[HTML][HTML] Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

B Nabet, FM Ferguson, BKA Seong, M Kuljanin… - Nature …, 2020 - nature.com
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …

The dTAG system for immediate and target-specific protein degradation

B Nabet, JM Roberts, DL Buckley, J Paulk… - Nature chemical …, 2018 - nature.com
Dissection of complex biological systems requires target-specific control of the function or
abundance of proteins. Genetic perturbations are limited by off-target effects …

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 …

[HTML][HTML] Targeted degradation via direct 26S proteasome recruitment

C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …

[HTML][HTML] Targeted protein degradation via intramolecular bivalent glues

O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …

Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins

TK Neklesa, HS Tae, AR Schneekloth… - Nature chemical …, 2011 - nature.com
The ability to regulate any protein of interest in living systems with small molecules remains
a challenge. We hypothesized that appending a hydrophobic moiety to the surface of a …

[HTML][HTML] A method for the acute and rapid degradation of endogenous proteins

D Clift, WA McEwan, LI Labzin, V Konieczny… - Cell, 2017 - cell.com
Methods for the targeted disruption of protein function have revolutionized science and
greatly expedited the systematic characterization of genes. Two main approaches are …

HaloPROTACS: use of small molecule PROTACs to induce degradation of HaloTag fusion proteins

DL Buckley, K Raina, N Darricarrere, J Hines… - ACS chemical …, 2015 - ACS Publications
Small molecule-induced protein degradation is an attractive strategy for the development of
chemical probes. One method for inducing targeted protein degradation involves the use of …

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 …

Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently

Z Yang, Y Sun, Z Ni, C Yang, Y Tong, Y Liu, H Li… - Cell Research, 2021 - nature.com
Dear Editor, Targeted protein degradation (TPD) represents a promising research field that
has quickly attracted attention and efforts from both academia and pharmaceutical industry …