Abstract Background Neurodegeneration with Brain Iron Accumulation (NBIA) is a heterogeneous group of heritable, mostly recessive, progressive neurodegenerative diseases characterized by iron deposition in the basal ganglia and brainstem. There are no solid global epidemiological data on prevalence and incidence of NBIA subtypes, but registry data and ...
Susanne A. Schneider +3 more
wiley +1 more source
Terpene-Based Thiazole Hydrazines as Negative Allosteric Modulators of MRGPRX4: In Vitro Evaluation and Binding Site Analysis. [PDF]
Haider S +5 more
europepmc +1 more source
Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley +1 more source
Efficient Characterization of GPCRs Allosteric Modulation: Application to the Rational Design of De Novo S1PR1 Allosteric Modulators. [PDF]
Cruz A, Warshel A.
europepmc +1 more source
Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino +3 more
wiley +1 more source
Brexanolone, zuranolone and related neurosteroid GABA<sub>A</sub> receptor positive allosteric modulators for postnatal depression. [PDF]
Wilson CA +6 more
europepmc +1 more source
ABSTRACT The Nav1.5 channel, a major isoform of voltage‐gated sodium ion channel, is mainly found in ventricular cardiomyocytes, playing a key role in generating essential cardiac action potentials for normal heart rhythms. Mutations in Nav1.5 have been associated with severe heart conditions such as long QT syndrome, Brugada syndrome, cardiac ...
Arkapravo Chattopadhyay +3 more
wiley +1 more source
The Discovery of Bridged Benzoazepine Amides as Selective Allosteric Modulators of RIPK1. [PDF]
Chen JL +19 more
europepmc +1 more source
Hsp90 Inhibition on the Western Blot: N‐Terminal Versus C‐Terminal Inhibitors in Breast Cancer
ABSTRACT Heat shock protein 90 (Hsp90) is an established and clinically validated anticancer target. By regulating the folding and maturation of diverse client proteins, it is indirectly involved in carcinogenesis. Key breast cancer oncogenic drivers, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, are ...
Jaka Dernovšek +3 more
wiley +1 more source
Short-term sleep benefits <i>versus</i> long-term pulmonary risks: an updated meta-analysis of benzodiazepine receptor positive allosteric modulators in COPD patients with comorbid insomnia. [PDF]
Cui XJ, Xie B, Yi XQ, Li PF.
europepmc +1 more source

