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 …

New insights into genome folding by loop extrusion from inducible degron technologies

E de Wit, EP Nora - Nature Reviews Genetics, 2023 - nature.com
Chromatin folds into dynamic loops that often span hundreds of kilobases and physically
wire distant loci together for gene regulation. These loops are continuously created …

Development of BromoTag: a “Bump-and-Hole”–PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins

AG Bond, C Craigon, KH Chan, A Testa… - Journal of Medicinal …, 2021 - ACS Publications
Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …

Targeted protein degradation: clinical advances in the field of oncology

AKAA Salama, MV Trkulja, E Casanova… - International Journal of …, 2022 - mdpi.com
The field of targeted protein degradation (TPD) is a rapidly developing therapeutic modality
with the promise to tame disease-relevant proteins in ways that are difficult or impossible to …

Ligand-induced degrons for studying nuclear functions

MT Kanemaki - Current Opinion in Cell Biology, 2022 - Elsevier
Conditional control of protein expression facilitates studies of nuclear functions, which are
highly dynamic and tightly linked to the cell cycle in proliferating cells. However, conditional …

PROTACs targeting epigenetic proteins

C Zhang, Y He, X Sun, W Wei, Y Liu… - Acta Materia Medica, 2023 - scienceopen.com
The field of epigenetics pertains to alterations in gene function that are inherited without
changes in the DNA sequence, including histone modifications, post-translational …

Targeted dephosphorylation of SMAD3 as an approach to impede TGFβ signaling

A Brewer, JF Zhao, R Fasimoye, N Shpiro… - iScience, 2024 - cell.com
TGFβ (transforming growth factor-β) signaling is involved in a myriad of cellular processes
and its dysregulation has been implicated in many human diseases, including fibrosis and …

Synthesis of 3,4,5-Trisubstituted 1,2,4-Triazoles via I2-Catalyzed Cycloaddition of Amidines with Hydrazones

X Li, X Yuan, Y Wu, H Guo, Q Liu… - The Journal of Organic …, 2024 - ACS Publications
A general and practical method for the construction of various 3, 4, 5-trisubstituted 1, 2, 4-
triazoles via I2-catalyzed cycloaddition of N-functionalized amidines with hydrazones is …

[HTML][HTML] Development of an AchillesTAG degradation system and its application to control CAR-T activity

GK Veits, CS Henderson, A Vogelaar, SJ Eron… - Current Research in …, 2021 - Elsevier
In addition to the therapeutic applicability of targeted protein degradation (TPD), the modality
also harbors unique properties that enable the development of innovative chemical biology …

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

X Zhao, Y Chen, H Su, L Zhang - Interdisciplinary Medicine, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD)
technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells. A …