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异位效应调节因子
异位效应调节因子近几年开始应用到创药领域、尤其是G蛋白质共轭容纳体(GPCR)参与领域。异位效应调节因子不只是作为选择性活化GPCR等标的特异机能，开发作为降低副作用风险的药剂，亦能作为解读创药GPCR信号传达复合体的工具。在Cambridge Healthtech Institute首次1日半的会议中，以异位效应调节因子为主题，提出GPCR及几个GPCR以外标的的异位效应调节因子传递及最适化的个案研究。

11月3日 星期四

异位效应调节因子的特别规定：理论和筛选方法

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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