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Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
PROTACs: an emerging therapeutic modality in precision medicine
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …
[HTML][HTML] A potent and selective small-molecule degrader of STAT3 achieves complete tumor regression in vivo
Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic
target. Here we report the discovery of SD-36, a small-molecule degrader of STAT3. SD-36 …
target. Here we report the discovery of SD-36, a small-molecule degrader of STAT3. SD-36 …
Bromodomains: a new target class for drug development
AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
Map** the degradable kinome provides a resource for expedited degrader development
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …
dependent degradation of proteins. TPD is of interest in drug development, as it can address …
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer
We report herein the discovery of highly potent PROTAC degraders of androgen receptor
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …
Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16
Ligand-dependent protein degradation has emerged as a compelling strategy to
pharmacologically control the protein content of cells. So far, however, only a limited number …
pharmacologically control the protein content of cells. So far, however, only a limited number …
Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Abstract PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …