Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

MYC protein interactors in gene transcription and cancer

C Lourenco, D Resetca, C Redel, P Lin… - Nature Reviews …, 2021 - nature.com
The transcription factor and oncoprotein MYC is a potent driver of many human cancers and
can regulate numerous biological activities that contribute to tumorigenesis. How a single …

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
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 …

Direct mapping of ligandable tyrosines and lysines in cells with chiral sulfonyl fluoride probes

Y Chen, GB Craven, RA Kamber, A Cuesta… - Nature Chemistry, 2023 - nature.com
Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …

MYC: a complex problem

SK Das, BA Lewis, D Levens - Trends in cell biology, 2023 - cell.com
The MYC protooncogene functions as a universal amplifier of transcription through
interaction with numerous factors and complexes that regulate almost every cellular process …

Target gene-independent functions of MYC oncoproteins

A Baluapuri, E Wolf, M Eilers - Nature Reviews Molecular Cell Biology, 2020 - nature.com
Oncoproteins of the MYC family are major drivers of human tumorigenesis. Since a large
body of evidence indicates that MYC proteins are transcription factors, studying their function …

MYC, metabolism, and cancer

ZE Stine, ZE Walton, BJ Altman, AL Hsieh, CV Dang - Cancer discovery, 2015 - AACR
The MYC oncogene encodes a transcription factor, MYC, whose broad effects make its
precise oncogenic role enigmatically elusive. The evidence to date suggests that MYC …

A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models

X Yu, D Li, J Kottur, Y Shen, HS Kim, KS Park… - Science translational …, 2021 - science.org
Interactions between WD40 repeat domain protein 5 (WDR5) and its various partners such
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …

Chromatin replication and epigenetic cell memory

KR Stewart-Morgan, N Petryk, A Groth - Nature cell biology, 2020 - nature.com
Propagation of the chromatin landscape across cell divisions is central to epigenetic cell
memory. Mechanistic analysis of the interplay between DNA replication, the cell cycle, and …

Imidazoles as potential anticancer agents: An update on recent studies

P Sharma, C LaRosa, J Antwi, R Govindarajan… - Molecules, 2021 - mdpi.com
Nitrogen-containing heterocyclic rings are common structural components of marketed
drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide …