Advances and Novel Methodologies for the Development of Small-Molecule Drugs

Introduction

Over the past decade, small-molecule drugs have remained the dominant force among approved therapeutics. Recent advances in artificial intelligence and structural biology now enable researchers to discover novel targets for small molecule inhibitors with greater precision and to pursue rational drug design, markedly accelerating the development of new small molecule drugs. Looking ahead, small-molecule drugs are poised to be deployed across an even broader spectrum of diseases. This Special Issue aims to spotlight recent advancements and new methods for the development of small-molecule drugs. This collection will feature articles that explore a diverse array of topics related to targeted small molecule compounds, including new chemotypes, degraders, covalent inhibitors, dual inhibitors, allosteric inhibitors, protein-protein interaction inhibitors, and novel methodologies. The special issue will captivate researchers in medicinal chemistry and biochemistry, as well as those involved in new drug development and crop protection.

Keywords

Targeted drugs, Degraders, Covalent inhibitors, Dual inhibitors, Allosteric inhibitors, PPI_ inhibitors, Heterocyclic skeletons

Sub-topics

• Advances in small-molecule compounds targeting enzymatic activity
• Advances in protein degraders
• Advances in covalent inhibitors
• Advances in dual-targeting inhibitors
• Advances in allosteric modulators
• Advances in inhibitors targeting protein-protein interactions
• Advances in the application of heterocyclic scaffolds within medicinal chemistry
• Novel methodologies for the discovery and development of targeted small-molecule compounds