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 …

WD40 repeat domain proteins: a novel target class?

M Schapira, M Tyers, M Torrent… - Nature reviews Drug …, 2017 - nature.com
Antagonism of protein–protein interactions (PPIs) with small molecules is becoming more
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …

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 …

Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1

Y Tao, D Remillard, EV Vinogradova… - Journal of the …, 2022 - ACS Publications
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex

DE Bussiere, L **e, H Srinivas, W Shu, A Burke… - Nature Chemical …, 2020 - nature.com
The anticancer agent indisulam inhibits cell proliferation by causing degradation of RBM39,
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …

Discovery of nanomolar DCAF1 small molecule ligands

ASM Li, S Kimani, B Wilson, M Noureldin… - Journal of Medicinal …, 2023 - ACS Publications
DCAF1 is a substrate receptor of two distinct E3 ligases (CRL4DCAF1 and EDVP), plays a
critical physiological role in protein degradation, and is considered a drug target for various …

High-definition analysis of host protein stability during human cytomegalovirus infection reveals antiviral factors and viral evasion mechanisms

K Nightingale, KM Lin, BJ Ravenhill, C Davies… - Cell host & …, 2018 - cell.com
Human cytomegalovirus (HCMV) is an important pathogen with multiple immune evasion
strategies, including virally facilitated degradation of host antiviral restriction factors. Here …

Promiscuous targeting of cellular proteins by Vpr drives systems-level proteomic remodeling in HIV-1 infection

EJD Greenwood, JC Williamson, A Sienkiewicz… - Cell reports, 2019 - cell.com
HIV-1 encodes four" accessory proteins"(Vif, Vpr, Vpu, and Nef), dispensable for viral
replication in vitro but essential for viral pathogenesis in vivo. Well characterized cellular …

Vpr targets TET2 for degradation by CRL4VprBP E3 ligase to sustain IL-6 expression and enhance HIV-1 replication

L Lv, Q Wang, Y Xu, LC Tsao, T Nakagawa, H Guo… - Molecular cell, 2018 - cell.com
HIV-1 expresses several accessory proteins to counteract host anti-viral restriction factors to
facilitate viral replication and disease progression. One such protein, Vpr, has been …

Structure of the DDB1-AMBRA1 E3 ligase receptor complex linked to cell cycle regulation

M Liu, Y Wang, F Teng, X Mai, X Wang, MY Su… - Nature …, 2023 - nature.com
AMBRA1 is a tumor suppressor protein that functions as a substrate receptor of the ubiquitin
conjugation system with roles in autophagy and the cell cycle regulatory network. The …