Results 81 to 90 of about 151,004 (296)
BiomoleculesArtificial lipids have become increasingly important in generating novel nanoenzymes and nanoparticles. Imidazole has been well established as a versatile catalyst in synthetic chemistry and through its related amino acid histidine in enzymes.
Gabriela Sachet-Fernandez +3 more
doaj +1 more source
Advances in the allostery of angiotensin II type 1 receptor
Cell & Bioscience, 2023 Angiotensin II type 1 receptor (AT1R) is a promising therapeutic target for cardiovascular diseases. Compared with orthosteric ligands, allosteric modulators attract considerable attention for drug development due to their unique advantages of high ...
Xi Zhang +4 more
doaj +1 more source
Deconstructing Allostery: Computational Assessment of the Binding Determinants of Allosteric PTP1B Modulators [PDF]
, 2023 It is currently challenging to predict whether fragment hits that do not bind to an orthosteric site could be elaborated into allosteric modulators, as in these cases binding does not necessarily translate into a functional effect.
Silvia, Lovera +3 more
core +2 more sources
Translating whole‐genome doubling into precision medicine in cancer
Molecular Oncology, EarlyView.Whole‐genome doubling creates a WGD‐positive tumor state characterized by persistent chromosomal instability, karyotypic diversification, and cellular stress. These same biological pressures drive aggressive tumor evolution while exposing therapeutic vulnerabilities, providing a rationale for WGD‐informed precision medicine. Whole‐genome doubling (WGD)
Sejung Lee, Junghyeok Lim, Jinhyuk Bhin
wiley +1 more source
Molecular Oncology, EarlyView.Loss of NAPRT promotes lung tumor initiation and growth through a noncanonical mechanism, independent of its role in NAD+ biosynthesis. Mechanistically, NAPRT depletion activates the mTORC2‐driven AKT/β‐catenin signaling axis to enhance clonogenic and invasive phenotypes. Furthermore, lung‐specific Naprt deletion significantly increases tumor burden in
Myung Joon Oh +11 more
wiley +1 more source
Molecular Oncology, EarlyView.Taxanes are widely used chemotherapeutics whose effects on cellular mechanics remain poorly understood. We show that paclitaxel induces rapid cellular contraction by promoting GEF‐H1 dissociation from microtubules and non‐muscle myosin II activation through RhoA/ROCK.
Gloria Asensio‐Juárez +5 more
wiley +1 more source
Frontiers in Endocrinology, 2016 We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer.
Susanne Neumann +7 more
doaj +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
Calculating Transfer Entropy from Variance-Covariance Matrices Provides Insight into Allosteric Communication in ERK2 [PDF]
, 2020 Transfer entropy methods provide an approach to understanding asymmetric information flow in coupled systems, with particular application to understanding allosteric interactions in biomolecular systems.
Daniel, Barr +3 more
core +1 more source
Heterotropic regulation and negative homotropic cooperativity
FEBS Open Bio, EarlyView.We identified a structural module common to some proteins that couple negative cooperativity with heterotropic regulation, two features that rarely coexist. These proteins are ring‐like and present an ordered asymmetry whereby noncontacting subunits are symmetric, and their tertiary structure differs from that of contacting subunits.
Veronica Morea +5 more
wiley +1 more source