[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
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 …
tackle disease-causing proteins that have historically been highly challenging to target with …
[HTML][HTML] PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
[HTML][HTML] Payload diversification: a key step in the development of antibody–drug conjugates
L Conilh, L Sadilkova, W Viricel, C Dumontet - Journal of Hematology & …, 2023 - Springer
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that
currently combines the selectivity of monoclonal antibodies with the potency of a payload …
currently combines the selectivity of monoclonal antibodies with the potency of a payload …
[HTML][HTML] Site-selective modification strategies in antibody–drug conjugates
SJ Walsh, JD Bargh, FM Dannheim… - Chemical Society …, 2021 - pubs.rsc.org
Antibody–drug conjugates (ADCs) harness the highly specific targeting capabilities of an
antibody to deliver a cytotoxic payload to specific cell types. They have garnered …
antibody to deliver a cytotoxic payload to specific cell types. They have garnered …
[HTML][HTML] Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
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 …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
Exploring the next generation of antibody–drug conjugates
Antibody–drug conjugates (ADCs) are a promising cancer treatment modality that enables
the selective delivery of highly cytotoxic payloads to tumours. However, realizing the full …
the selective delivery of highly cytotoxic payloads to tumours. However, realizing the full …
The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics
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 …
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …
[HTML][HTML] Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy
J Gao, B Hou, Q Zhu, L Yang, X Jiang, Z Zou… - Nature …, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) has been exploited to degrade
putative protein targets. However, the antitumor performance of PROTACs is impaired by …
putative protein targets. However, the antitumor performance of PROTACs is impaired by …
[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …