[HTML][HTML] 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 …

Nrf2/Keap1/ARE signaling: Towards specific regulation

AV Ulasov, AA Rosenkranz, GP Georgiev, AS Sobolev - Life sciences, 2022 - Elsevier
The Nrf2 transcription factor governs the expression of hundreds genes involved in cell
defense against oxidative stress, the hallmark of numerous diseases such as …

Target and tissue selectivity of PROTAC degraders

RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …

The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Chasing molecular glue degraders: screening approaches

A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …

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 …

Expanding chemical probe space: quality criteria for covalent and degrader probes

IV Hartung, J Rudolph, MM Mader… - Journal of Medicinal …, 2023 - ACS Publications
Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

Target protein deglycosylation in living cells by a nanobody-fused split O-GlcNAcase

Y Ge, DH Ramirez, B Yang, AK D'Souza… - Nature chemical …, 2021 - nature.com
Abstract O-linked N-acetylglucosamine (O-GlcNAc) is an essential and dynamic post-
translational modification that is presented on thousands of nucleocytoplasmic proteins …

[HTML][HTML] Predicting the structural basis of targeted protein degradation by integrating molecular dynamics simulations with structural mass spectrometry

T Dixon, D MacPherson, B Mostofian… - Nature …, 2022 - nature.com
Targeted protein degradation (TPD) is a promising approach in drug discovery for degrading
proteins implicated in diseases. A key step in this process is the formation of a ternary …

[HTML][HTML] Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

WH Guo, X Qi, X Yu, Y Liu, CI Chung, F Bai… - Nature …, 2020 - nature.com
Current efforts in the proteolysis targeting chimera (PROTAC) field mostly focus on choosing
an appropriate E3 ligase for the target protein, improving the binding affinities towards the …