Results 41 to 50 of about 383,210 (284)
Advance in Reversible Covalent Kinase Inhibitors [PDF]
arXiv, 2021 Reversible covalent kinase inhibitors (RCKIs) are a class of novel kinase inhibitors attracting increasing attention because they simultaneously show the selectivity of covalent kinase inhibitors, yet avoid permanent protein-modification-induced adverse effects.
arxiv
British Journal of Pharmacology, 2014 The cyclin‐dependent kinase CDK9 is an important therapeutic target but currently available inhibitors exhibit low specificity and/or narrow therapeutic windows.
T. Albert +7 more
semanticscholar +1 more source
Using the structural kinome to systematize kinase drug discovery [PDF]
arXiv, 2021 Kinase-targeted drug design is challenging. It requires designing inhibitors that can bind to specific kinases when all kinase catalytic domains share a common folding scaffold that binds ATP. Thus, obtaining the desired selectivity, given the whole human kinome, is a fundamental task during early-stage drug discovery.
arxiv
A knowledge graph representation learning approach to predict novel kinase-substrate interactions [PDF]
arXiv, 2022 The human proteome contains a vast network of interacting kinases and substrates. Even though some kinases have proven to be immensely useful as therapeutic targets, a majority are still understudied. In this work, we present a novel knowledge graph representation learning approach to predict novel interaction partners for understudied kinases.
arxiv
Cyclin-dependent kinase inhibitors: efficacy and safety
Медицинский совет, 2019 Breast Cancer is the most common type of cancer worldwide. Scientific advances and new ways of treating have significantly improved the prognosis of breast cancer in recent decades.
I. B. Kononenko +2 more
doaj +1 more source
Design New Compound of Meisoindigo Derivative as Anti Breast Cancer Based on QSAR Approach
Jurnal Kimia Sains dan Aplikasi, 2020 Design new compounds of Meisoindigo using the QSAR approach with semiempirical methods have been successfully made with better biological activity as anti-breast cancer results.
Agus Dwi Ananto +2 more
doaj +1 more source
Restriction Checkpoint Controls Bradyzoite Development in Toxoplasma gondii
Microbiology Spectrum, 2022 Human toxoplasmosis is a life-threatening disease caused by the apicomplexan parasite Toxoplasma gondii. Rapid replication of the tachyzoite is associated with symptomatic disease, while suppressed division of the bradyzoite is responsible for chronic ...
Anatoli V. Naumov +9 more
doaj +1 more source
Genes & Development, 1993 The product (pRb) of the retinoblastoma gene (RB-1) prevents S-phase entry during the cell cycle, and inactivation of this growth-suppressive function is presumed to result from pRb hyperphosphorylation during late G1 phase.
J. Kato +4 more
semanticscholar +1 more source
Deciphering the modes of human separase inhibition by securin and CDK1-CCNB1
Molecular & Cellular Oncology, 2021 Accurate chromosome segregation depends on tight regulation of the protease separase, which cleaves the ring-shaped cohesin complex that entraps the two sister chromatids.
Pierre Raia, Jun Yu, Andreas Boland
doaj +1 more source
Targeting Protein-Protein Interactions to Inhibit Cyclin-Dependent Kinases
Pharmaceuticals, 2023 Cyclin-dependent kinases (CDKs) play diverse and critical roles in normal cells and may be exploited as targets in cancer therapeutic strategies. CDK4 inhibitors are currently approved for treatment in advanced breast cancer.
Mark Klein
doaj +1 more source