The hallmarks of cancer metabolism: Still emerging
Metabolism of cancer cells is geared toward biomass production and proliferation. Since the
metabolic resources within the local tissue are finite, this can lead to nutrient depletion and …
metabolic resources within the local tissue are finite, this can lead to nutrient depletion and …
PROTACs: an emerging therapeutic modality in precision medicine
DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
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 …
The E3 ligase adapter cereblon targets the C-terminal cyclic imide degron
The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and
lenalidomide, therapeutic agents used in the treatment of haematopoietic malignancies …
lenalidomide, therapeutic agents used in the treatment of haematopoietic malignancies …
Development of targeted protein degradation therapeutics
PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
Targeted protein degradation as a therapeutic modality has seen dramatic progress and
massive investment in recent years because of the convergence of two key scientific …
massive investment in recent years because of the convergence of two key scientific …
Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders
J Yamamoto, T Ito, Y Yamaguchi… - Chemical Society Reviews, 2022 - pubs.rsc.org
Progress in strategies aimed at breaking down therapeutic target proteins has led to a
paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein …
paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein …
Cullin-RING ubiquitin ligase regulatory circuits: a quarter century beyond the F-box hypothesis
JW Harper, BA Schulman - Annual review of biochemistry, 2021 - annualreviews.org
Cullin-RING ubiquitin ligases (CRLs) are dynamic modular platforms that regulate myriad
biological processes through target-specific ubiquitylation. Our knowledge of this system …
biological processes through target-specific ubiquitylation. Our knowledge of this system …
Lessons in PROTAC design from selective degradation with a promiscuous warhead
Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
Ubiquitylation at the crossroads of development and disease
M Rape - Nature reviews Molecular cell biology, 2018 - nature.com
Human development requires intricate cell specification and communication pathways that
allow an embryo to generate and appropriately connect more than 200 different cell types …
allow an embryo to generate and appropriately connect more than 200 different cell types …
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome
In historical attempts to treat morning sickness, use of the drug thalidomide led to the birth of
thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and …
thousands of children with severe birth defects. Despite their teratogenicity, thalidomide and …
Cancer cell metabolism: the essential role of the nonessential amino acid, glutamine
J Zhang, NN Pavlova, CB Thompson - The EMBO journal, 2017 - embopress.org
Biochemistry textbooks and cell culture experiments seem to be telling us two different
things about the significance of external glutamine supply for mammalian cell growth and …
things about the significance of external glutamine supply for mammalian cell growth and …