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アロステリック調節因子は、近年、創薬分野、特にGタンパク質共役受容体（GPCR）が関与する分野への応用が始まりました。アロステリック調節因子は、GPCRなどの標的の特異的機能を選択的に活性化し副作用のリスクを低減するための薬剤として開発されるだけでなく、創薬においてGPCRの信号伝達複合体を解読するためのツールとして用いることができます。Cambridge Healthtech Instituteによる初の1日半の会議では、アロステリック調節因子をテーマに、GPCRおよびいくつかのGPCR以外の標的のためのアロステリック調節因子のデリバリーと最適化に関するケーススタディをお届けします。 11月3日（木）
アロステリック調節因子の特定：理論とスクリーニングアプローチ 1:30 pm Chairperson’s Remarks Andrew Alt, Ph.D., Senior Research Investigator, Lead Discovery, Bristol Myers Squibb
2:40 A Case Study: Evaluating Allosteric Modulators of CCR1 for Multiple Myeloma Annette Gilchrist, Ph.D., Assistant Professor, Pharmaceutical Sciences, Midwestern University Osteolytic bone destruction is one of the most frequent complications of multiple myeloma (MM), a clonal B-cell disorder characterized by the accumulation of malignant plasma cells in the bone marrow. Studies have recently emerged that suggest a role for the chemokine receptor CCR1 in multiple myeloma progression. To evaluate the role of CCR1 in MM we used several previously described allosteric small molecule inhibitors. Results from radioactive binding assays, and beta-arrestin translocation assays will be presented. 3:10 Networking Refreshment Break in the Exhibit Hall with Poster Viewing 3:45 Opportunities and Challenges in Developing High-Throughput Screens for Allosteric Modulators of G Protein-Coupled Receptors Andrew Alt, Ph.D., Senior Research Investigator, Lead Discovery, Bristol Myers Squibb Allosteric modulation of G protein-coupled receptors is an emerging therapeutic strategy that can potentially provide improved selectivity and safety, along with maintenance of spatial and temporal regulation associated with native receptor signaling. Accordingly, drug discovery efforts at GPCR targets have increasingly focused on the identification of allosteric modulators. This presentation will focus on the special challenges, opportunities and current strategies for high-throughput screening for allosteric GPCR modulators, with particular focus on the identification of positive allosteric modulators. 4:15 Sponsored Presentations (Opportunities Available) 4:45 Positive Allosteric Modulation of Metabotropic Glutamate Receptors in Neurotransmission: Specific Activity-Dependent Regulation of Defined Synaptic Circuits in vivo Thomas Salt, Ph.D., Professor, Visual Neuroscience, University College London Institute of Ophthalmology This talk will review use of Positive Allosteric Modulators (PAMs) to enhance mGlu synaptic and extra-synaptic function. I will show how PAMs can affect synaptic function under different physiological and pathological conditions in the whole organism based on recent experimental data on PAM action in thalamic circuitry from various groups (including the presenter’s). This will be placed in the context of how PAMs can affect sensory/pain processes, cognitive processes, schizophrenia, and epileptic mechanisms in vivo.
5:45 End of Day
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