Work

Drugging Challenging Cancer Targets Using Fragment-Based Methods

Year: 2025

Type: review

Abstract: There are many highly validated cancer targets that are difficult or impossible to drug due to the absence of suitable pockets that can bind small molecules. Fragment-based methods have been shown to be a useful approach for identifying ligands to proteins that were previously thought to be undruggable. In this review, I will give an overview of fragment-based ligand discovery and provide examples from our own work on how fragment-based methods were used to discover high affinity ligands for challenging cancer drug targets.

Source: Chemical Reviews

DOI: 10.1021/acs.chemrev.4c00892

Author: Stephen W. Fesik

Institution: Vanderbilt University

Language: English

Topic: Computational Drug Discovery Methods

Subfield: Computational Theory and Mathematics

Field: Computer Science

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500