Authors Charles H Williams , Leif R Neitzel , Jessica Cornell , Samantha Rea , Ian Mills , Maya S Silver , Jovanni D Ahmad , Konstantin G Birukov , Anna Birukova , Henry Brem , Betty Tyler , Eli E Bar , Charles C Hong Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

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. Registration over Subscribe to Dr. GPCR's Newsletter to be the first to learn about the next courses! What would you like to learn today?

Principles of Pharmacology in Drug Discovery II Advanced Methods for the Optimization of Candidate Selection Dr. Terry Kenakin Advanced Methods for the Optimization of Candidate Selection This course continues with the basics learned in Course 1 and extends the ideas to apply GPCR utilization in drug therapy . Specifically, the ideas discussed cover the complex pleiotropic behaviors of GPCRs and how these may be exploited for new drug discovery. Receptor data shows how GPCR control of cellular function goes far beyond simple second messenger production (i.e., calcium, cAMP), and these new behaviors are being used to create novel GPCR therapies. The five-lecture series describes essential additional elements to GPCR discovery programs that extend the discovery process and increase therapeutic opportunity. Registrants will learn: The powerful applications of new cellular assays to determine GPCR ligand behavior in different functional systems. Understanding real-time kinetics to predict activity and in vivo target coverage. New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and signaling, location bias, signaling bias). Modules October 31st: The Eyes to See- The Importance of Pharmacologic Assays. November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable. November 14th: The Application of GPCR Ligand Kinetics to Candidate Design. November 21st: Unconventional GPCR Ligands as Drugs. December 5th: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. 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 are the main objectives of the course? Allow registrants to appreciate the great versatility of GPCRs and how small molecules can affect their behavior for therapeutic benefit. What will students gain from taking this course? Learn how to therapeutically exploit GPCRs (Physiology’s ‘Swiss Army Knife’) wide repertoire of ways to control cell function. Apply unique pharmacologic assays and unconventional ligands to unveil GPCR activities. Adjust ligand kinetics and tissue disposition for optimal therapeutic activity. Are there any specific textbooks or readings students should be aware of? Pharmacology in Drug Discovery and Development (3rd ed.) T>P> Kenakin, Elsevier or ''A Pharmacology Primer' (6th ed.) T.P. Kenakin, Elsevier. Register today! Early-bird registration is over. Principles of Pharmacology II $ 675 675$ +$20.25 Transaction fee Advanced Methods for the Optimization of Candidate Selection Valid for 6 months Select Subscribe to Dr. GPCR's Newsletter to be the first to know about the next courses! What would you like to learn today?

inhibitor, suppresses the TGF-α-induced migration of hepatocellular carcinoma cells via inhibition of the c-Jun HuH7 cells through the activation of AKT, p38 mitogen-activated protein kinase (MAPK), Rho-kinase and c-Jun

As part of the degree, she undertook a 1-year research-based placement at the Charles Perkins Centre

The C. elegans ascaroside-sensing GPCR, SRBC66 and GPCRs of many fungi are also predicted for dual localization An SRBC64/66-GprC chimaeric protein was functional in A. flagrans, and C. elegans SRBC64/66 and DAF38 Authors Xiaodi Hu, David S Hoffmann, Mai Wang, Lars Schuhmacher, Maria C Stroe, Birgit Schreckenberger

Francisco, he joined the CNRS as a Research Fellow in 1987 in the INSERM Laboratory directed by Jean-Charles

Authors Quanbo Wang , Charles R Mackay Tags Gut microbiota , Western lifestyle diseases , portal vein

Authors Jong Min Hong , Jin-Woo Lee , Dong-Seung Seen , Jae-Yeon Jeong , Won-Ki Huh Tags Cancer , Chemokine

of CXCR2 antagonists in inflammatory diseases and cancers Published date March 15, 2023 Abstract " C-X-C

G-protein-coupled receptor class C group 5 member D (GPRC5D), an orphan GPCR predominantly expressed Jeong, Junhyeon Park, Geun Young Mo, Jinwoo Shin, Yunje Cho Tags GPRC5D , Multiple myeloma , class C

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

Authors Guang-Hong Qiu, Bin Yu, Mei Ma Tags GPCRs , cancer immune checkpoints , cancer immunotherapy

dermatitis , BAM8-22 , BP , Beta chain , Bovine adrenal medulla peptide 8-22 , Bullous pemphigoid , C-C

Josh C Snyder (2012) Dr.

News < GPCRs in Oncology and Immunology Stable Binding of Full-Length Chemerin is Driven by Negative Charges Here, we demonstrate that negative charges in the CMKLR1 N-terminus are involved in the formation of strong contacts with a specific positively charged patch at the surface of full-length chemerin, which

generating highly refined model structures of C5aR2, respectively in free (inactive), complexed to C-terminal

Joseph , Anthony Habgood , Amanda L Tatler , Katalin Susztak , Matthew Palmer , Stefan Offermanns , Neil C

Authors Ze Wu , Qiongqiong Jia , Boqun Liu , Lanlan Fang , Peter C K Leung , Jung-Chien Cheng Tags Invasion

Biswas, Michael J Miller, Julia E Myers, Stephen M Matthews, Amanda B Wass, Christine M O'Connor, Gary C

Authors Trang T T Nguyen , Wen Lu , Wandi S Zhu , K Mark Ansel , Hong-Erh Liang , Arthur Weiss .

Single-cell RNA sequencing on long-bone stromal cells of 9-wk-old male ColI(2.3)+/Rs1+ mice and littermate L Wentworth, Tania Moody, Ariane Zamarioli, Apsara Ram, Gauri Ganesh, Misun Kang, Sunita Ho, Edward C

Authors Hong Zeng , Li Cheng , De-Zhi Lu , Shuai Fan , Ke-Xin Wang , Li-Li Xu , Bin Cai , Mou-Wang Zhou

Zhang , Jiawei Zhou , Jianqiang Guo , Yafeng Liu , Chao Liang , Wenyang Wang , Yingru Xing , Jing Wu , Dong

Bryan S Yung , Farhoud Faraji , Robert Saddawi-Konefka , Zhiyong Wang , Alexander T Wenzel , Miranda J Song Pagadala , Lauren M Clubb , Joshua Chiou , Sanju Sinha , Marin Matic , Francesco Raimondi , Thomas S Hoang

Authors Ahmad Raza , Meng-Chi Yen , Gangga Anuraga , Iram Shahzadi , Muhammad Waqar Mazhar , Hoang Dang

Dandan Guo, Haizhen Lin, Muhammad Asad Farooq, Chenxu Jin, Li Zhang, Ying Zhou, Jie Yao, Yixin Duan, Cong

< GPCR News < GPCRs in Oncology and Immunology Severity of neurological long-COVID symptoms correlates The pathogenesis of Long-COVID is currently under heavy scrutiny and existing data on the role of auto-immune moderate SARS-CoV-2 infection up to 12 months prior to enrollment with (n = 72) or without (n = 58) Long-COVID Results: The prevalence and concentrations of evaluated autoantibodes were significantly higher in Long-COVID significantly higher number of patients with simultaneous detection of more than one autoantibody in Long-COVID