Results 91 to 100 of about 92,511 (354)

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

Concepts of GPCR‐controlled navigation in the immune system

Immunological Reviews, 2019
G‐protein–coupled receptor (GPCR) signaling is essential for the spatiotemporal control of leukocyte dynamics during immune responses. For efficient navigation through mammalian tissues, most leukocyte types express more than one GPCR on their surface ...
T. Lämmermann, W. Kastenmüller
semanticscholar   +1 more source

The evolution and mechanism of GPCR proton sensing

Journal of Biological Chemistry, 2020
Of the 800 G protein–coupled receptors (GPCRs) in humans, only three (GPR4, GPR65, and GPR68) regulate signaling in acidified microenvironments by sensing protons (H+). How these receptors have uniquely obtained this ability is unknown.
J. Rowe, N. Kapolka, G. Taghon, William M Morgan, D. Isom   +4 more
semanticscholar   +1 more source

Genetically‐Programmed Hypervesiculation of Lactiplantibacillus Plantarum Increases Production of Bacterial Extracellular Vesicles with Therapeutic Efficacy in a Preclinical Inflammatory Bowel Disease Model

Advanced Science, EarlyView.
The development of a novel engineered strain of Lactiplantibacillus plantarum (Lp) is reported that can produce bacterial extracellular vesicles (BEVs) at >60‐fold higher yields than the unmodified parental strain. These Lp BEVs retain therapeutic bioactivity as validated in a mouse model of dextran sodium sulfate‐induced colitis.
Nicholas H Pirolli, Daniel Levy, Alyssa Schledwitz, Natalia Sampaio Moura, Mitali Sarkar, Talia J. Solomon, Emily H. Powsner, Raith Nowak, Zuzanna Mamczarz, Christopher J. Bridgeman, Sulayman Khan, Andrew Hui, Nidhi Anne, Laura Reus, William E. Bentley, Jean‐Pierre Raufman, Steven M. Jay   +16 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

G12/13 is activated by acute tethered agonist exposure in the adhesion GPCR ADGRL3

Nature Chemical Biology, 2020
The adhesion G-protein-coupled receptor (GPCR) latrophilin 3 (ADGRL3) has been associated with increased risk of attention deficit hyperactivity disorder (ADHD) and substance use in human genetic studies.
Signe Mathiasen, T. Palmisano, Nicole A. Perry, Hannah M. Stoveken, Alex Vizurraga, Dyke P. McEwen, Najeah Okashah, T. Langenhan, A. Inoue, N. Lambert, G. Tall, J. Javitch   +11 more
semanticscholar   +1 more source

Integrated ERK‐PKA‐YAP/TAZ‐SHH Signaling Orchestrates Cortical Radial Glia Identity and Lineage Diversification

Advanced Science, EarlyView.
This study shows that ERK/PKA upregulation in mammalian cortical radial glia (RGs) sustains neurogenesis and suppresses gliogenesis. YAP/TAZ activation promotes ependymal cell formation, while enhanced SHH‐SMO signaling induces astrocyte, oligodendrocytes, and olfactory bulb interneuron generation.
Zhuangzhi Zhang, Zhejun Xu, Tongye Fu, Jialin Li, Feihong Yang, Chuannan Yang, Wenhui Zheng, Zizhuo Sha, Yanjing Gao, Mengge Sun, Zhenmeiyu Li, Jing Ding, Xiaosu Li, Zhengang Yang   +13 more
wiley   +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

Electrosensitive Heterogeneous Short Fibers via Acousto‐Electric Coupling for Sequential Bone Regeneration in Infectious Defects

Advanced Science, EarlyView.
Electrosensitive heterogeneous short fibers can accurately respond to ultrasonic field regulation through the synergistic interaction of piezoelectric and conductive dual elements. At an ultrasound intensity of 1.5 W cm−2, it can effectively activate bacterial peroxisome and necrotic apoptotic pathway and promote bacterial apoptosis.
Xiaoyu Han, Fan Wang, Pengcheng Xiao, Zheng Yang, Mingyue Liu, Zeyu Han, Zijie Wang, Anan Jiang, Jindong Tan, Juan Wang, Wenguo Cui, Dingqun Bai   +11 more
wiley   +1 more source