Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

Control of protein stability by post-translational modifications

JM Lee, HM Hammarén, MM Savitski… - Nature …, 2023 - nature.com
Post-translational modifications (PTMs) can occur on specific amino acids localized within
regulatory domains of target proteins, which control a protein's stability. These regions …

Exploring treatment options in cancer: tumor treatment strategies

B Liu, H Zhou, L Tan, KTH Siu, XY Guan - Signal transduction and …, 2024 - nature.com
Traditional therapeutic approaches such as chemotherapy and radiation therapy have
burdened cancer patients with onerous physical and psychological challenges …

PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature reviews Drug discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

The emerging role of mass spectrometry-based proteomics in drug discovery

F Meissner, J Geddes-McAlister, M Mann… - Nature Reviews Drug …, 2022 - nature.com
Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

Antibody targeting of E3 ubiquitin ligases for receptor degradation

H Marei, WTK Tsai, YS Kee, K Ruiz, J He, C Cox, T Sun… - Nature, 2022 - nature.com
Most current therapies that target plasma membrane receptors function by antagonizing
ligand binding or enzymatic activities. However, typical mammalian proteins comprise …

The MYC oncogene — the grand orchestrator of cancer growth and immune evasion

R Dhanasekaran, A Deutzmann… - Nature reviews Clinical …, 2022 - nature.com
The MYC proto-oncogenes encode a family of transcription factors that are among the most
commonly activated oncoproteins in human neoplasias. Indeed, MYC aberrations or …

Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …