Results 241 to 250 of about 67,162 (289)

Allosteric regulation of Keap1 by 8β-hydroxy-α-cyclocostunolide for the treatment of acute lung injury. [PDF]

Acta Pharm Sin B
Zhang J, Zhang M, Zhu QM, Xu XR, Feng YL, Lin S, Qiu F, Sun CP.   +7 more
europepmc   +1 more source

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

The return of metabolism: biochemistry and physiology of glycolysis

Biological Reviews, EarlyView.
ABSTRACT Glycolysis is a fundamental metabolic pathway central to the bioenergetics and physiology of virtually all living organisms. In this comprehensive review, we explore the intricate biochemical principles and evolutionary origins of glycolytic pathways, from the classical Embden–Meyerhof–Parnas (EMP) pathway in humans to various prokaryotic and ...
Nana‐Maria Grüning, Federica Agostini, Camila Caldana, Johannes Hartl, Matthias Heinemann, Markus A. Keller, Jan Lukas Krüsemann, Costanza Lamperti, Carole L. Linster, Steffen N. Lindner, Julia Muenzner, Jens Nielsen, Zoran Nikoloski, Bettina Siebers, Jacky L. Snoep, Hezi Tenenboim, Bas Teusink, Spencer J. Williams, Mirjam M. C. Wamelink, Markus Ralser   +19 more
wiley   +1 more source

A helical fulcrum in eIF2B coordinates allosteric regulation of stress signaling. [PDF]

Nat Chem Biol
Lawrence RE, Shoemaker SR, Deal A, Sangwan S, Anand AA, Wang L, Marqusee S, Walter P.   +7 more
europepmc   +1 more source

Clinical Applications of Phosphoproteomics: Illuminating Cancer Signaling and Enabling Rational Therapeutic Strategies

Cancer Science, EarlyView.
Mass spectrometry‐based phosphoproteomics for mechanistic dissection of cancer signaling pathways and uncovering therapeutic vulnerabilities. ABSTRACT Protein phosphorylation is a central post‐translational modification regulating cellular signaling, frequently dysregulated in cancer.
Hirokazu Shoji, Narikazu Boku, Jun Adachi   +2 more
wiley   +1 more source

Allosteric regulation of nitrate transporter NRT via the signaling protein PII. [PDF]

Proc Natl Acad Sci U S A
Li B, Wang XQ, Li QY, Xu D, Li J, Hou WT, Chen Y, Jiang YL, Zhou CZ.   +8 more
europepmc   +1 more source

Potassium–chloride cotransporter 2 activity dampens induced ictal‐like activity in neocortical slices containing the seizure propagation zone of temporal lobe epilepsy patients

Epilepsia, EarlyView.
The K⁺/Cl− cotransporter (KCC2) limits induced ictal‐like events and their spread in the supragranular layer of human neocortical slices from the seizure‐propagation zone of temporal lobe epilepsy patients. Cl⁻ extrusion is present in supragranular pyramidal neurons but limited under high somatic Cl⁻ load.
Alice Falck, Janna Lehnhoff, Mahraz Behbood, Egor Byvaltcev, Annette Aigner, Helena Radbruch, Pawel Fidzinski, Jan‐Hendrik Schleimer, Gabriel M. S. Janach, Noah Döhne, Julia Onken, Thilo Kalbhenn, Thomas Sauvigny, Rudolf A. Deisz, Susanne Schreiber, Martin Holtkamp, Ulf Strauss   +16 more
wiley   +1 more source

A randomized, double‐blind, placebo‐controlled, multicenter study to evaluate the efficacy and safety of adjunctive cenobamate in Asian patients with focal seizures

Epilepsia, EarlyView.
A randomized, double‐blind, placebo‐controlled, multicenter study to evaluate the efficacy and safety of adjunctive cenobamate in Asian patients with focal seizures. Abstract Objectives This randomized, double‐blind, placebo‐controlled study (NCT04557085), conducted in China, Japan, and the Republic of Korea, evaluated the efficacy and safety of ...
Sang Kun Lee, Peimin Yu, Eunyeong Choe, Louis Ferrari, Kyoung Heo, Seung Bong Hong, Zhen Hong, Koji Iida, Yong Heui Jeon, Jiwon Jung, Marc Kamin, Kensuke Kawai, Ji Hyun Kim, Myung Won Kim, Xiaorong Liu, Jungshin Park, William E. Rosenfeld, Takamichi Yamamoto, Dong Zhou, Suiqiang Zhu, Sunita N. Misra   +20 more
wiley   +1 more source

Dynamic inter-domain transformations mediate the allosteric regulation of human 5, 10-methylenetetrahydrofolate reductase. [PDF]

Nat Commun
Blomgren LKM, Huber M, Mackinnon SR, Bürer C, Baslé A, Yue WW, Froese DS, McCorvie TJ.   +7 more
europepmc   +1 more source

Modifying inhibitor specificity for homologous enzymes by machine learning

The FEBS Journal, EarlyView.
We present a machine learning method for the design of selective enzyme inhibitors, reducing experimental effort thus accelerating the development of targeted therapeutics. Trained on existing data for three related matrix metalloproteinases (MMPs), our method successfully designed a novel inhibitor variant with enhanced selectivity for one MMP over ...
Dor S. Gozlan, Reut Meiri, Gili Shapira, Matt Coban, Evette S. Radisky, Yaron Orenstein, Niv Papo   +6 more
wiley   +1 more source