Results 121 to 130 of about 149,452 (339)

The mechanism of allosteric inhibition of protein tyrosine phosphatase 1B.

PLoS ONE, 2014
As the prototypical member of the PTP family, protein tyrosine phosphatase 1B (PTP1B) is an attractive target for therapeutic interventions in type 2 diabetes.
Shuai Li, Jingmiao Zhang, Shaoyong Lu, Wenkang Huang, Lv Geng, Qiancheng Shen, Jian Zhang   +6 more
doaj   +1 more source

Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor [PDF]

, 2010
L-glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a fundamental role in the control of motor function, cognition and mood.
Grove, Simon J .A., Jamieson, Craig, Maclean, John K. F., Morrow, John A., Rankovic, Zoran   +4 more
core   +1 more source

Resolvin D5 Inhibits CXCL8 Expression in Colonic Epithelial Cells Through Activating GPR101 to Impede Neutrophil Recruitment and Consequently Alleviate Ulcerative Colitis

Advanced Science, EarlyView.
RvD5 effectively alleviates UC by inhibiting STAT1 signaling to reduce CXCL8 expression in colonic epithelial cells via activation of GPR101, which subsequently decreases the infiltration of neutrophils in the colonic mucosal epithelium. Epimedin A1, a natural allosteric inhibitor of 5‐LOX, demonstrates potential as a therapeutic agent for UC by ...
Pengxiang Guo, Yilei Guo, Yanrong Zhu, Ke Yan, Yulai Fang, Jiafeng Zhang, Yue He, Zhifeng Wei, Yufeng Xia, Yue Dai   +9 more
wiley   +1 more source

p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia [PDF]

, 2011
Background: The t(9;22) translocation leads to the formation of the chimeric breakpoint cluster region/c-abl oncogene 1 (BCR/ABL) fusion gene on der22, the Philadelphia chromosome.
Mahajna, Jamal, Metodieva, Anna, Mian, Afsar Ali, Najajreh, Yousef, Ottmann, Oliver Gerhard, Ruthardt, Martin   +5 more
core   +2 more sources

Halorotetin B, A Novel Terpenoid Compound Derived from Marine Ascidian, Suppresses Tumor Growth by Targeting the Cell Cycle Regulator UBE2C

Advanced Science, EarlyView.
Halorotetin B, a novel small‐molecule terpenoid identified from an edible marine ascidian, exhibits strong anti‐tumor activity both in vitro and in vivo through direct targeting UBE2C to induce tumor cell cycle arrest and then lead tumor cell senescence. As a newly discovered UBE2C inhibitor, Halorotetin B can serve as a novel potential cell senescence
Shanhao Han, Jianhui Li, Yuting Zhu, Penghui Liu, Yaoyao Zheng, Muchun He, Bo Dong   +6 more
wiley   +1 more source

Targeting the GPX4–FUNDC1 Interaction with Magnesium Lithospermate B Attenuates Sepsis‐Associated Lung Injury

Advanced Science, EarlyView.
The diagram depicts the endothelial‐protective mechanism of magnesium lithospermate B (MLB) in sepsis‐associated lung injury. MLB binds GPX4 at Gly79, disrupts its interaction with FUNDC1, prevents mitophagy‐mediated GPX4 degradation, restores mitophagic flux, reduces ROS, and limits ferroptosis.
Zhixi Li, Chang Liu, Zhaoxue Ma, Dongyou Zheng, Renkai Wang, Yongjing Yu, Guangmin Chen, Chenglong Li, Yue Bu, Hang Cao, Bing Zhang   +10 more
wiley   +1 more source

Identification of the Allosteric Regulatory Site of Insulysin

PLoS ONE, 2011
Insulin degrading enzyme (IDE) is responsible for the metabolism of insulin and plays a role in clearance of the Aβ peptide associated with Alzheimer's disease. Unlike most proteolytic enzymes, IDE, which consists of four structurally related domains and exists primarily as a dimer, exhibits allosteric kinetics, being activated by both small substrate ...
Nicholas Noinaj, Sonia K Bhasin, Eun Suk Song, Kirsten E Scoggin, Maria A Juliano, Luiz Juliano, Louis B Hersh, David W Rodgers   +7 more
openaire   +3 more sources

GPCRs in CAR‐T Cell Immunotherapy: Expanding the Target Landscape and Enhancing Therapeutic Efficacy

Advanced Science, EarlyView.
Chimeric antigen receptor T cell therapy faces dual challenges of target scarcity and an immunosuppressive microenvironment in solid tumors. This review highlights how G protein‐coupled receptors can serve as both novel targets to expand the therapeutic scope and functional modules to enhance CAR‐T cell efficacy.
Zhuoqun Liu, Yuchen Xiao, Yamin Zhao, Lihe Dai, David J.H. Shih, Shikang Liang, Honglei Tian, Liu Liu, Feng Tian, Bing Liu, Lei Chang, Chao Zhang   +11 more
wiley   +1 more source

Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention [PDF]

, 2021
Hayley Whitfield, Andrew M. Hemmings, Stephen Mills, Kendall Baker, Gaye F. White, Stuart A. Rushworth, Andrew M. Riley, Barry V. L. Potter, Charles A. Brearley   +8 more
openalex   +1 more source

Cryo‐EM Structures Reveal the Molecular Basis of Asymmetric Allosteric Activation by MMOB in the Hydroxylase of Soluble Methane Monooxygenase

Advanced Science, EarlyView.
Cryo‐EM analysis reveals an asymmetric MMOH–MMOB complex with distinct protomers, where MMOB binding triggers structural rearrangements from the surface to the active site. This conformational asymmetry shortens the Fe···Fe distance to 2.7 Å in one protomer, forming a geometry suitable for O2 activation and supporting a sequential catalytic mechanism ...
Yunha Hwang, Bumhan Ryu, Soyeon Park, Dong‐Heon Lee, Hyo Jin Hong, Jeong‐Geol Na, Chul Gyu Song, Hyun Goo Kang, Edwin Pozharski, Seung Jae Lee   +9 more
wiley   +1 more source