Mark E. Fitzgerald
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View article: BiDAC-dependent degradation of plasma membrane proteins by the endolysosomal system
BiDAC-dependent degradation of plasma membrane proteins by the endolysosomal system Open
The discovery of bifunctional degradation activating compounds (BiDACs) has led to the development of a new class of drugs that promote the clearance of their protein targets. BiDAC-induced ubiquitination is generally believed to direct cy…
View article: Discovery of an orally bioavailable, CNS active pan-mutant RET kinase heterobifunctional degrader
Discovery of an orally bioavailable, CNS active pan-mutant RET kinase heterobifunctional degrader Open
Herein we highlight the discovery of a pan-mutant, orally bioavailable RET degrader with activity against intracranial tumors.
View article: Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex
Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex Open
View article: Morphological and genetic screens reveal mechanisms of BiDAC-induced plasma membrane protein degradation
Morphological and genetic screens reveal mechanisms of BiDAC-induced plasma membrane protein degradation Open
The discovery of bifunctional degradation activating compounds (BiDACs) has led to the development of a new class of drugs that promote the clearance of their protein targets. BiDAC-induced ubiquitination is generally believed to direct cy…
View article: A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition
A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition Open
View article: Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models
Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models Open
Targeted, catalytic degradation of oncoproteins using heterobifunctional small molecules is an attractive modality, particularly for hematologic malignancies, which are often initiated by aberrant transcription factors and are challenging …
View article: A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination
A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination Open
Recent advances in targeted protein degradation have enabled chemical hijacking of the ubiquitin-proteasome system to treat disease. The catalytic rate of cereblon (CRBN)-dependent bifunctional degradation activating compounds (BiDAC), whi…
View article: Identification of Highly Specific Diversity-Oriented Synthesis-Derived Inhibitors of <i>Clostridium difficile</i>
Identification of Highly Specific Diversity-Oriented Synthesis-Derived Inhibitors of <i>Clostridium difficile</i> Open
In 2013, the Centers for Disease Control highlighted Clostridium difficile as an urgent threat for antibiotic-resistant infections, in part due to the emergence of highly virulent fluoroquinolone-resistant strains. Limited therapeutic opti…
View article: Back Cover: Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET‐BRET (ChemMedChem 23/2016)
Back Cover: Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET‐BRET (ChemMedChem 23/2016) Open
The back cover picture shows a schematic of a bioluminescent energy transfer (BRET) system that reports on in-cell target engagement of small molecules to the bromodomain and extra-terminal domain (BET) family of chromatin-regulating prote…