Results 71 to 80 of about 61,856 (262)

Identifying GPCR-drug interaction based on wordbook learning from sequences

BMC Bioinformatics, 2020
Background G protein-coupled receptors (GPCRs) mediate a variety of important physiological functions, are closely related to many diseases, and constitute the most important target family of modern drugs.
Pu Wang, Xiaotong Huang, Wangren Qiu, Xuan Xiao   +3 more
doaj   +1 more source

Targeting Gi/o protein–coupled receptor signaling blocks HER2-induced breast cancer development and enhances HER2-targeted therapy

JCI Insight, 2021
GPCRs are highly desirable drug targets for human disease. Although GPCR dysfunction drives development and progression of many tumors, including breast cancer (BC), targeting individual GPCRs has limited efficacy as a cancer therapy because numerous ...
Cancan Lyu, Yuanchao Ye, Maddison M. Lensing, Kay-Uwe Wagner, Ronald J. Weigel, Songhai Chen   +5 more
doaj   +1 more source

Von In‐Silico bis In‐Cerebro – Entwicklung des Orexinrezeptor Antagonisten „Photorexant“ zur Photomodulation In Vitro und im Gehirn der Maus

Angewandte Chemie, EarlyView.
Durch einen strukturbasierten Designansatz wurden photoschaltbare Derivate des von der FDA zugelassenen Arzneistoffes Suvorexant entwickelt, gedockt, synthetisiert und pharmakologisch an den Orexin‐1‐ und 2‐Rezeptoren (OX1R und OX2R) charakterisiert.
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

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

In Silico to In Cerebro—Development of the Orexin Receptor Antagonist “Photorexant” for Photomodulation In Vitro and in Mouse Brains

Angewandte Chemie International Edition, EarlyView.
Following a structure‐based design approach, photoswitchable derivatives of the FDA‐approved drug suvorexant were designed, docked, synthesized, and characterized pharmacologically at the orexin 1 and 2 receptors (OX1R and OX2R). Optimized “photorexant” showed up to an 11‐fold difference in IC50 between photoisomers, enabled dynamic and reversible ...
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

Editorial: Insights in cellular endocrinology: 2022

Frontiers in Endocrinology, 2023
Ralf Jockers, Oreste Gualillo
doaj   +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

Activation of the pituitary adenylate cyclase-activating polypeptide type I receptor promotes neuroblastoma proliferation and migration through distinct G protein pathways

Cell Communication and Signaling
The pituitary adenylate cyclase-activating polypeptide type I receptor (PAC1R) is a class B G protein-coupled receptor implicated in a variety of physiological and pathological processes, including cancer.
Sarah Jang, Jae-Yeon Jeong, Won-Ki Huh
doaj   +1 more source

Quantum Phenomena in Molecular and Biological Systems: A Decoherence‐Based Decision Framework With Falsifiable Predictions and a Failure‐Mode Taxonomy

Advanced Physics Research, EarlyView.
A physics‐grounded framework based on decoherence timescales (τ_dec vs τ_func), Markovian validity, and falsifiability criteria is applied across molecular systems to distinguish where quantum effects are necessary, marginal, or irrelevant. The analysis integrates quantum chemistry, biological quantum mechanisms, and quantum computing under a unified ...
Sarfaraz K. Niazi
wiley   +1 more source