Results 101 to 110 of about 4,452,404 (339)
Nature Communications, 2020 Allosteric regulation is an innate control in most metabolic and signalling cascades that enables living organisms to adapt to the changing environment by tuning the affinity and regulating the activity of target proteins. For a microscopic understanding
Olga Bozovic +2 more
doaj +1 more source
Advanced Science, EarlyView.This study uncovers a non‐canonical role of SNORA80B in ESCC, showing it mediates AR‐driven metabolic reprogramming via N⁶‐methyladenosine (m6A) methylation. By binding YTHDC1, SNORA80B stabilizes cholesterol‐metabolic enzyme mRNAs and promotes tumor progression. The FDA‐approved drug clinofibrate inhibits SNORA80B by disrupting cholesterol homeostasis,
Hongyu Yuan +7 more
wiley +1 more source
Orthosteric and allosteric binding sites of P2X receptors [PDF]
European Biophysics Journal, 2008 P2X receptors for ATP comprise a distinct family of ligand gated ion channels with a range of properties. They have been shown to be involved in a variety of physiological processes including blood clotting, sensory perception, pain sensation, bone formation as well as inflammation and may provide a number of novel drug targets.
openaire +3 more sources
Advanced Science, EarlyView.By simply conjugating thrombin's active‐site inhibitor, dabigatran, with an exosite inhibitor, aptamer HD1, the resulting EXosite‐ACTive site (EXACT) inhibitors show two orders of magnitude higher potency and selectivity via synergistic binding, while maintaining the aptamer's antidote‐reversible trait, yielding a potential substitute for the animal ...
Haixiang Yu +11 more
wiley +1 more source
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 +6 more
doaj +1 more source
Advanced Science, EarlyView.Cinnamic‐hydroxamic‐acid derivatives (CHADs) are identified as novel inhibitors of the bacterial nucleoid‐associated protein HU, exhibiting potent antibacterial, anti‐biofilm (both inhibition and eradication), and DNA relaxation (anti‐supercoiling) activities. Moreover, CHADs demonstrate strong synergistic effects with multiple antibiotics.
Huan Chen +22 more
wiley +1 more source
Precise Regulation of Membrane Proteins: From Physical Technology to Biomolecular Strategy
Advanced Science, EarlyView.This review summarizes the emerging strategies for the precise regulation of membrane proteins using physical stimuli and biomolecule‐based tools. These methods provide new insights into cell regulation and offer promising directions for future disease treatment.
Xiu Zhao +6 more
wiley +1 more source
Semi-explicit Solvation Improves Ligand Binding Site Design in an Allosteric Protein [PDF]
, 2020 Zion R. Perry +2 more
openalex +1 more source
Journal of Medicinal Chemistry, 2015 Undesirable side effects associated with orthosteric agonists/antagonists of cannabinoid 1 receptor (CB1R), a tractable target for treating several pathologies affecting humans, have greatly limited their translational potential. Recent discovery of CB1R
P. Kulkarni +12 more
semanticscholar +1 more source
Advanced Science, EarlyView.Punicalagin, a pomegranate molecule, helps the body fight Mycobacterium abscessus. It preferentially boosts interstitial macrophages in the lung, stabilizing mitochondria and switching on the autophagy via SIRT1/FoxO3a, which lowers bacterial load without directly killing bacteria.
Kefan Bi +4 more
wiley +1 more source