymal-like tumor cells will be presented together with strategies for rational definition of effective drug combinations. Both pre-clinical and clinical data will be presented. 2:55 Identification of a New Class of c-Met Inhibitors with a Unique Mode of Action and a Distinct Profile Against Activating Mutations Jason D. Katz, Chemistry Program Team Lead, Department of Chemistry, Merck Research Laboratories 3:25 Networking Refreshment Break in the Exhibit Hall with Poster Viewing 4:05 Multifaceted Intervention by the Hsp90 Inhibitor Ganetespib in Cancers with Activated JAK/STAT Signaling David Proia, Ph.D., Senior Scientist, Synta Pharmaceuticals Corp. Persistent JAK/STAT activation is oncogenic and characteristic of many human malignancies and thereby provides an attractive point of intervention for molecularly targeted therapeutics. In this presentation, we show that the Hsp90 inhibitor ganetespib has profound antitumor activity in an array of JAK/STAT-driven cancers and, importantly, can abrogate aberrant signaling through multiple mechanisms. 4:35 A New LIMK Inhibitor Stabilizes Microtubules and has Anticancer Activity Laurence Lafanechère, Ph.D., Director of Research, CNRS, Team# 03, Polarity, Development & Cancer, Department of Cellular Differentiation and Tansformation, Albert Bonniot Institute We identified a highly selective cell permeable LIMK inhibitor that reversibly stabilized microtubules and blocked actin microfilament dynamics. We established that the microtubule stabilizing effect of the compound is the result of its inhibitory effect on LIMK, independently of its effect on the actin cytoskeleton. The compound inhibits cell motility and is effective on multidrug resistant cancerous cell lines. It is also effective in animals, where it delays tumors formation while showing a good tolerability. 5:05 Interactive Breakout Discussion Groups 6:15 – 7:15 Welcoming Reception in the Exhibit Hall with Poster Viewing
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