October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling advanced NanoLuc/FlAsH-based biosensors reveals distinct conformational signatures of β-arrestin1 and 2 when

coupled receptors under diverse states Fan Liu , Han Zhou , Xiaonong Li , Liangliang Zhou , Chungong Yu

and subsequent activation of the G-protein heterotrimeric complex (α, β, and γ); it is at this point when Liu-Chen, and J.R. J Biol Chem, 2009. 284(27): p. 18357-67. https://pubmed.ncbi.nlm.nih.gov/19416973/ 5.

Through developing a high-resolution method, Hao Chen et al. directly visualized the fusion of vesicles Chen, X. Zhang, and L. Ma. 2008.

this has the potential to enhance GPCR subtype-selectivity, it also presents a significant challenge when modulators (NAMs), that fully or partially dampen the receptor's functional response to the ligand (Wold, Chen selectivity, which can arise from greater sequence variation in allosteric sites among receptor subtypes when This is particularly important when dealing with receptor subtypes that exhibit significant similarity substantial doses of allosteric modulators with a diminished risk of target-related toxicity (Wold, Chen

J Biol Chem, 2018. 293(19): p. 7466-7473. 8.      Nat Chem Biol, 2020. 16(8): p. 841-849. 10.    J Biol Chem, 2007. 282(14): p. 10576-84. 13.   

activation initiates conformational changes, exposing an intracellular cavity (Kang, Y. et al. 2015, Chen F et al. 2021, Chen, H. et al. 2022).

Norton Cheng and Dr.

was the most common method for predicting G protein-coupled receptor (GPCR) structures, especially when antipsychotic-like effects in rodent models, reinforcing the value of AlphaFold in drug discovery, especially when Nat Chem Biol   7 , 769-778 (2011).   https://doi.org/10.1038/nchembio.662 Diaz-Holguin, A.  

When I started studying aGPCRs, the structural conformation of the GAIN domain of ADGRL1/Lphn1 and ADGRB3 of human ADGRL3-G13, this paper reports that the stalk peptide of ADGRL3 adopts a hook conformation when Furthermore, when an alignment analysis of the Stalk peptide of the aGPCR family was performed highlighted ., Zhu, X., Wang, N., Xu, Z., Xia, R., Liang, J., Duan, Y., Yin, H., Xiong, Y., Zhang, A., Guo, C., Chen

Dysfunction of the adhesion GPCR latrophilin 1 (ADGRL1/LPHN1) increases the risk of obesity Norton Cheng

When it comes to signal transduction, cellular context matters. Pharmaceuticals (Basel, Switzerland), 14(5), 439. https://doi.org/10.3390/ph14050439 Chen, K.

Chem Rev, 2017. 117 (1): p. 111-138.

When comparing the CKRs structures complexes, the disulfide bridges formed between the N-loop and the agonist (maraviroc) (Tan, Zhu et al. 2013, Zheng, Han et al. 2017, Isaikina, Tsai et al. 2021, Zhang, Chen CCL15L (residues 26-92) and CCL15M (residues 27-92), while the third structure lacks a ligand (Shao, Shen conformational change of Y2917.43 tilted toward TM2, a model supported by mutagenesis experiments (Shao, Shen

Experienced Pharmaceutical Executive Toshihiro Maeda as Chief Operating Officer Rhythm Pharmaceuticals and LG Chem