scispace - formally typeset
Open AccessJournal ArticleDOI

Drugging the 'undruggable' cancer targets

TLDR
Four scientists working in the 'undruggable' cancer research field are asked for their opinions on the most crucial advances, as well as the challenges and what the future holds for this important area of research.
Abstract
The term 'undruggable' was coined to describe proteins that could not be targeted pharmacologically. However, progress is being made to 'drug' many of these targets, and therefore more appropriate terms might be 'difficult to drug' or 'yet to be drugged'. Many desirable targets in cancer fall into this category, including the RAS and MYC oncogenes, and pharmacologically targeting these intractable proteins is now a key challenge in cancer research that requires innovation and the development of new technologies. In this Viewpoint article, we asked four scientists working in this field for their opinions on the most crucial advances, as well as the challenges and what the future holds for this important area of research.

read more

Content maybe subject to copyright    Report

Citations
More filters
Journal ArticleDOI

Therapeutic target database 2020: enriched resource for facilitating research and early development of targeted therapeutics

TL;DR: The Therapeutic Target Database (TTD) is constructed with expanded information about target-regulating microRNAs and transcription factors, target-interacting proteins, and patented agents and their targets, which can be conveniently retrieved and is further enriched with regulatory mechanisms or biochemical classes.
Journal ArticleDOI

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

TL;DR: SD-36 achieves complete and long-lasting tumor regression in multiple xenograft mouse models at well-tolerated dose schedules and is a promising cancer therapeutic strategy.
Journal ArticleDOI

The role of ubiquitination in tumorigenesis and targeted drug discovery

TL;DR: The latest progress in understanding the substrates for ubiquitination and their special functions in tumor metabolism regulation, TME modulation and CSC stemness maintenance are summarized and potential therapeutic targets for cancer are reviewed.
Journal ArticleDOI

Selective degradation of splicing factor CAPERα by anticancer sulfonamides

TL;DR: These sulfonamides represent selective chemical probes for disrupting CAPERα function and designate DCAFs as promising drug targets for promoting selective protein degradation in cancer therapy.
References
More filters
Journal ArticleDOI

Cancer Genome Landscapes

TL;DR: This work has revealed the genomic landscapes of common forms of human cancer, which consists of a small number of “mountains” (genes altered in a high percentage of tumors) and a much larger number of "hills" (Genes altered infrequently).
Journal ArticleDOI

The future of immune checkpoint therapy

TL;DR: The way forward for this class of novel agents lies in the ability to understand human immune responses in the tumor microenvironment, which will provide valuable information regarding the dynamic nature of the immune response and regulation of additional pathways that will need to be targeted through combination therapies to provide survival benefit for greater numbers of patients.
Journal ArticleDOI

Selective inhibition of BET bromodomains.

TL;DR: A cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains is reported, establishing proof-of-concept for targeting protein–protein interactions of epigenetic ‘readers’, and providing a versatile chemical scaffold for the development of chemical probes more broadly throughout the b romodomain family.
Journal ArticleDOI

MYC on the Path to Cancer

TL;DR: The richness of the understanding of MYC is reviewed, highlighting new biological insights and opportunities for cancer therapies.
Related Papers (5)