Circular dichroism in drug discovery and development: an abridged review

Analytical and Bioanalytical Chemistry
C BertucciAngela De Simone

Abstract

Chirality plays a fundamental role in determining the pharmacodynamic and pharmacokinetic properties of drugs, and contributes significantly to our understanding of the mechanisms that lie behind biorecognition phenomena. Circular dichroism spectroscopy is the technique of choice for determining the stereochemistry of chiral drugs and proteins, and for monitoring and characterizing molecular recognition phenomena in solution. The role of chirality in our understanding of recognition phenomena at the molecular level is discussed here via several selected systems of interest in the drug discovery and development area. The examples were selected in order to underline the utility of circular dichroism in emerging studies of protein-protein interactions in biological context. In particular, the following aspects are discussed here: the relationship between stereochemistry and pharmacological activity--stereochemical characterization of new leads and drugs; stereoselective binding of leads and drugs to target proteins--the binding of drugs to serum albumins; conformational transitions of peptides and proteins of physiological relevance, and the stereochemical characterization of therapeutic peptides.

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Citations

Mar 27, 2013·Analytical and Bioanalytical Chemistry·Anthony Veloso, Kagan Kerman
Apr 1, 2014·Journal of Pharmaceutical and Biomedical Analysis·Cecilia FortugnoCarlo Bertucci
Aug 29, 2012·Analytical and Bioanalytical Chemistry·Angela De SimoneVincenza Andrisano
Apr 16, 2013·Journal of Pharmaceutical and Biomedical Analysis·Milan NobilisMilan Pour
Jan 11, 2012·Molecular Aspects of Medicine·Gabriella FanaliPaolo Ascenzi
Feb 22, 2011·Journal of Pharmaceutical and Biomedical Analysis·Aline StaubSerge Rudaz
Jan 22, 2013·Biotechnology and Bioengineering·Spyridon KonstantinidisNigel Titchener-Hooker
Mar 15, 2015·Journal of Pharmaceutical and Biomedical Analysis·Daniele Tedesco, Carlo Bertucci
Mar 17, 2015·Journal of Pharmaceutical and Biomedical Analysis·Cecilia FortugnoCarlo Bertucci
Jan 4, 2015·Journal of Pharmaceutical and Biomedical Analysis·Daniele TedescoCarlo Bertucci
Jul 16, 2016·Journal of Photochemistry and Photobiology. B, Biology·Xiaoyi LiuYing Zhou
Jun 4, 2013·Dalton Transactions : an International Journal of Inorganic Chemistry·Chew-Hee NgWeng Kee Leong
Feb 8, 2011·Journal of Separation Science·Chunguang Lv, Zhiqiang Zhou
Jun 27, 2012·Chembiochem : a European Journal of Chemical Biology·Chahrazade El AmriMichael Smietana
Oct 14, 2019·Journal of Pharmaceutical and Biomedical Analysis·Angela De SimoneVincenza Andrisano
Dec 9, 2020·International Journal of Molecular Sciences·Jaime Ribeiro-FilhoMárcia Regina Piuvezam
Mar 6, 2021·Advances in Colloid and Interface Science·Aixa Aguilera-GarridoJulia Maldonado-Valderrama
May 10, 2021·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Nikki KuharSiva Umapathy

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