Related Experiment Video
Updated: Aug 10, 2026

Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
A critical appraisal of structure-based drug design
Marina Tintelnot-Blomley1, Richard A Lewis
1Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland. marina.tintelnot-blomley@novartis.com
Abstract:
Even though conceptually started in the early 1980s, the use of protein structure information in drug discovery has never reached the current level of significance, nor has it experienced the revolutionary development that it is currently undergoing. Initially used for lead optimization, structure-based drug design (SBDD) now covers and supports virtually all steps in the drug- discovery pipeline. This commentary is a critical appraisal of the current state of the art, examining both successes and failures. Future directions in SBDD are also discussed.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Drug Discovery: Overview
Biopharmaceutical Factors Influencing Drug Product Design: Overview
Prodrugs
Prodrugs help overcome...
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
