February 2022 " Ermium Therapeutics Announces the Formation of a Scientific Advisory Board comprising international leaders in GPCRs pharmacology, immunology, drug discovery and development for auto-immune diseases" Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "We are an experienced, innovative, global team on a bold mission to improve health by creating and developing life-changing medicines for people around the world." Read more at the source #DrGPCR #GPCR #IndustryNews

March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers. SCIENTIFIC MISSIONS (STSM) We offer short-term scientific mission grants to Ukrainian researchers who have Our scientific perspective is broad, and we are happy to consider any research proposals from those in

November 2021 Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc. has Janssen Pharmaceuticals, Inc., part of the Janssen Pharmaceutical Companies of Johnson & Johnson , has

December 2021 OMass Therapeutics 's founder, Carol Robinson , has been awarded the prestigious Louis-Jeantet in Chemistry from The Franklin Institute " Huge congratulations to our founder, Carol Robinson , who has Her work in the field has been instrumental and is set to shape the future of drug discovery for years

May 2022 "We are thrilled to announce that our co-founder Margaux Duchamp has been selected as a 30

Nicole (Nicki) Perry-Hauser is now available What a fun chat! 📹Would you like to see the video? GPCR has! ➡️https://bit.ly/3TCJVQQ #gpcr #drgpcr

There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s new structure-based technology has

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer

pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today reported its half-year recent financing from Armistice Capital and the extension of our strategic collaboration with Indivior have

March 2022 Crinetics Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief for rare endocrine diseases and endocrine-related tumors, today announced the appointment of James Hassard Hassard is a commercial leader with more than three decades of experience leading sales and marketing

However, only a few general-purpose libraries have been commercially available for drug discovery. The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors. To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better

September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and disease functions, yet knowledge of their role in colon cancer stem cell maintenance is still lacking. In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation are poorly understood. Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing β-catenin stability and transcriptional activity. Both PAR4 and PAR2 are able to drive the association of methyltransferase EZH2 with β-catenin, culminating in β-catenin methylation. This methylation on a lysine residue at the N-terminal portion of β-catenin suppresses the ubiquitination of β-catenin, thereby promoting PAR-induced β-catenin stability and transcriptional activity. Indeed, EZH2 is found to be directly correlated with high PAR4-driven tumors, and is abundantly expressed in large tumors, whereas very little to almost none is expressed in small tumors. A truncated form of β-catenin, ∆N133β-catenin, devoid of lysine, as well as serine/threonine residues, exhibits low levels of β-catenin and a markedly reduced transcriptional activity following PAR4 activation, in contrast to wt β-catenin. Our study demonstrates the importance of β-catenin lysine methylation in terms of its sustained expression and function. Taken together, we reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally involved in colon cancer." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Psychedelics, also known as classical hallucinogens, affect processes related to perception understanding of psychedelic pharmacology is derived from rodent models, but most of this preclinical research has

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

In the prospect of a psychedelic drug becoming again an approved treatment, much of these efforts have

Serotonergic psychedelics are substances that induce alterations in mood, perception, and thought, and have This review therefore elaborates on the in vitro molecular techniques that have been used the most abundantly Read more at the source #DrGPCR #GPCR #IndustryNews 5-HT2AR, GPCR, hallucinogens, in vitro assay, psychedelics

Biased agonism at the GLP-1R has been extensively studied, revealing that different ligands can stabilize Moreover, exendin-P5 has been observed to reduce adipose tissue size more effectively than exendin, suggesting Denise Wootten and colleagues has highlighted the importance of extracellular loop 2 (ECL2) in stabilizing The concept of biased agonism has been effectively leveraged in drug discovery, as demonstrated by the Tirzepatide’s superior effect over semaglutide has been attributed in part to biased agonism at the GLP

In this context, mutagenesis has emerged as an "old-school" but essential technology to fill these knowledge This technique has uncovered fundamental aspects of the G protein-coupled receptor (GPCR) function, including has seen a resurgence in recent times for exploratory analyses to identify previously unknown regions For example, random mutagenesis, combined with novel specificity high-throughput selection, has been Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist

The possibility of dimerization in class A and class B GPCRs, however, has been more controversial, despite For example, dimerization has been shown to affect signaling pathways in class A dopamine receptors like bioluminescence resonance energy transfer (BRET) and fluorescence resonance energy transfer (FRET) has In summary, dimerization in class B1 GPCRs is an emerging area of research that has far-reaching implications Harikumar, K.G., et al., Impact of secretin receptor homo-dimerization on natural ligand binding.  

Since then, the National Human Genome Research Institute (NHGRI) has supported annual events across the What does DNA Day have to do with GPCRs? Overal, genomics has been a driving force in advancing scientific knowledge and innovation within the integration of genomics with structural biology, pharmacology, bioinformatics, and clinical research has As we celebrate Happy DNA Day, it's a testament to how genomics has revolutionized our understanding

In the endosomes, sustained G protein signaling has been associated with prolonged interactions between This phenomenon has been demonstrated for receptors such as the parathyroid hormone receptor (PTHR) and The role of β-arrestins in endosomal signaling has been extensively studied, highlighting their ability GPCRs such as the β1-adrenergic receptor (B1AR) and the thyroid-stimulating hormone receptor (TSHR) has signaling mechanism is linked with the fact that dysregulation of compartmentalized GPCR signaling has

Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous decades—but the two-year-old biotech believes the area is still ripe for development, and it now has The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz , M.D., has 50 years of experience

neurophysiology "The awareness of the potential importance of functional selectivity/biased signaling has A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent Although this field has exploded during the past two decades, it is only recently that highly β-arrestin We discuss the importance of understanding the translatability of cell and animal models to have more precise functional targeting to harness the value of this signaling pathway."

Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. 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."

of the RGS family are selective for certain GPCRs, as a proof RGS4 which is expressed in the brain, has RGS4 is expressed in various immune cells, including T cells and B cells, and has been shown to modulate Relating to pain, RGS4 in pain regulation is a topic of increasing interest because it has been identified In hypertension, dysregulation of RGS proteins has been shown to contribute to the pathogenesis of the The dysregulation of these proteins has been implicated in a range of diseases, and understanding the

., of the University of Oxford , has joined Exscientia as Chief Scientist of Biologics AI. She has held numerous senior roles at the University of Oxford , where she is currently Professor of She has played an active role during the COVID-19 pandemic as the UKRI’s COVID Response Director, and

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has These complex properties have driven the need for development of specialized tools that can sense neuropeptide Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the