E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
Phase I First-in-Human Dose Escalation Study of the oral SF3B1 modulator H3B-8800 in myeloid neoplasms
DP Steensma, M Wermke, VM Klimek, PL Greenberg… - Leukemia, 2021 - nature.com
We conducted a phase I clinical trial of H3B-8800, an oral small molecule that binds Splicing
Factor 3B1 (SF3B1), in patients with MDS, CMML, or AML. Among 84 enrolled patients (42 …
Factor 3B1 (SF3B1), in patients with MDS, CMML, or AML. Among 84 enrolled patients (42 …
Small-molecule-induced polymerization triggers degradation of BCL6
Effective and sustained inhibition of non-enzymatic oncogenic driver proteins is a major
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
pharmacological challenge. The clinical success of thalidomide analogues demonstrates …
Antibody–PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4
M Maneiro, N Forte, MM Shchepinova… - ACS chemical …, 2020 - ACS Publications
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
AD Cowan, A Ciulli - Annual Review of Biochemistry, 2022 - annualreviews.org
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 …
Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
Controlled perturbation of protein activity is essential to study protein function in cells and
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
[PDF][PDF] Haven't got a glue: protein surface variation for the design of molecular glue degraders
Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation
L Lv, P Chen, L Cao, Y Li, Z Zeng, Y Cui, Q Wu, J Li… - Elife, 2020 - elifesciences.org
Molecular-glue degraders mediate interactions between target proteins and components of
the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a …
the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a …
Strategies for designing proteolysis targeting chimaeras (PROTACs)
S He, G Dong, J Cheng, Y Wu… - Medicinal Research …, 2022 - Wiley Online Library
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique
for new drug discovery and development. Currently, the largest challenge in the molecular …
for new drug discovery and development. Currently, the largest challenge in the molecular …
Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective
LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …
degradation in a highly selective and effective manner, has created tremendous excitement …