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Techniques will be described to quantify drug activity in terms of affinity, efficacy, and allosteric function Modules: Week 1 - Fundamentals of Pharmacology Week 2 - Characterizing Agonists Week 3 - Characterizing

The recently determined structures of B2R have provided molecular insights into the functions and regulation In this review, we summarize the structure and function of B2R in relation to drug discovery and discuss future research directions to elucidate the remaining unknown functions of B2R dimerization."

This effect involves the sequential and additive action of protein kinase A, casein kinase I, and the Fused (FU) kinase. Moreover, in the presence of very high levels of HH, the second effect of FU leads to the local enrichment

experimental structure of these receptors has yet to be determined, and key-residues controlling their function test case, we examined the accuracy of the TAS2R16 model with site-directed mutagenesis and in vitro functional This combination of in silico and in vitro results clarifies sequence-function relationships and proposes functional molecular switches that encode agonist sensing and downstream signaling mechanisms within Read full article

spontaneously formed nanoaggregates of GPCRs (natural nano-GPCRs) may enhance GPCR-related signalling and functions It will provide a fundamental platform for developing powerful and safe GPCR-targeted drugs and nanoparticle Authors Yuhong Jiang , Yuke Li , Xiujuan Fu , Yue Wu , Rujing Wang , Mengnan Zhao , Canquan Mao , Sanjun Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function

LP2 acted synergistically with 5-FU and the EGFR inhibitor erlotinib. synergism with selected drugs and, together with its excellent specificity, safety and stability, warrant further Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function

Single-cell transcriptome further delineated the tumor microenvironment as immune-inflamed, -deficient Authors Jie Xiong , Yu-Ting Dai , Wen-Fang Wang , Hao Zhang , Chao-Fu Wang , Tong Yin , Shu Cheng , Hui-Juan Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function