Advancing Strategies for Proteolysis-Targeting Chimera Design.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01555
Abstract: Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by degrading various disease-causing proteins, particularly those related to tumors. Therefore, the introduction of PROTACs has ushered in a new chapter of antitumor drug development, marked by… read more here.
Keywords: targeting chimera; design; strategies proteolysis; proteolysis ... See more keywords
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.8b10320
Abstract: The receptor tyrosine kinase FLT-3 is frequently mutated in acute myeloid leukemia; however, current small molecule inhibitors suffer from limited efficacy in the clinic. Conversion of a FLT-3 inhibitor (quizartinib) into a proteolysis targeting chimera… read more here.
Keywords: targeting chimera; flt; flt itd; proteolysis targeting ... See more keywords
Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC).
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc00272h
Abstract: We developed a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8). The PROTAC induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the… read more here.
Keywords: targeting chimera; degradation; protac; proteolysis targeting ... See more keywords
Targeting autophagy in disease: established and new strategies.
Sign Up to like & getrecommendations! Published in 2021 at "Autophagy"
DOI: 10.1080/15548627.2021.1936359
Abstract: Macroautophagy/autophagy is an evolutionarily conserved pathway responsible for clearing cytosolic aggregated proteins, damaged organelles or invading microorganisms. Dysfunctional autophagy leads to pathological accumulation of the cargo, which has been linked to a range of human… read more here.
Keywords: targeting chimera; new strategies; kinase; disease ... See more keywords
Crizotinib‐based proteolysis targeting chimera suppresses gastric cancer by promoting MET degradation
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Science"
DOI: 10.1111/cas.15733
Abstract: As one of the common malignant cancer types, gastric cancer (GC) is known for late‐stage diagnosis and poor prognosis. Overexpression of the receptor tyrosine kinase MET is associated with poor prognosis among patients with advanced… read more here.
Keywords: proteolysis targeting; targeting chimera; cancer; gastric cancer ... See more keywords