Results 101 to 110 of about 2,925,762 (288)
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.An artificial bifunctional N‐deacetylase/N‐sulfotransferase was engineered in Escherichia coli by combining screened N‐deacetylases with an NST domain. The integrated engineering strategy improved enzyme performance. The optimized enzyme efficiently converted heparosan into N‐sulfated heparosan, addressing a key bottleneck in microbial heparin ...
Xintong Xi +8 more
wiley +1 more source
Identification of a Novel Inhibitory Allosteric Site in p38α
PLOS ONE, 2016 In the present study, we report the discovery of a novel allosteric inhibitory site for p38α, a subclass of the mitogen-activated protein kinases (MAPK) family. The putative site was discovered after inspection of the crystallographic structure of the p38α-MK2 complex.
Patricia Gomez-Gutierrez +3 more
openaire +4 more sources
Advanced Science, EarlyView.Engineering of the 148‐germline (148‐GL) antibody reveals a roadmap for overcoming SARS‐CoV‐2 viral escape. By introducing four specific somatic hypermutations, the resulting 148‐M4 variant restores potent neutralization against Omicron BA.1 and BA.4/5.
Huibin Lv +14 more
wiley +1 more source
Advanced Science, EarlyView.ABSTRACT Amplification‐free Cas12a diagnostics with split crRNA enable rapid and programmable target recognition, yet insufficient understanding of DNA activator architecture prevents predictable control over trans‐cleavage activity and sensitivity. Here we systematically map over 200 split DNA activator configurations by introducing nicks at every ...
Xiaoyan Tang +8 more
wiley +1 more source
An evolutionarily conserved allosteric site modulates beta-lactamase activity
, 2016 Declining efficiency of antibiotic-inhibitor combinatorial therapies in treating beta-lactamase mediated resistance necessitates novel inhibitor development.
Akbulut, Berna Sariyar +4 more
core +2 more sources
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
Identification of a Lipid-Exposed Extrahelical Binding Site for Positive Allosteric Modulators of the Dopamine D₂ Receptor [PDF]
Recently, the first small-molecule positive allosteric modulators (PAMs) of the dopamine D2 receptor (D2R) were identified. The more potent PAM potentiated the effects of D2R signaling in vitro and in an in vivo model predictive of anti-Parkinson’s ...
Wood, Martyn +13 more
core +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
Cancer‐Associated BCL‐2 Mutants Reveal Mechanisms Towards Venetoclax Resistance
Advanced Science, EarlyView.Venetoclax (VEN) resistance in chronic lymphocytic leukemia arises from diverse BCL2 mutations. We map mechanisms contributing to VEN resistance across common BCL‐2 variants. G101V and D103Y reduce drug binding and increase sequestration of pro‐apoptotic proteins. V156D blocks VEN allosterically.
Jonas Aufdermauer +9 more
wiley +1 more source