7 research outputs found
Conformationally Constrained Peptides from CD2 To Modulate Protein–Protein Interactions between CD2 and CD58
Integrated Teaching of Structure-Based Drug Design and Biopharmaceutics: A Computer-Based Approach
Structure-activity studies of peptides from the "hot-spot" region of human CD2 protein: Development of peptides for immunomodulation
10.1021/jm0503547Journal of Medicinal Chemistry48206236-6249JMCM
Inhibition of protein–protein interaction of HER2–EGFR and HER2–HER3 by a rationally designed peptidomimetic
An Empirical Study of Neural Network-Based Audience Response Technology in a Human Anatomy Course for Pharmacy Students
Expanding the medicinal chemistry synthetic toolbox
The key objectives of medicinal chemistry are to efficiently design and synthesize bioactive compounds that have the potential to become safe and efficacious drugs. Most medicinal chemistry programmes rely on screening compound collections populated by a range of molecules derived from a set of known and robust chemistry reactions. Analysis of the role of synthetic organic chemistry in subsequent hit and lead optimization efforts suggests that only a few reactions dominate. Thus, the uptake of new synthetic methodologies in drug discovery is limited. Starting from the known limitations of reaction parameters, synthesis design tools, synthetic strategies and innovative chemistries, here we highlight opportunities for the expansion of the medicinal chemists’ synthetic toolbox. More intense crosstalk between synthetic and medicinal chemists in industry and academia should enable enhanced impact of new methodologies in future drug discovery. © 2018 Springer Nature Limited. All rights reserved