⚠️Mark your calendar for the Dr. GPCR Summit 2022 held between Oct. 10 - 16, it's FREE!

September 2022 "Introduction Protease activated receptors 1 (PAR1) and 4 (PAR4) agonists are used to Here we show that C1INH affects platelet activation through PAR1 and PAR4 agonists. The platelet suspensions were exposed to PAR1 agonists SFLLRN, TFLLR and TFLLRN; PAR4 agonists AYPGKF

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by of PAR2 that induces unique cellular signaling, distinct from trypsin and PAR2-activating peptide (AP Interestingly, unlike PAR2-AP, GB83 and trypsin induced sustained receptor endocytosis and PAR2 colocalization by GB83, which may be the reason why GB83 is recognized as an antagonist of PAR2. Our results revealed that GB83 is a bona fide agonist of PAR2 that uniquely modulates PAR2-mediated cellular

Our guest is Mark Schmeizl!

Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally PAR4 emerges as a potent oncogene, capable of inducing tumor generation. Here, we demonstrate identification of a pleckstrin-homology (PH)-binding motif within PAR4, critical It effectively attenuates PAR2&4-Akt/PKB associations; PAR4 instigated Matrigel invasion and migration The presence of PAR2 and PAR4 in biopsies of aggressive breast and colon cancer tissue specimens is demonstrated

October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate In this review, we will focus on the evidence for PAR interactions with members of their own family,

Mark Connor! Learn more about #GPCRs and life as an academic wearing different hats.

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Remarkably, a significant part of the bound ligands appears exposed to the membrane lipids.

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with pioneer as co-founder "J an 27, 2022 07:00am Septerna wants to spark a second golden age in G-protein-coupled Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous

Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing Both PAR4 and PAR2 are able to drive the association of methyltransferase EZH2 with β-catenin, culminating Indeed, EZH2 is found to be directly correlated with high PAR4-driven tumors, and is abundantly expressed residues, exhibits low levels of β-catenin and a markedly reduced transcriptional activity following PAR4 Taken together, we reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally

antagonists, which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

June 2022 "June 15, 2022 06:30 AM EDT - In 2016, Abbie Celniker was promoted to partner at Third Rock Ventures as the firm raised just over $600 million for its fourth fund. Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far — at a whopping $1.1 billion. Adding it all up, Third Rock has raised $3.8 billion since its inception. That money has gone to some 60 biotechs, much of it as early funding." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Sosei Heptares Confirms Senior Leadership Changes to Drive the Company Through the Next Stage Sosei Group Corporation (“the Company”; TSE: 4565) today confirms that a series of Executive Management changes

mucosal inflammation via enhancing NLRP3 inflammasome activation in macrophages "The putative medium-chain

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic are central to appropriate glucose homeostasis through their secretion of insulin, and islet function can

September 2022 "Parkinson’s disease (PD) as a progressive neurodegenerative disorder arises from multiple

the lipid composition of intracellular membranes may influence GPCR dynamics and signaling outcomes, changing Showing that this spatially biased signaling through arrestins can influence transcriptional responses Additionally, the conditions within endosomes, such as low pH and high protease activity, can degrade Pharmaceuticals (Basel, Switzerland), 14(5), 439. https://doi.org/10.3390/ph14050439 Chen, K. Nature communications, 8(1), 443. https://doi.org/10.1038/s41467-017-00357-2 Jong, Y.

Liebscher, Hannes Schihada, and Gunnar Schulte et al. on their study on understudied GPCRs and their dark You can sign up for our waitlist. We will be offering this live course later this year. If you are on the waitlist, you'll be the first notified and can register for the course ahead of everyone our events, and get a complimentary Premium Membership with only 4 hours/monthly commitment on your part cAMP signaling in the Hedgehog pathway Unraveling the Interplay of Extracellular Domain Conformational Changes

"We recently hosted our annual Scientific Advisory Board (SAB) summit at our site within Granta Park. It was great to bring everyone together and also welcome new member John Parkinson ."

Our Chief Matchmaker, Mark Schmeizl, is here to assist you. mechanisms of β-arrestin-1 revealed by 19F NMR spectroscopy Role of protease activated receptor 4 (PAR4 Allostery of G-Protein-Coupled Receptors Industry News Sosei Heptares to take back GPCR agonist after GSK changes Therapeutics Enters into Definitive Merger Agreement with Roche New Clinical Trial Explores Novel Target In Parkinson

Nbs typically consist of a single polypeptide chain which contains the antigen-binding site and the effector They are derived from the heavy-chain antibodies found in camelids (such as camels and llamas) and their They have also been used as biosensors to monitor conformational changes of GPCRs in living cells. J., Pardon, E., Casarosa, P., Chae, P. S., Devree, B. T., Rosenbaum, D. M., Thian, F. (New York, N.Y.), 347(6226), 1113–1117. https://doi.org/10.1126/science.aaa5026 Wu, A., Salom, D., Hong

Chemistry and Founder of (and ongoing consultant to) OMass Therapeutics , which is based at Oxford Science Park

Mark:  “Beth, why did you decide to join Crinetics?” Mark:  “Are there particular assay types of interest?” Mark:  “Beth, why would someone want you as their boss?” comments sound good to you, please reach out to me at mschmeizl@grnwindsor.com or 860-325-3505 and we can By: Mark Schmeizl Chief Matchmaker at Dr. GPCR

allostericmodulator pipeline and the potential $4 billion market for our lead compound #dipraglurant in #PDLID (#Parkinsonsdisease

Stay tuned for more details, and mark your calendars for registration opening in July 2024. Dr. compounds: A microphysiological system for cardiac drug development GPCRs in Neuroscience Astrocytic PAR1

Our Chief Matchmaker, Mark Schmeizl, had a great conversation about this position with Beth Fleck, Director Also, Mark Schmeizl can help you find your perfect match if you want to hire or be hired. Mark has experience connecting candidates with employers and will work with you to understand your needs Contact Mark today to get started. microbial metabolites and GPCRome in Alzheimer's disease Methods & Updates in GPCR Research Single-chain

recognized for inhibiting G protein signaling, they also influence specific pathways such as MAPK signaling (Song F et al. 2021, Chen, H. et al. 2022). include nuclear magnetic resonance (NMR) spectroscopy for conformational dynamics analysis context (Park be activated through specific β-arrestin conformations (Song, X. et al. 2008, Coffa, S. et al. 2011) Changes in the availability of regulatory proteins like GRKs can impact GPCR phosphorylation and subsequent