Results 91 to 100 of about 31,985 (308)

A pilot study comparing the metabolic profiles of elite-level athletes from different sporting disciplines [PDF]

, 2018
Background: The outstanding performance of an elite athlete might be associated with changes in their blood metabolic profile. The aims of this study were to compare the blood metabolic profiles between moderate- and high-power and endurance elite ...
A Boldyrev, A Leibowitz, AA Ferrando, AA Smith, B Lecka-Czernik, C Fasolato, C Harteneck, C Morris, CL Hoppel, D Belelli, D Fietz, E Asmussen, E Chorell, E Pohjanen, G Lac, G Van Hall, GC Bogdanis, GD Lewis, GJ Rietjens, H Budde, H Budde, H Karlic, H Yokoyama, J Henriksson, JB Walker, JH Mitchell, JK Nicholson, JM Peake, JS Fuqua, K Goto, K Sahlin, K Sahlin, K Sato, K Sato, KR Howarth, LS Eriksson, ME Powers, MH Jacob, MH Williams, MJ Ormsbee, ML Circu, ML Goodwin, P Yin, PC Tullson, R Berton, RF Coburn, S Naz, SC Lu, SK Powers, TE Graham, W Dudzinska, YP Pitsiladis   +51 more
core   +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

Unnatural Tripeptides as Potent Positive Allosteric Modulators of T1R2/T1R3 [PDF]

ACS Medicinal Chemistry Letters, 2019
T1R2/T1R3 belongs to G protein coupled receptors, which recognizes diverse natural and synthetic sweeteners. A novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 was identified through high-throughput screening campaign. Comparing the structure of the potent compound with previously known PAM, we classified the structure of known PAM ...
Kei Yamada, Masakazu Nakazawa, Kayo Matsumoto, Uno Tagami, Takatsugu Hirokawa, Keisuke Homma, Suguru Mori, Ryo Matsumoto, Wakana Saikawa, Seiji Kitajima   +9 more
openaire   +2 more sources

The phytocannabinoid, Δ(9) -tetrahydrocannabivarin, can act through 5-HT1 A receptors to produce antipsychotic effects [PDF]

, 2015
Funded by: •GW Pharmaceuticals Acknowledgements: The authors wish to thank Mrs Lesley Stevenson for technical support and Dr John Raymond, Dr Keith Parker and Dr Ethan Russo for providing human 5-HT1A CHO cells.
Cascio, Maria Grazia, Marini, Pietro, Parolaro, Daniela, Pertwee, Roger G., Zamberletti, Erica   +4 more
core   +1 more source

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

Evolution of sparsity and modularity in a model of protein allostery

, 2014
The sequence of a protein is not only constrained by its physical and biochemical properties under current selection, but also by features of its past evolutionary history.
Hemery, Mathieu, Rivoire, Olivier
core   +3 more sources

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

The 10–23 DNAzyme in Biosensing and Diagnostics: Applications, Challenges, and Future Directions

Angewandte Chemie, EarlyView.
This review focuses on the 10–23 DNAzyme in diagnostics, spanning unregulated and regulated target‐recognition modes, and their functionalization across colorimetric, fluorescent, electrochemical, electrochemiluminescent, and intracellular biosensing strategies.
Connor Nurmi, Jake Brill, Sanne Roumans, Amal Mathai, John D. Brennan, Yingfu Li   +5 more
wiley   +2 more sources

Positive Allosteric Modulators for mGluR2 Receptors: A Medicinal Chemistry Perspective [PDF]

Current Topics in Medicinal Chemistry, 2014
This review summarizes drug discovery efforts on mGluR2 positive allosteric modulators (PAMs) from 2000 to 2013. Medicinal chemistry programs and the identified 21 chemotypes are analyzed and compared in terms of their biological activity and ligand efficiency. Comparative analysis of ligand efficiency metrics including ligand efficiency and lipophilic
Szabó, György, Keserű, György Miklós   +1 more
openaire   +2 more sources

Synthetic Analogues of the Snail Toxin 6-Bromo-2-mercaptotryptamine Dimer (BrMT) Reveal That Lipid Bilayer Perturbation Does Not Underlie Its Modulation of Voltage-Gated Potassium Channels [PDF]

, 2018
Drugs do not act solely by canonical ligand–receptor binding interactions. Amphiphilic drugs partition into membranes, thereby perturbing bulk lipid bilayer properties and possibly altering the function of membrane proteins.
Aldrich, Richard W., Andersen, Olaf S., Dockendorff, Chris, Dodge, Matthew W., Eum, Kenneth S., Gandhi, Disha M., Ingolfsson, Helgi I., Kapoor, Ruchi, Kimball, Ian H., Martin, Stephen F., Peyear, Thasin, Rusinova, Radda, Sack, Jon T.   +12 more
core   +2 more sources