Results 111 to 120 of about 130,849 (328)

Clinofibrate Disrupts the SNORA80B/YTHDC1‐Driven M6A Modification to Suppress Cholesterol Metabolism and Cisplatin Resistance in ESCC

open access: yesAdvanced 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

Treatment of type 2 diabetes by free fatty acid receptor agonists [PDF]

open access: yes, 2014
Dietary free fatty acids (FFAs), such as ω-3 fatty acids, regulate metabolic and anti-inflammatory processes, with many of these effects attributed to FFAs interacting with a family of G protein-coupled receptors.
Hudson, Brian D.   +3 more
core   +2 more sources

An Aptamer‐Based EXACT Anticoagulant as a Sustainable, Animal‐Free Alternative to Unfractionated Heparin

open access: yesAdvanced 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

Genome-scale architecture of small molecule regulatory networks and the fundamental trade-off between regulation and enzymatic activity [PDF]

open access: yes, 2017
Metabolic flux is in part regulated by endogenous small molecules that modulate the catalytic activity of an enzyme, e.g., allosteric inhibition. In contrast to transcriptional regulation of enzymes, technical limitations have hindered the production of ...
Briars, Emma   +6 more
core   +2 more sources

Cinnamic‐Hydroxamic‐Acid Derivatives Exhibit Antibiotic, Anti‐Biofilm, and Supercoiling Relaxation Properties by Targeting Bacterial Nucleoid‐Associated Protein HU

open access: yesAdvanced 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

A three-level regulatory mechanism of the aldo-keto reductase subfamily AKR12D

open access: yesNature Communications
Modulation of protein function through allosteric regulation is central in biology, but biomacromolecular systems involving multiple subunits and ligands may exhibit complex regulatory mechanisms at different levels, which remain poorly understood. Here,
Zhihong Xiao   +13 more
doaj   +1 more source

Stochastic approach to molecular interactions and computational theory of metabolic and genetic regulations

open access: yes, 2006
Binding and unbinding of ligands to specific sites of a macromolecule are one of the most elementary molecular interactions inside the cell that embody the computational processes of biological regulations.
Ackers   +35 more
core   +1 more source

Author Response: PI(3,4,5)P3 allosteric regulation of repressor activator protein 1 controls antigenic variation in trypanosomes

open access: gold, 2023
Abdoulie O. Touray   +6 more
openalex   +1 more source

Precise Regulation of Membrane Proteins: From Physical Technology to Biomolecular Strategy

open access: yesAdvanced 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

Probing the activity modification space of the cysteine peptidase cathepsin K with novel allosteric modifiers.

open access: yesPLoS ONE, 2014
Targeting allosteric sites is gaining increasing recognition as a strategy for modulating the activity of enzymes, especially in drug design. Here we investigate the mechanisms of allosteric regulation of cathepsin K as a representative of cysteine ...
Marko Novinec   +2 more
doaj   +1 more source

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