exploration of key concepts in pharmacology, offering a nuanced understanding of drug interactions and mechanisms

October 2022 Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment prescription of traditional Chinese Medicine (TCM), is widely used in the treatment of depression, but its mechanism pharmacology method was used to constructe the "herb-component-target" network, and elucidated KXS potential mechanisms Go enrichment analysis indicated that the mechanism of KXS in treating depression was involved in the

September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs), mechanistic understanding of how these modulators alter GPCR function is of significance. Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor CB1 bound to the positive allosteric modulator (PAM) ZCZ011. These structures show that ZCZ011 binds to an extrahelical site in the transmembrane 2 (TM2)-TM3-TM4 surface. Through (un)biased molecular dynamics simulations and mutagenesis experiments, we show that TM2 rearrangement is critical for the propagation of allosteric signals. ZCZ011 exerts a PAM effect by promoting TM2 rearrangement in favor of receptor activation and increasing the population of receptors that adopt an active conformation. In contrast, ORG27569, a negative allosteric modulator (NAM) of CB1, also binds to the TM2-TM3-TM4 surface and exerts a NAM effect by impeding the TM2 rearrangement. Our findings fill a gap in the understanding of CB1 allosteric regulation and could guide the rational design of CB1 allosteric modulators." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric IUPHAR Review 34 "Functional advances have guided our knowledge of physiological and fatal pathological mechanisms dynamics of AngII receptors and how structural knowledge can be transformative in understanding the mechanisms

Hong Pheng Loh , Min Thura , Abhishek Gupta , Sheng Hui Tan , Kelvin Kam Yew Kuan , Koon Hwee Ang , Khurshid Merchant , Kenneth Tou En Chang , Hui Yi Yon , Yong Chen , Mathew Hern Wang Cheng , Arjandas Mahadev

Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Biochemical Mechanisms Keith Moffat, he studied the structural mechanisms of bacterial photoreceptors using time-resolved Laue After completing his training, he joined the faculty at Duke, with a focus on the mechanisms underlying His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the

< GPCR News < GPCRs in Oncology and Immunology The binding mechanism of an anti-multiple myeloma antibody potential, the insufficient understanding regarding of the receptor's structure and antibody recognition mechanism