The hallmarks of cancer metabolism: Still emerging

NN Pavlova, J Zhu, CB Thompson - Cell metabolism, 2022 - cell.com
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 …

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 …

The E3 ligase adapter cereblon targets the C-terminal cyclic imide degron

S Ichikawa, HA Flaxman, W Xu, N Vallavoju, HC Lloyd… - Nature, 2022 - nature.com
The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and
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 …

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 …

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 …

Lessons in PROTAC design from selective degradation with a promiscuous warhead

DP Bondeson, BE Smith, GM Burslem… - Cell chemical …, 2018 - cell.com
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 …

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 …

Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome

KA Donovan, J An, RP Nowak, JC Yuan, EC Fink… - elife, 2018 - elifesciences.org
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 …

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 …