Targeting cryptic allosteric sites of G protein-coupled receptors as a novel strategy for biased drug discovery by Xin Qiao, Xiaolong Li, Mingyang Zhang, Ning Liu, Yanmei Wu, Shaoyong Lu, Ting Chen

Subjects: “…G protein-coupled receptors…”
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Orphan G protein-coupled receptor GPRC5B controls macrophage function by facilitating prostaglandin E receptor 2 signaling by Jeonghyeon Kwon, Haruya Kawase, Kenny Mattonet, Stefan Guenther, Lisa Hahnefeld, Jamal Shamsara, Jan Heering, Michael Kurz, Sina Kirchhofer, Cornelius Krasel, Michaela Ulrich, Margherita Persechino, Sripriya Murthy, Cesare Orlandi, Christian D. Sadik, Gerd Geisslinger, Moritz Bünemann, Peter Kolb, Stefan Offermanns, Nina Wettschureck

“…Abstract Macrophages express numerous G protein-coupled receptors (GPCRs) that regulate adhesion, migration, and activation, but the function of orphan receptor GPRC5B in macrophages is unknown. …”
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A lipidated peptide derived from the C-terminal tail of the vasopressin 2 receptor shows promise as a new β-arrestin inhibitor by Rebecca L. Brouillette, Christine E. Mona, Michael Desgagné, Malihe Hassanzedeh, Émile Breault, Frédérique Lussier, Karine Belleville, Jean-Michel Longpré, Michel Grandbois, Pierre-Luc Boudreault, Élie Besserer-Offroy, Philippe Sarret

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Re-annotation of SARS-CoV-2 proteins using an HHpred-based approach opens new opportunities for a better understanding of this virus by Brézellec, Pierre

“…Equally interestingly, Lutropin-choriogonadotropic hormone receptor showed similarities with 23 viral G-protein coupled receptors, particularly from Herpesvirales. …”
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Rapid expansion and specialization of the TAS2R bitter taste receptor family in amphibians. by Kathleen W Higgins, Akihiro Itoigawa, Yasuka Toda, Daniel Winston Bellott, Rachel Anderson, Roberto Márquez, Jing-Ke Weng

“…TAS2Rs are a family of G protein-coupled receptors that function as bitter taste receptors in vertebrates. …”
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Complex regulation of Cav2.2 N-type Ca2+ channels by Ca2+ and G-proteins. by Jessica R Thomas, Jinglang Sun, Juan De la Rosa Vazquez, Amy Lee

“…G-protein coupled receptors inhibit Cav2.2 N-type Ca2+ channels by a fast, voltage-dependent pathway mediated by Gαi/Gβγ and a slow, voltage-independent pathway mediated by Gαq-dependent reductions in phosphatidylinositol 4,5-bisphosphate (PIP2) or increases in arachidonic acid. …”
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Post sleeve gastrectomy-enriched gut commensal Clostridia promotes secondary bile acid increase and weight loss by Shaoqian Zhao, Huibin Lin, Wen Li, Xiaoqiang Xu, Qihan Wu, Zhifeng Wang, Juan Shi, Yufei Chen, Lingxia Ye, Liuqing Xi, Lijia Chen, Mingyang Yuan, Junlei Su, Aibo Gao, Jiabin Jin, Xiayang Ying, Xiaolin Wang, Yaorui Ye, Yingkai Sun, Yifei Zhang, Xiaxing Deng, Baiyong Shen, Weiqiong Gu, Guang Ning, Weiqing Wang, Jie Hong, Jiqiu Wang, Ruixin Liu

“…Furthermore, both Clostridia-enriched spore-forming bacteria and GDCA supplementation increased the expression of genes responsible for lipolysis and fatty acid oxidation in adipose tissue and reduced adiposity via Takeda G-protein-coupled receptor 5 (TGR5) signaling. Our findings reveal post-SG gut microbiome and C-SBAs as contributory to SG-induced weight loss, in part via TGR5 signaling, and suggest SBA-producing gut microbes as a potential therapeutic target for obesity intervention.…”
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Novel risk loci encompassing genes influencing STAT3, GPCR, and oxidative stress signaling are associated with co-morbid GERD and COPD. by Ava C Wilson, Alison Rocco, Joe Chiles, Vinodh Srinivasasainagendra, Wassim Labaki, Deborah Meyers, Bertha Hidalgo, Marguerite R Irvin, Surya P Bhatt, Hemant Tiwari, Merry-Lynn McDonald

“…The co-heritability of GERD and COPD was 39.7% (h2 = 0.397, SE = 0.074) and we identified several ancestry-independent loci associated with co-morbid GERD and COPD (within LINC02493 and FRYL) known to be involved in oxidative stress and G protein-coupled receptor (GPCR) signaling mechanisms. We found several loci associated with co-morbid GERD and COPD previously associated with GERD or COPD individually, including HCG17, which plays a role in oxidative stress mechanisms. …”
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CCR2 signaling regulates anti-chlamydia T cell immune responses in the airway. by Shuaini Yang, Jinxi Yu, Xue Dong, Jiajia Zeng, Lu Tan, Hong Zhang, Ruoyuan Sun, Yuqing Tuo, Jing Yang, Chunxiao Wan, Hong Bai

“…CCR2, a member of the G protein-coupled receptor (GPCR) superfamily, is widely expressed on monocytes, macrophages, activated T cells, and other cell types, and plays a critical role in coordinating the immune response to various infections. …”
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Integrative bioinformatic approach reveals novel melatonin-related biomarkers for Alzheimer’s disease by Hua-xiong Zhang, Dilmurat Hamit, Qing Li, Xiao Hu, San-feng Li, Fu Xu, Ming-yuan Wang, Guo-qing Bao, Hong-yan Li

“…After overlapping with 3,490 DEGs and 550 MRGs in GSE5281, four genes were found to be causally related to AD, namely, G protein-coupled receptor, family C, group 5, member B (GPRC5B), Methyltransferase-like protein 7 A (METTL7A), NF-κB inhibitor alpha (NFKBIA) and RAS association domain family 4(RASSF4). …”
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Optimasi Data Tidak Seimbang pada Interaksi Drug Target dengan Sampling dan Ensemble Support Vector Machine by Nabila Sekar Ramadhanti, Wisnu Ananta Kusuma, Annisa Annisa

“…Metode ini sudah diuji pada dataset Nuclear Receptor, G-Protein Coupled Receptor dan Ion Channel dengan rasio ketidakseimbangannya sebesar 14.6%, 32.36%, dan 28.2%. …”
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Efficacy and safety of SHR8554 on postoperative pain in subjects with moderate to severe acute pain following orthopedic surgery: A multicenter, randomized, double-blind, dose-expl... by Yanhua Zhao, Zhisheng Lu, Xuesong Song, Haihui Xie, Xungang Xiao, Guonian Wang, Qi Zhou, Qingmei Zhang, Liang Liu, Zhijian Lan, Ning Bai, Haiyan Wang, Zhihao Pan, Liang Dong, Xianzhong Lin, Gang Chen, Qinghui Wang, Jiangtao Dong, Jia Deng, Yongshan Nan, Jiaqiang Zhang, Xiaohua Zhou, Yanjuan Huang, Yongquan Chen, Huanzhong He, Ye Yang, Dengpan Yao, Jintai Jia, Shuan Jin, Yafeng Zhang, Zhonghui Luo, Jiangang Li, Linzhong Zhang, Fang Wang, Juehua Jing, Jiang Zhu, Lin Li, Guangda Wang, Huajing Guo, Qiang Wang, Diansan Su, Weifeng Yu, Xiyao Gu

“…Biased µ-opioid receptor (MOR) agonists enhance pain relief by selectively activating G protein-coupled receptor signaling and minimizing β-arrestin-2 activation, resulting in fewer side effects. …”
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