Results 81 to 90 of about 64,182 (259)

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

A Precision‐Delivered Singlet Oxygen Generator With an Inbuilt Safety Switch for Induction of Pancreatic Beta Cell Stress and Death

Angewandte Chemie, EarlyView.
ROXendin668 is a peptidic GLP‐1 receptor agonist that generates toxic singlet oxygen upon irradiation with far‐red light. Pancreatic beta cells can be photo‐ablated in a spatiotemporally controlled manner. This approach has the potential to provide a safer alternative to streptozotocin or alloxan for creating model systems for type 1 diabetes research.
Kilian Roßmann, Owen Bendor‐Samuel, Christopher Carlein, Kaja Rupar, Leticia Prates Roma, Ramona Birke, Tolga Soykan, Ingo Breng, Andreas Oder, Iona Davies, Ben Jones, Alice Adriaenssens, Michelle M. Martinez Irizarry, Rachael Morara, Martin Lehmann, Amelia K. Linnemann, David J. Hodson, Johannes Broichhagen   +17 more
wiley   +2 more sources

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

EphB1 Receptor Blockade Augments Morphine Antinociception via Inhibiting GRK2‐Mediated µ‐Opioid Receptor Internalization

Advanced Science, EarlyView.
Administration of opioids activates ephrinB2‐EphB1 receptor signaling. Activated EphB1 receptors induce GRK2‐mediated phosphorylation of MOR at Ser375, which initiates the internalization of MOR and reduces opioid antinociception at the behavioral level. ABSTRACT Opioids are the primary treatment for severe pain in clinical practice.
Bo Peng, Xiaqing Lin, Hongyu Yao, Cheng Li, Huabao Liao, Yuexin Liu, Boxu Cao, Xue‑Jun Song   +7 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

A Fluorogenic Cysteine‐Tetrapeptide Tagging Strategy for Nonperturbative Protein Labeling and Protein–Ligand Interaction Tracking

Advanced Science, EarlyView.
A compact Phe‐Cys‐Pro‐Phe (FCPF) tag and an environment‐sensitive SBD‐Cl‐derived probe form a sequence‐selective fluorogenic pair for wash‐free live‐cell protein imaging. This minimally perturbing chemistry allows flexible insertion at termini or loops, produces strong fluorescence upon local microenvironment confinement, supports FRET‐assisted ...
Xiao Wang, Xingcan Pan, Yongling Ying, Ziqian Bai, Jingming Zhang, Zhuang Shao, Jialiang Qian, Hongwei Li, Ning Zhang, Fan Yang, Yuan Liu, Xing Yang   +11 more
wiley   +1 more source

Gapless Complete Genome and Multi‐Omics Illuminate Immune Adaptation and Host‐Virus Interactions in a Coronavirus Reservoir

Advanced Science, EarlyView.
We present a complete T2T genome assembly for a key bat reservoir. Integrating population genomics, comparative genomics, transcriptomics, single‐cell omics, and functional assays, we resolve previously inaccessible genomic regions and identify evolutionary signatures associated with immune adaptation.
Yuting Wang, Sheng Zhang, Linxia Ouyang, Xin Du, Xin Huang, Zhilin Wang, Huixian Xie, Jiale Tang, Liyi Lou, Wenqing Ling, Weihao Wang, Jiang Zhou, Zhen Liu, Yibo Hu, Fuwen Wei, Guangping Huang   +15 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

Melatonin Mitigates Doxorubicin‐Induced Cardiotoxicity by Targeting the USP18/PKM2 Axis Without Compromising Antitumor Efficacy

Advanced Science, EarlyView.
Melatonin engages MT1/MT2 receptors to suppress STAT1‐driven USP18 upregulation, thereby redirecting PKM2 ubiquitination from K33‐linked autophagic degradation toward K27‐linked nuclear translocation. This prevents PKM2‐mediated proinflammatory gene expression in the heart, alleviating doxorubicin‐induced cardiotoxicity without compromising antitumor ...
Zhenyu Feng, Yijin Yang, Jie Bai, Pengqi Sun, Xuyang Sun, Jinshu Shang, Yang Liu, Zhen Ning, Ningning Zhang, Yun‐long Xia, Yunpeng Xie   +10 more
wiley   +1 more source