GPCR Summit 2022 is less than a month away!

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function. In a constant effort to develop drugs with less side effects, and tools to explore the ORs nature and function, various (poly)pharmacological ligand design approaches have been performed. That is, besides classical ligands, a great number of bivalent ligands (i. e. aiming on two distinct OR subtypes), univalent heteromer-selective ligands and bitopic and allosteric ligands have been synthesized for the ORs. The scope of our review is to present the most important of the aforementioned ligands, highlight their properties and exhibit the current state-of-the-art pallet of promising drug candidates or useful molecular tools for the ORs." Read more at the source #DrGPCR #GPCR #IndustryNews

neuron morphogenesis and shapes chemo- and mechanosensation-dependent behavior in C. elegans via a trans Caenorhabditis elegans can also function independently of their seven-transmembrane domain and C terminus (trans Here, we show that Latrophilin-1 acts in trans to mediate morphogenesis of sensory structures in the This trans function is physiologically relevant in copulation behavior.

Finally, we observed that the Ca2+o -stimulated CaSR operated exclusively via signaling in-trans and not via combined in-trans and in-cis signaling.

References: Jin, B. K., Odongo, S., Radwanska, M., & Magez, S. (2023). M., Thian, F. S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R. K., Gellman, S.

Recent studies showed that some AVPR2 mutations could cause biased Gαq/11 protein coupling rather than R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor.

GPCR is much more than a podcast? Come check out the brand new Dr.

The suppressive rather than activating effects of pGRP were confined to blood flow at a high shear rate Blockage of PTK2 or interference of CIB1 no more than slightly affected thrombus formation at a low shear

Carola Weiss is a Senior Executive with more than 20 years of international experience in the biopharmaceutical

This time with none other than Dr. Bryan Roth There are 10 open tickets available. Get yours now!

GPCR Podcast, we have none other than Dr. Marta Filizola!

Our guest is none other than Dr. Juan Jose Fung, Principal Scientist, at GPCR Therapeutics.

The move comes less than three weeks after X4 pulled together a $55 million PIPE and amended a loan facility

Our first guest speaker is none other than Dr. Ben Myers!

determine partner preference; or (iii) the dynamics of GPCR binding to different types of partners rather than

Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous

Hassard is a commercial leader with more than three decades of experience leading sales and marketing

One potential solution is to develop analgesics that act at targets other than opioid receptors.

A much smaller conformational change of helix VI upon activation than previously solved class A GPCR-Gi

In less than a decade, nanobodies, or recombinant single-domain antibody fragments from camelids, have

Vraniak’s career spans more than 20 years of financial and commercial experience in the life sciences

and anxiety, has shown, in the last decade, increasing evidence of its antitumoral properties in more than

In fact, it is often costly, frustrating, and tortuous—and more often than not it ends in failure.

each G protein with the receptor showed that there are more polar interactions in Gq/Gs engagements than Qian, Y., Ma, Z., Liu, C., Li, X., Zhu, X., Wang, N., Xu, Z., Xia, R., Liang, J., Duan, Y., Yin, H.,

intermediate state complex comprising β1-AR and nucleotide-free Gs is more stable when binding a full agonist than

Six compounds showed more than 50% displacement of the radioligand at 10 µM concentration with compound

He has led teams that have filed more than 10 Investigational New Drug Applications (IND), as well as

However, our predictions were many folds shorter than those determined experimentally.