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Home → Flash News → This new study reveals how the conformation of parathyroid hormone (PTH) and the C-terminal Category GPCR Weekly News This new study reveals how the conformation of parathyroid hormone (PTH) and the C-terminal

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Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Dr. Terry Kenakin Techniques for Effective Lead Optimization of Candidate Molecules GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program aimed at the discovery of new Drugs. The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators) and the process of characterizing the mechanism of action of ligands to enable the prediction of activity in vivo systems. In general, registrants will receive a comprehensive understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways. Registrants will learn: Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity). Application of this knowledge to determine the mechanism of action of new GPCR ligands. The required elements of a comprehensive and effective GPCR Discovery. Modules: October 3rd: GPCR Project Initiation and Design for Discovery of New Molecules. October 10th: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists. October 17th: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling. October 24th: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect. Registrations start on Monday, July 15th, 2024. Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST. Sessions will include a 1-hour live lecture plus 30 minutes of Q&A. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. A splendid time is guaranteed for all. What others are saying about the courses Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere Anonymous Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him Anonymous Thank you for bringing this course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field Anonymous Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. Anonymous The content had enough depth to satisfy the hunger for theory while being full of practical knowledge Anonymous The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work Anonymous The best pharmacology teacher teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology Anonymous What would you like to learn today?

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David Sibley (1988) Memories our panelists shared with us Enjoying the Dr. GPCR Podcast?

Qing is a structural biologist interested in the molecular mechanisms controlling how class C GPCRs transmit

described the molecular mechanisms of MRAP2 regulation of the GHSR1a, and where I notably developed the C-terminal This theory states that the post-translational modification of GHSR1a’ C-terminal tail is not a docking

molecular mechanisms involved in the opposite regulation of dopamine D1 and D5 receptors by protein kinase C. As part of Bouvier’s team, Bianca used Bioluminescence Resonance Energy Transfer (BRET)-based technology

Josh C Snyder (2012) Dr.

Disruption of these features reduced autoproteo-lytic activity in ADGRL1/LPHN1 and restored cleavage We assign the N-terminal CADH1-8 module as necessary for cell adhesion and we show the C-terminal CAHD9 Authors & Affiliations "Garbett, Krassimira, Kordon, Szymon P., Shearer, Tanner, Sando, Richard C.*, A stable π-edge contact with a conserved phenylalanine and a protonated glutamate side-chain catalyze MD simulations with the parameterized ester intermediate reveal a protonation-dependent dynamic desolvation

Affiliations "Rosell, Júlia (1) Holmkvist, Jesper L. (1) Arastoo, Mohammad Reza (1) Vejre, Phillip C. Burruss (Harvard Medical School); Andrew Kruse (Harvard Medical School); Stephen C.

intracellular calcium mobilization: Cell type-dependent involvement of Gi, Gq, Gs proteins and protein kinase C intracellular calcium mobilization: Cell type-dependent involvement of Gi, Gq, Gs proteins and protein kinase C Adipocytes Derivation of hiPSC line (ICADRB2i007-A-3) from an individual with osteoporosis linked to ADRB2: c.46G

autoproteolytic cleavage in the GAIN domain, creating a heterodimer of an N-terminal fragment (NTF) and a C-terminal

GPCR-autoproteolysis site (GPS) enclosed within the larger GAIN domain to generate the N-terminal (NTF) and C-terminal

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bulls Derivation of hiPSC line (ICADRB2i007-A-3) from an individual with osteoporosis linked to ADRB2: c.46G

hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or a BAI3 lacking the C-terminal

"Srivastava, Swati1; Singh, Abhishek Kumar1; Gunawan, Felix2; Gentile, Alessandra2; Petersen, Sarah C.3 Restoration of ADGRB1 expression slowed tumor growth and improved survival in mice bearing MB xenografts