Results 141 to 150 of about 131,252 (300)

Determination of the Cannabinoid CB1 Receptor’s Positive Allosteric Modulator Binding Site through Mutagenesis Studies

Pharmaceuticals
Positive allosteric modulators (PAMs) of the cannabinoid CB1 receptor (CB1) offer potential therapeutic advantages in the treatment of neuropathic pain and addiction by avoiding the adverse effects associated with orthosteric CB1 activation.
Hayley M. Green, Daniel M. J. Fellner, David B. Finlay, Daniel P. Furkert, Michelle Glass   +4 more
doaj   +1 more source

Supramolecular Allostery Achieves Tunable Luminescence Aromatic Bridged Phenothiazine Noncovalent Frameworks

Advanced Science, EarlyView.
Tunable luminescent supramolecular organic framework enabled by multiple allosteric effects, composed of a tetracation vinylphenylpyridinium‐modified aromatic‐bridged phenothiazine guest and cucurbit[8]uril, not only exhibits unique guest oxidation‐driven NIR luminescence blue‐shift and effectively enhances the quantum yield by 46‐fold to 22.2% but ...
Xinping Lu, Jianchong Chen, Jie Yu
wiley   +1 more source

Machine learning approaches in predicting allosteric sites [PDF]

Allosteric regulation is a fundamental biological mechanism that can control critical cellular processes via allosteric modulator binding to protein distal functional sites.
Zoe, Cournia, Francho, Nerín-Fonz
core   +2 more sources

Co‐activation of Selective Nicotinic Acetylcholine Receptor Subtypes Is Required for Neuroprotection against Alzheimer's Disease

Advanced Science, EarlyView.
ABSTRACT Beta‐amyloid peptide (Aβ)‐induced suppression of hippocampal GABAergic interneuron activity drives hyperexcitability, amyloid pathology, and cognitive impairment in Alzheimer's disease (AD), suggesting that enhancing hippocampal inhibition may be protective.
Rahmi Lee, Gayeon Kim, Ellison R. Black, Seonil Kim   +3 more
wiley   +1 more source

Allosteric modulators of M1 muscarinic receptors enhance acetylcholine efficacy and decrease locomotor activity and turning behaviors in zebrafish

Scientific Reports
Allosteric modulation of muscarinic acetylcholine receptors (mAChR) has been identified as a potential strategy for regulating cholinergic signaling in the treatment of various neurological disorders.
Corey J. Widman, Sestina Ventresca, Jillian Dietrich, Gwendolynne Elmslie, Hazel Smith, Gina Kaup, Aaron Wesley, Madeline Doenecke, Frederick E. Williams, Isaac T. Schiefer, John Ellis, William S. Messer Jr.   +11 more
doaj   +1 more source

FBP1‐Mediated Compartmentalization of Glycolytic Enzyme Complexes Suppresses PKM2 Function to Ameliorate MASLD Progression

Advanced Science, EarlyView.
In normal hepatocytes, FBP1 forms compartmentalized complexes with PKM2, ENO1, and LDHA independent of its catalytic activity, inhibiting PKM2 activity and restricting excessive glycolysis. During MASLD progression, FBP1 downregulation markedly reduces the abundance of these complexes and releases the “hijacked” glycolytic enzymes, leading to PKM2 ...
Busong Wang, Yiping Tang, Na Li, Xuening Dai, Jing Wu, Bin Xue, Yuxin Chen, Jingzi Zhang, Lingdong Kong, Chaojun Li, Lei Fang   +10 more
wiley   +1 more source

Noncanonical Peloruside A Biosynthesis by an Uncultivated Verrucomicrobiota Symbiont

Angewandte Chemie, EarlyView.
Noncanonical biochemistry of the peloruside PKS characterized in this work, comprising double bond generation by a noncanonical tridomain (blue), acetyl‐CoA recycling (orange), and proofreading systems (purple and yellow). The Z‐double bond is installed by TEB1 through O‐acetylation and acetate elimination. The acyl ligase PelB (AL, orange) selectively
Amy E. Fraley, Michael Rust, Moritz Wagner, Ida R. Hipfinger, Paul J. N. Böhm, Cora L. Dieterich, Christopher M. Field, Michael J. Page, Jeremy G. Owen, Robert A. Keyzers, Shinichi Sunagawa, Jörn Piel   +11 more
wiley   +2 more sources

Bioenergetic Materials for Tissue Regeneration: Modulating Metabolism to Promote Cellular Anabolism

Advanced Science, EarlyView.
Bioenergetic materials (BEMs) modulate cellular metabolism to promote tissue regeneration. Their principal mechanisms of action include metabolic substrate supplementation, metabolic enzyme modulation, organelle transfer, electrical current regulation, redox homeostasis modulation, and oxygen tension modulation.
Yuchen He, Yuwen Wang, Jonathan F. Gong, Yiting Lei, Fei Jin, Weihong Zhu, Rocky S. Tuan, Zhong Alan Li   +7 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

Angewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma, Komal Sharma, Anku Sharma, Kamya Rao, Rahul Jain, Brett VanVeller   +5 more
wiley   +2 more sources

Transport–Reaction–Signal Coupling in Lateral Flow Assays for Next‐Generation Point‐of‐Care Diagnostics

Advanced Science, EarlyView.
Lateral flow assays are evolving into interdisciplinary, system‐level sensing platforms. Recent innovations are deconstructed through coupled phases of mass transfer, reaction, and signal transduction, revealing interdependence across porous materials, interfacial chemistry, nanolabels, readout devices, and data‐enabled analysis.
Yan Pan, Yuewei Li, Chao Mi, Zhengwen Yang, Lana McClements, Steven J. Langford, Jiayan Liao   +6 more
wiley   +1 more source