October 2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut

Here, we provide guidelines and terminology for any scientists to design and report ligand bias experiments The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities analytical methods are still evolving and should benefit from and contribute to the implementation of the guidelines

September 2022 Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism , microbiota, and T cell-induced inflammation "Gut intraepithelial lymphocytes (IELs) are thought to Here, we show that the gut IEL GLP-1 receptor (GLP-1R) is not required for enteroendocrine L cell GLP Instead, the gut IEL GLP-1R is essential for the full effects of GLP-1RAs on gut microbiota. Such effects are mediated by the suppression of gut IEL effector functions linked to the dampening of

August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose tissue and urinary bladder. It is a therapeutic target because it plays a role in thermogenesis, lipolysis, and bladder relaxation. Two β3 -AR agonists are used clinically: mirabegron 1 and vibegron 2, which are indicated for overactive bladder syndrome. However, these drugs show adverse effects, including increased blood pressure in mirabegron patients. Hence, new β3 -AR agonists are needed as starting points for drug development. Previous pharmacophore modeling studies of the β3 -AR did not involve experimental in vitro validation. Therefore, this study aimed to conduct prospective virtual screening and confirm the biological activity of virtual hits. Ligand-based pharmacophore modeling was performed since no 3D structure of human β3 -AR is yet available. A dataset consisting of β3 -AR agonists was prepared to build and validate the pharmacophore models. The best model was employed for prospective virtual screening, followed by physicochemical property filtering and a docking evaluation. To confirm the activity of the virtual hits, an in vitro assay was conducted, measuring cAMP levels at the cloned β3 -AR. Out of 35 tested compounds, 4 compounds were active in CHO-K1 cells expressing the human β3 -AR, and 8 compounds were active in CHO-K1 cells expressing the mouse β3 -AR." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

Lukas Grätz , Jan Voss , and Gunnar Schulte , for their study on Class-Wide Analysis of Frizzled-Dishevelled

Kosar et al. (2024) addressed this question by using the role of the Trp258 6.48 residue to guide and

manipulates neuroactive signals and may onset metabolic disturbances GPCR Binders, Drugs, and more Gut

Conformational dynamics underlying atypical chemokine receptor 3 activation   Michael Trogdon , J Silvio Gutkind in pre-clinical retinopathy models Reviews, GPCRs, and more Lessons from the physiological role of guanosine continues to deliver strong sales growth and core margin expansion in Q2; raises FY 2024 bottom-line guidance

Mikel Garcia-Marcos for their work on Get ready to sharpen your tools:A short guide to heterotrimeric phosphorylation-dependent and independent desensitization mechanisms Get ready to sharpen your tools:A short guide

Gunnar Schulte  for his study on the International Union of Basic and Clinical Pharmacology.

Persistent Contextual Memory Engram β-arrestins are scaffolding proteins required for Shh-mediated axon guidance

AlphaFold2 structures guide prospective ligand discovery.

Witness the passion and excitement of our guests as you catch up on missed episodes.

In 2017, Gupte et al. introduced GPCR priming, which posits that non-cognate G proteins can enhance the Gupte et al. utilized a systematic protein affinity strength modulation (SPASM) technique to show that Gupte, T.M., et al., Priming GPCR signaling through the synergistic effect of two G proteins. 

Zhan-Guo Gao, Mansour Haddad, and Kenneth A Jacobson for their work on A2B adenosine receptor signaling

This will greatly impact not only the way we understand how aGPCR works but might also provide a guide

signaling Jiankun Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide Partial Activation of the Prototypic G Protein-Coupled Adenosine A2A Receptor AlphaFold2 structures guide

Chakit Arora, J Silvio Gutkind, and Francesco Raimondi for their work on The landscape of cancer-rewired

in models of autism spectrum disorders Systematic characterization of multi-omics landscape between gut

Screening of a Chemically Diverse "Superscaffold" Library Enables Ligand Discovery for a Key GPCR Target Gunnar

receptor in 1984 (Cerione et al. 1984), where reconstitution of purified β2-adrenergic receptors from guinea

Hoare's expert guidance, you will gain invaluable skills in data analysis.

Hoare's expert guidance. More details are coming soon—stay tuned! Dr.

assembled from publicly available deep-sequenced human samples GPCR Activation and Signaling Structure-guided

Magdalena M Scharf, Antonella Di Pizio, Ines Liebscher, Hannes Schihada, and Gunnar Schulte et al. on

Gunnar Schulte et al. on the study of the interaction of Clostridioides difficile toxin B and FZD7.

GPCR drug discovery via multitask learning GPCRs in Cardiology, Endocrinology, and Taste The Role of Gut