Results 41 to 50 of about 692,160 (279)
Tyrosine phosphatase SHP2 inhibitors in tumor-targeted therapies
Acta Pharmaceutica Sinica B, 2021 Src homology containing protein tyrosine phosphatase 2 (SHP2) represents a noteworthy target for various diseases, serving as a well-known oncogenic phosphatase in cancers.
Zhendong Song +6 more
doaj +1 more source
Data set of competitive and allosteric protein kinase inhibitors confirmed by X-ray crystallography
Data in Brief, 2021 A data set was generated comprising currently available competitive and allosteric human protein kinase inhibitors confirmed by X-ray crystallography. This data set has been used to systematically explore structural relationships between these types of ...
Huabin Hu +3 more
doaj +1 more source
Role of GSK-3β Inhibitors: New Promises and Opportunities for Alzheimer’s Disease [PDF]
Advanced Pharmaceutical Bulletin, 2023 Glycogen synthase kinase-3 (GSK-3) was discovered to be a multifunctional enzyme involved in a wide variety of biological processes, including early embryo formation, oncogenesis, as well cell death in neurodegenerative diseases.
Suggala Ramya Shri +3 more
doaj +1 more source
Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach.
PLoS ONE, 2019 Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are highly toxic and ...
Lilian Hernández Alvarez +3 more
doaj +1 more source
Inhibitors in AKTion: ATP-competitive vs allosteric [PDF]
Biochemical Society Transactions, 2020 Aberrant activation of the PI3K pathway is one of the commonest oncogenic events in human cancer. AKT is a key mediator of PI3K oncogenic function, and thus has been intensely pursued as a therapeutic target. Multiple AKT inhibitors, broadly classified as either ATP-competitive or allosteric, are currently in various stages of clinical development ...
Glorianne Lazaro +2 more
openaire +3 more sources
Inhibitors of BRAF dimers using an allosteric site [PDF]
Nature Communications, 2020 AbstractBRAF kinase, a critical effector of the ERK signaling pathway, is hyperactivated in many cancers. Oncogenic BRAFV600E signals as an active monomer in the absence of active RAS, however, in many tumors BRAF dimers mediate ERK signaling. FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which leads to tumor resistance.
Xiomaris M. Cotto-Rios +9 more
openaire +3 more sources
Plasmin Regulation through Allosteric, Sulfated, Small Molecules
Molecules, 2015 Plasmin, a key serine protease, plays a major role in clot lysis and extracellular matrix remodeling. Heparin, a natural polydisperse sulfated glycosaminoglycan, is known to allosterically modulate plasmin activity.
Rami A. Al-Horani +3 more
doaj +1 more source
Novel allosteric sites on Ras for lead generation. [PDF]
PLoS ONE, 2011 Aberrant Ras activity is a hallmark of diverse cancers and developmental diseases. Unfortunately, conventional efforts to develop effective small molecule Ras inhibitors have met with limited success.
Barry J Grant +6 more
doaj +1 more source
Molecules, 2022 Since its emergence in early 2019, the respiratory infectious virus, SARS-CoV-2, has ravaged the health of millions of people globally and has affected almost every sphere of life.
Shah Faisal +6 more
doaj +1 more source
InterAKTions with FKBPs - mutational and pharmacological exploration [PDF]
, 2013 The FK506-binding protein 51 (FKBP51) is an Hsp90-associated co-chaperone which regulates steroid receptors and kinases. In pancreatic cancer cell lines, FKBP51 was shown to recruit the phosphatase PHLPP to facilitate dephosphorylation of the kinase Akt,
Andreas März +23 more
core +2 more sources