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.

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

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

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

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

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

"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 ."

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:  “Have you found this to be accurate?” Beth:  “Yes.  Mark:  “Are there particular assay types of interest?” Mark:  “Beth, why would someone want you as their boss?” By: Mark Schmeizl Chief Matchmaker at Dr. GPCR

Saline-injected rats served as controls." Read more at the source #DrGPCR #GPCR #IndustryNews

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

Liebscher, Hannes Schihada, and Gunnar Schulte et al. on their study on understudied GPCRs and their dark GPCR University Last week marked the beginning of our first Dr.GPCR University course, 'Applying Pharmacology our events, and get a complimentary Premium Membership with only 4 hours/monthly commitment on your part Scaling up Functional Analyses of the G Protein-Coupled Receptor Rhodopsin Reviews, GPCRs, and more The dark

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 Therapeutics Enters into Definitive Merger Agreement with Roche New Clinical Trial Explores Novel Target In Parkinson

July 21st marks our next Dr. CLIC4 Regulates Endothelial Barrier Control by Mediating PAR1 Signaling via RhoA.

Mark your calendars for September and October 2024! We are excited to announce that Dr. GPCR Matchmaking Meet Mark Schmeizl, our Chief Matchmaker. Whether you’re hiring top talent or seeking a new career opportunity, Mark’s expertise ensures successful Mark discussed this position with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals Mark your calendar for the GPCRs as Therapeutic Targets symposium on October 11th, 2024.

Mark your calendar for September and October 2024. Dr. GPCR Matchmaking Mark Schmeizl, our Chief Matchmaker, can help you find your perfect match if you want Mark has experience connecting candidates with employers and will work with you to understand your needs Contact Mark today to get started. Dr. Mark your calendar for October 23 - 25, 2024, as we kick off the 11th Adhesion GPCR Workshop in Mexico

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.

Our Chief Matchmaker, Mark Schmeizl, had a great conversation about this position with Beth Fleck, Director Also, if you are looking to hire or be hired, Mark Schmeizl can help you find your perfect match. Mark has experience connecting candidates with employers and will work with you to understand your needs Contact Mark today to get started.

Mark your calendar for October 10th and 16th.

GPCR University Today marks the final day of the Dr. GPCR Matchmaking Read Mark's job spotlight article for a Principal Scientist in In Vitro Pharmacology Mark recently discussed this exciting opportunity with Beth Fleck, Director of In Vitro Pharmacology

Mark your calendars! The Dr. GPCR Podcast is back this week with a brand new episode.