Results 141 to 150 of about 83,092 (356)

Modular Rh‐Catalyzed Synthesis and Biological Profiling of Diverse Pentafluorobenzenesulfonamide Reactive Fragments

Chemistry – A European Journal, EarlyView.
A modular Rh‐catalyzed synthetic approach enabled the preparation of diverse reactive fragments from available substrates. The reactive fragments modified Aurora A kinase via several distinct modification reaction classes. In a complex biological environment, the constellation of modified proteins depended critically on the reactive fragment structure.
Julian Chesti, Jennifer A. Miles, George J. Wade, Scott Grossman, George W. Preston, Richard Bayliss, Stuart L. Warriner, Megan H. Wright, Adam Nelson   +8 more
wiley   +1 more source

The Serotonin 2B (5‐HT2B) Receptor: A Narrative Review of Preclinical and Clinical Evidence on the Safety Considerations and Therapeutic Potential for the Treatment of Depression

Clinical Pharmacology &Therapeutics, EarlyView.
Major depressive disorder (MDD) and treatment‐resistant depression (TRD) remain leading causes of disability, providing the impetus for receptor‐level treatment strategies beyond monoamine reuptake. The serotonin 5‐HT2B receptor (5‐HT2BR) is uniquely positioned at the interface of central‐antidepressant mechanisms and peripheral cardiac risks.
Gia Han Le, Sabrina Wong, Danica E. Johnson, Diana K. Orsini, Yang Jing Zheng, Kayla M. Teopiz, Christine E. Dri, Joshua D. Rosenblat, Roger S. McIntyre   +8 more
wiley   +1 more source

Transmembrane receptors (GPCR) [PDF]

, 2016
GPCR (receptori na koje su vezani G-proteini) čine obitelj receptora sa sedam transmembranskih zavojnica (7TM receptori) koji prenose izvanstanični signal aktivirajući unutrastanične molekule, poznate pod nazivom sekundarni glasnici, koje su posrednici u
Sladić, Kristina
core  

Characterization of Ligand Binding to GPCRs Through Computational Methods

, 2017
The recent increase in available G protein-coupled receptor structures now contributes decisively to the structure-based ligand design. In this context, computational approaches in combination with medicinal chemistry and pharmacology are extremely ...
Silvana Vasile, Vasile, Silvana,, Jespers, Willem,, Hugo Gutiérrez-de-Terán, Mauricio Esguerra, Sallander, Jessica,, Oliveira, Ana,, Åqvist, Johan,, Ana Oliveira, Willem Jespers, Jessica Sallander, Johan Åqvist, Gutiérrez-de-Terán, Hugo,, Esguerra, Mauricio,   +13 more
core   +1 more source

toGC: A pipeline to correct gene model for functional excavation of dark GPCRs in Phytophthora sojae

Journal of Integrative Agriculture
The accuracy of genomic annotation is crucial for subsequent functional investigations; however, computational protocols used in high-throughput annotation of open reading frames (ORFs) can introduce inconsistencies.
Min Qiu, Chun Yan, Huaibo Li, Haiyang Zhao, Siqun Tu, Yaru Sun, Saijiang Yong, Ming Wang, Yuanchao Wang   +8 more
doaj   +1 more source

Structural elucidation of ligand binding sites in family B GPCRs and their application in drug discovery  [PDF]

, 2016
Ali Jazayeri, A.S. Dore, Daniel Lamb, Harini Krishnamurthy, Stacey M. Southall, Asma Baig, Andrea Bortolato, Markus Koglin, N.J. Robertson, James C. Errey, Stephen P. Andrews, Alastair Brown, Roger Cooke, Malcolm Weir, Fiona H. Marshall   +14 more
openalex   +1 more source

In silico analysis of putative interactions identifies fibroblasts as hubs for cell–cell communication during early regeneration of the zebrafish heart

Developmental Dynamics, EarlyView.
Abstract Background The zebrafish heart regenerates upon injury. During injury response, fibroblasts and endothelial cells accumulate at the site of damage, and cardiomyocyte cell cycle reentry allows cardiac muscle regrowth. It is relevant to understand how the different cell types communicate with each other to coordinate regeneration.
João A. S. Carvalho, Prateek Arora, Ines J. Marques, María Galardi‐Castilla, Louk Timmer, Eva van Rooij, Nadia Mercader   +6 more
wiley   +1 more source

P-Rex1 limits the agonist-induced internalization of GPCRs independently of its Rac-GEF activity

Cell Reports
Summary: The guanine-nucleotide exchange factor (GEF) P-Rex1 mediates G protein-coupled receptor (GPCR) signaling by activating the small GTPase Rac. We show here that P-Rex1 also controls GPCR trafficking.
Martin J. Baker, Elizabeth Hampson, Priota Islam, Ruben Pelaez Moral, Eve A. Maunders, Kirsti Hornigold, Elpida Tsonou, Angeliki Malliri, David C. Hornigold, Roderick E. Hubbard, Andrew J. Massey, Heidi C.E. Welch   +11 more
doaj   +1 more source

Transcriptomic signatures reveal systemic adaptations and immune modulation in response to training and competitive racing in horses

Equine Veterinary Journal, EarlyView.
Abstract Background The molecular mechanisms underlying adaptation to physical exertion and racing stress in horses remain incompletely understood. Peripheral blood transcriptomics offers a minimally invasive method to monitor systemic responses to exercise and identify biomarkers of adaptation or overload. Objectives To evaluate transcriptomic changes
Izabela Dąbrowska, Jowita Grzędzicka‐Agko, Paula Kiełbik, Michał Trela, Olga Witkowska‐Piłaszewicz   +4 more
wiley   +1 more source

Genome-wide pan-GPCR cell libraries accelerate drug discovery

Acta Pharmaceutica Sinica B
G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery.
Hanting Yang, Yongfu Wang, Wei Liu, Taiping He, Jiayu Liao, Zhongzhi Qian, Jinghao Zhao, Zhaotong Cong, Dan Sun, Zhixiang Liu, Can Wang, Lingping Zhu, Shilin Chen   +12 more
doaj   +1 more source