Results 111 to 120 of about 149,452 (339)
Optimal allosteric stabilization sites using contact stabilization analysis [PDF]
Journal of Computational Chemistry, 2016 Proteins can be destabilized by a number of environmental factors such as temperature, pH, and mutation. The ability to subsequently restore function under these conditions by adding small molecule stabilizers, or by introducing disulfide bonds, would be a very powerful tool, but the physical principles that drive this stabilization are not well ...
Alex, Dickson +2 more
openaire +2 more sources
Advanced Science, EarlyView.Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang +14 more
wiley +1 more source
Design of Allosteric Stimulators of the Hsp90 ATPase as New Anticancer Leads [PDF]
, 2017 Allosteric compounds that stimulate Hsp90 adenosine triphosphatase (ATPase) activity were rationally designed, showing anticancer potencies in the low micromolar to nanomolar range.
Agard, Da +10 more
core +1 more source
Advanced Science, EarlyView.This study reports a novel targeted protein degradation strategy termed “HSP70‐PROTAC” that recruits Hsc70 complex to a target protein for inducing degradation. Among them, GDAz‐3 exhibits effective GPX4 degradation activity via UPS/CMA processes, triggering ferroptosis‐driven anticancer activity in vitro and in vivo.
Jinyun Dong +15 more
wiley +1 more source
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
Simulation of spontaneous G protein activation reveals a new intermediate driving GDP unbinding [PDF]
, 2018 Activation of heterotrimeric G proteins is a key step in many signaling cascades. However, a complete mechanism for this process, which requires allosteric communication between binding sites that are ~30 Å apart, remains elusive.
Blumer, Kendall J +3 more
core +1 more source
Effects of insecticidal ketones present in mint plants on GABA A receptor from mammalian neurons [PDF]
, 2017 The genus Mentha, an important member of the Lamiaceae family, is represented by many species commonly known as mint. The insecticidal activity of Mentha oil and its main components has been tested and established against various insects/pests.
Delgado Marín, Leticia Ester +2 more
core +2 more sources
A New Paradigm for KIM-PTP Drug Discovery: Identification of Allosteric Sites with Potential for Selective Inhibition Using Virtual Screening and LEI Analysis [PDF]
, 2021 James Truslow Adams +2 more
openalex +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.A mutually exclusive screening system is established to identify negative regulators of highly plastic genes. Dual specificity phosphatase (DUSP9) is a novel negative regulatory molecule of PD‐L1 by dephosphorylating STAT3, and acts as a target molecule in combination with PD‐1 antibody for tumor immunotherapy and a new clinical biomarker for ...
Yuzhe Hu +9 more
wiley +1 more source