Results 91 to 100 of about 92,178 (306)

High-resolution deep mutational scanning of the melanocortin-4 receptor enables target characterization for drug discovery

eLife
Deep Mutational Scanning (DMS) is an emerging method to systematically test the functional consequences of thousands of sequence changes to a protein target in a single experiment.
Conor J Howard, Nathan S Abell, Beatriz A Osuna, Eric M Jones, Leon Y Chan, Henry Chan, Dean R Artis, Jonathan B Asfaha, Joshua S Bloom, Aaron R Cooper, Andrew Liao, Eden Mahdavi, Nabil Mohammed, Alan L Su, Giselle A Uribe, Sriram Kosuri, Diane E Dickel, Nathan B Lubock   +17 more
doaj   +1 more source

TBXA2R gene variants associated with bleeding

Platelets, 2018
Platelet activity is regulated by a number of surface expressed G protein-coupled receptors (GPCRs) including the α isoform of the thromboxane receptor (TPα receptor). With the advance of genomic technologies, there has been a substantial increase in the
Stuart James Mundell, Andrew Mumford
doaj   +1 more source

Sensing and Reprogramming Surface Receptor Activation With Synthetic Transcriptional Circuits

Advanced Science, EarlyView.
A synthetic receptor‐signalling induced transcription (RESIT) circuit is designed based on receptor activation mediated split protease complementation and release of membrane‐tethered synthetic transcriptional modules. The RESIT system enables probing Ca2+ entry, receptor tyrosine kinase (RTK) activities and Ras activation, and reprogramming RTK ...
Fei Liu, Mei Yuan, Li‐Juan Tang, Fenglin Wang, Xia Chu, Jian‐Hui Jiang   +5 more
wiley   +1 more source

GPCRomics: An Approach to Discover GPCR Drug Targets.

TIPS - Trends in Pharmacological Sciences, 2019
G protein-coupled receptors (GPCRs) are targets for ∼35% of approved drugs but only ∼15% of the ∼800 human GPCRs are currently such targets. GPCRomics, the use of unbiased, hypothesis-generating methods [e.g., RNA-sequencing (RNA-seq)], with tissues and ...
P. Insel, K. Sriram, M. Gorr, Shu Z. Wiley, A. Michkov, C. Salmerón, Amy M. Chinn   +6 more
semanticscholar   +1 more source

Peptide‐Incorporated Biomaterials Promote Regeneration of Peripheral Nerve Injuries

Advanced Science, EarlyView.
Peptide‐incorporated biomaterials provide precise, tunable biological cues that mimic functional protein domains to regulate behaviors of neurons, Schwann cells, immune cells, and endothelial cells, thereby enhancing axon elongation, Schwann cell support, inflammatory microenvironment modulation, and vascularization, offering a promising alternative to
Zhiwei Zhao, Jianfeng Liu, Jincheng Li, Di Li, Jianxun Ding, Bin Liu   +5 more
wiley   +1 more source

GPCR heterodimerization in the reproductive system: functional regulation and implication for biodiversity

Frontiers in Endocrinology, 2013
A G protein-coupled receptor (GPCR) functions not only as a monomer or homodimer but also as a heterodimer with another GPCR. GPCR heterodimerization results in the modulation of the molecular functions of the GPCR protomer, including ligand binding ...
Honoo eSatake, Shin eMatsubara, Masato eAoyama, Tsuyoshi eKawada, Tsubasa eSakai   +4 more
doaj   +1 more source

Harnessing Ion-Binding Sites for GPCR Pharmacology

Pharmacological Reviews, 2019
Endogenous ions play important roles in the function and pharmacology of G-protein coupled receptors (GPCRs). Historically the evidence for ionic modulation of GPCR function dates to 1973 with studies of opioid receptors, where it was demonstrated that ...
B. Zarzycka, S. Zaidi, B. Roth, V. Katritch   +3 more
semanticscholar   +1 more source

Neuromodulator Dynamics Underlying Associative Learning in the Ventral Striatum's Olfactory Tubercle

Advanced Science, EarlyView.
Using fiber photometry and genetically encoded sensors, the dynamic release patterns of four neuromodulators in the olfactory tubercle (OT)—a brain region overlapping with the olfactory cortex and ventral striatum—were systematically monitored in response to external rewards and distinct reward‐associated learning processes.
Maojun Hong, Liuting Zou, Yiqing Chen, Juan Guo, Zhixiang Xu, Tong Ma, Shuaishuai Hu, Rongfeng K. Hu   +7 more
wiley   +1 more source

Regulation of CXCR4 function by S1P1 through heteromerization

Cell Communication and Signaling
Background The trafficking of immune cells between lymphoid organs and circulation depends on gradients of CXCL12 and sphingosine-1-phosphate (S1P), mediated through their cognate receptors C-X-C chemokine receptor type 4 (CXCR4) and S1P receptor type 1 (
Hyun-Tae Kim, Jae-Yeon Jeong, Won-Ki Huh
doaj   +1 more source

An Alternative Mode of GPCR Transactivation: Activation of GPCRs by Adhesion GPCRs

International Journal of Molecular Sciences
G protein-coupled receptors (GPCRs), critical for cellular communication and signaling, represent the largest cell surface protein family and play important roles in numerous pathophysiological processes. Consequently, GPCRs have become a primary focus in drug discovery efforts. Beyond their traditional G protein-dependent signaling pathways, GPCRs are
openaire   +2 more sources