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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation 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 …

Rational discovery of molecular glue degraders via scalable chemical profiling

C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …

Molecular glues: the adhesive connecting targeted protein degradation to the clinic

JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

Arginine reprograms metabolism in liver cancer via RBM39

D Mossmann, C Müller, S Park, B Ryback, M Colombi… - Cell, 2023 - cell.com
Metabolic reprogramming is a hallmark of cancer. However, mechanisms underlying
metabolic reprogramming and how altered metabolism in turn enhances tumorigenicity are …

Defining molecular glues with a dual-nanobody cannabidiol sensor

S Cao, S Kang, H Mao, J Yao, L Gu, N Zheng - Nature communications, 2022 - nature.com
Abstract “Molecular glue”(MG) is a term coined to describe the mechanism of action of the
plant hormone auxin and subsequently used to characterize synthetic small molecule …

Haven't got a glue: protein surface variation for the design of molecular glue degraders

Z Kozicka, NH Thomä - Cell Chemical Biology, 2021 - cell.com
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 …

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

T Wu, H Yoon, Y Xiong, SE Dixon-Clarke… - Nature Structural & …, 2020 - nature.com
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 …