Results 191 to 200 of about 823,777 (226)

Design, Synthesis, Biological Studies and Putative Binding Mode of Novel Benzotriazolothalidomide Derivatives as Cereblon Ligands. [PDF]

open access: yesChem Biol Drug Des
Ganguly P   +12 more
europepmc   +1 more source

Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies

Cancer Letters, 2022
PROteolysis TArgeting Chimeras (PROTACs) degrade target proteins via the ubiquitin-proteasome system, providing novel insights into drug development for hematologic malignancies. PROTACs outperform conventional therapeutics and currently available small molecule inhibitors in terms of efficacy, tissue-and cell-selectivity, and side effect profile. Most
Yangping Wu   +3 more
openaire   +2 more sources

In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)

Bioorganic & Medicinal Chemistry, 2021
Chemical knockdown of therapeutic targets using proteolysis targeting chimeras (PROTACs) is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that generally show poor bioavailability due to their relatively high molecular weight.
Shusuke Tomoshige, Minoru Ishikawa
openaire   +2 more sources

Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC)

Bioorganic Chemistry, 2022
Clinical FLT3 mutations caused poor therapeutic benefits toward the present FLT3 inhibitors, and degradation of the FLT3 mutant protein may be a promising alternative approach to protect against acute myeloid leukemia (AML). Herein, we report the discovery of small molecule FLT3 degraders based on the proteolysis targeting chimera (PROTAC).
Yong, Chen   +7 more
openaire   +2 more sources

PROTAC (PROteolysis TArgeting Chimera)

La Chimica e l'Industria, 2022
PROTAC technology represents the spearhead of Targeted Protein Degradation, a new paradigm that in the past recent years has become increasingly used in pharmacology. Characterized by a profoundly different mechanism of action compared to classic approaches, it can be useful in tackling elusive molecular targets and hopefully help dealing with ...
openaire   +1 more source

Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC) [PDF]

open access: yesEuropean Journal of Medicinal Chemistry, 2020
Histone deacetylases (HDACs) play important roles in inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD). Unravelling of and interfering with the functions of specific isoenzymes contributing to inflammation provides ...
Frank J Dekker, Deng Chen, Fangyuan Cao
exaly   +3 more sources

Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)

European Journal of Medicinal Chemistry, 2020
PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules that trigger the poly-ubiquitination of the protein of interest (POI) inducing its degradation via the recruitment of the ubiquitin-proteasome system, thus suppressing the POI's intracellular levels and indirectly all its functions.
Tomaselli D.   +3 more
openaire   +3 more sources

Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery

Bioorganic Chemistry, 2022
Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation.
Jia-Yue, Xi   +7 more
openaire   +2 more sources

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