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
Developing Allosteric Inhibitors of SARS-CoV-2 RNA-Dependent RNA Polymerase. [PDF]
Chayka A +10 more
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
Structural Models for a Series of Allosteric Inhibitors of IGF1R Kinase. [PDF]
Verma J, Vashisth H.
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
Structure features of Streptococcus pneumoniae FabG and virtual screening of allosteric inhibitors. [PDF]
Xu K, Zhong J, Li J, Cao Y, Wei L.
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
Theoretical study on the design of allosteric inhibitors of diabetes associated protein PTP1B. [PDF]
Zhan J, Liu Z, Gao H.
europepmc +1 more source
The FGF/FGFR System in the Biology and Therapeutic Landscape of Pediatric CNS Tumors
ABSTRACT Central nervous system (CNS) tumors are the most common solid malignancies in children, comprising a highly heterogeneous group of neoplasms defined by distinct molecular alterations and clinical behaviors. Advances in molecular genetics have underscored the relevance of specific signaling pathways in driving pediatric tumorigenesis, among ...
Serena Filiberti +6 more
wiley +1 more source
Inhibition of human mevalonate kinase by allosteric inhibitors of farnesyl pyrophosphate synthase. [PDF]
Salari S, Lee HF, Tsantrizos YS, Park J.
europepmc +1 more source

