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March 2022 "March 3, 2022 Susanna Naggie, MD, and Sudarshan Rajagopal, MD, PhD Two School of Medicine faculty members — Susanna Naggie, MD, and Sudarshan Rajagopal, MD, PhD — have been elected to the American Naggie and Rajagopal are two of 95 new members elected to the society for 2022.

As research in this area expands, further insights are made into the role of neuropeptides and their This review focuses on the role of neuropeptides in maintaining the homeostasis of the ocular surface

Kosar et al. (2024) addressed this question by using the role of the Trp258 6.48 residue to guide and Furthermore, data on the role of specific residues within receptors can provide valuable insights for Advances in bioinformatics and machine learning will play a pivotal role in addressing these obstacles Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist

highlight how G proteins and β-arrestins are involved in driving intracellular signaling and reinforce the role

studies suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play a crucial role evidence suggests that their ability to form dimers—whether homodimers or heterodimers—plays a critical role

We also report on unexpected Fog-independent roles for Smog in maintaining epithelial integrity and organizing

We also report on unexpected Fog-independent roles for Smog in maintaining epithelial integrity and organizing

Recently, several GPCRs have been found to play important roles in the cochlea. Moreover, Frizzleds and Celsrs have been demonstrated to play core roles in the modulation of cochlear Here, we review the key findings of GPCR in the cochlea and discuss the role of GPCR in the cochlea,

adjuvant therapy at single administration or in combinatorial human trials, arising as a good pick and roll

October 2022 "Neisseria meningitidis is a Gram-negative opportunistic pathogen that is responsible for causing human diseases with high mortality, such as septicemia and meningitis. The molecular mechanisms N. meningitidis employ to manipulate the immune system, translocate the mucosal and blood-brain barriers, and exert virulence are largely unknown. Human-associated bacteria encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling molecules. However, only a small fraction of these metabolites has been identified from the human microbiota thus far. Here, we heterologously expressed an N-acyltransferase encoded in the obligate human pathogen N. meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. During this process, we also characterized two mammalian N-acyl amides derived from the bovine medium. Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell types, but they also suppress the pro-inflammatory interleukin-17A+ population in TH 17-differentiated CD4+ T cells." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and demonstrated that in GH3 cells SST2 and SST5 can form both homo- and hetero-dimers and that FLNA plays a role

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). FSHR is involved in reproductive processes such as gonadal development and maturation. Structurally, the extensive extracellular domain, which contains the hormone-binding site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors. How this HR is involved in hormone binding and signal transduction is still an open question. We combined in vitro and in situ chemical crosslinking, disulfide pattern analysis, and mutation data with molecular modeling to generate experimentally driven full-length models. These models provide insights into the interface, important side-chain interactions, and activation mechanism. The interface indicates a strong involvement of the connecting loop. A major rearrangement of the HR seems implausible due to the tight arrangement and fixation by disulfide bonds. The models are expected to allow for testable hypotheses about signal transduction and drug development for GPHRs." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental the regulation of cardiovascular system function and the drug target exploration, we summarize the role

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent Here, we focused on disclosing the integrin-dependent roles of focal adhesion kinase (protein tyrosine This work thereby supports the role of PTK2 in integrin αIIbβ3 activation and signaling."

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in The D1 receptor (D1R) is a Gαs/olf-coupled GPCR which activates a cAMP/PKA/DARPP-32 signalling cascade

We demonstrate how tail composition plays a role in modulating the binding of PI(4,5)P2 lipids to GCGR

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment Like many other organs, various GPCRs play a role in regulating liver function. In particular, a better understanding of the role of GPCRs in hepatic stellate cells (HSCs), the primary In this review, we describe the functions of multiple GPCRs expressed in HSCs, their roles in liver fibrogenesis

immune cells and platelets, revealing significant findings that enhance our understanding of GPCRs' roles , such as vasopressin receptors, were expressed in hematopoietic stem cells, suggesting a potential role The identification of a diverse array of GPCRs in immune cells underscores their potential roles in modulating ability to profile GPCR expression in a highly sensitive manner also opens doors for exploring the roles

This paper thoroughly investigated the role of single amino acid changes to clarify the molecular mechanisms GPCRs, including β2AR, play key roles in various conditions, such as asthma, cardiovascular diseases, While this case study highlights the essential role of mutagenesis in GPCR research, it is not the only Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery. Dr. GPCR Ecosystem; Dr. GPCR Ecosystem. https://www.ecosystem.drgpcr.com/post/decoding-gpcr-function-the-role-of-mutagenesis-in-rational-drug-discovery

In this study, the molecular signature of CCR2 scavenging role is investigated. In this study, the role of these 3 molecular players (G proteins, GRKs, and β-arrestin) is investigated In this study, it is revealed that CCR2 scavenging role was largely independent of the classical GPCR But why do canonical chemokine receptors have this dual role in physiology? How balanced is this dual role?

In this newly created role, she will focus on the application of artificial intelligence (AI), machine She has held numerous senior roles at the University of Oxford, where she is currently Professor of Structural She will maintain both of these roles, in addition to her role at Exscientia. She has played an active role during the COVID-19 pandemic as the UKRI’s COVID Response Director, and

Choosing the Right Lab The lab you choose plays a pivotal role in shaping your PhD journey. The Role of Mentors and Supervisors Having the right mentor is indispensable for a successful PhD journey My supervisors played an instrumental role in my growth.

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, little is known about the roles in osteoclasts. But GPR110 knockout and subsequent rescue experiments revealed a pivotal role of GPR110 in the attenuation

chemokines to direct cell migration during immune surveillance and inflammation, as well as to play vital roles canonical CKRs have also been shown to not only directly regulate migration but also play a scavenging role To comprehensively elucidate the role of scavenging in normal physiology and the potential implications

Specifically, previous research has identified mechanistically distinct and cell type–specific roles In light of these new results, it is imperative that we revisit previous studies regarding the role of Thus, this review will cover specific roles of C3aR in driving cell type–specific and tissue specific

Beth is also the hiring manager for their open Principal Scientist, In Vitro Pharmacology role posted Mark:  “So, what are the qualities of the perfect candidate for the Principal Scientist role?”

Specifically, we explore the role of actin cytoskeleton in regulating the dynamics of the serotonin1A receptor, a crucial neurotransmitter G protein-coupled receptor (GPCR) that plays a major role in the On a broader perspective, these results assume significance in understanding the modulatory role of the