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In Quest for Improved Drugs against Diabetes: The Added Value of X-ray Powder Diffraction Methods

Section of Genetics, Cell Biology and Development, Department of Biology, University of Patras, GR-26500 Patras, Greece
Author to whom correspondence should be addressed.
Academic Editor: Dilano K. Saldin
Biomolecules 2017, 7(3), 63;
Received: 10 July 2017 / Revised: 14 August 2017 / Accepted: 16 August 2017 / Published: 22 August 2017
(This article belongs to the Special Issue Protein Crystallography 2016)
Human insulin (HI) is a well-characterized natural hormone which regulates glycose levels into the blood-stream and is widely used for diabetes treatment. Numerous studies have manifested that despite significant efforts devoted to structural characterization of this molecule and its complexes with organic compounds (ligands), there is still a rich diagram of phase transitions and novel crystalline forms to be discovered. Towards the improvement of drug delivery, identification of new insulin polymorphs from polycrystalline samples, simulating the commercially available drugs, is feasible today via macromolecular X-ray powder diffraction (XRPD). This approach has been developed, and is considered as a respectable method, which can be employed in biosciences for various purposes, such as observing phase transitions and characterizing bulk pharmaceuticals. An overview of the structural studies on human insulin complexes performed over the past decade employing both synchrotron and laboratory sources for XRPD measurements, is reported herein. This review aims to assemble all of the recent advances in the diabetes treatment field in terms of drug formulation, verifying in parallel the efficiency and applicability of protein XRPD for quick and accurate preliminary structural characterization in the large scale. View Full-Text
Keywords: insulin; phenolic derivatives; crystallography; powder diffraction insulin; phenolic derivatives; crystallography; powder diffraction
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Karavassili, F.; Valmas, A.; Fili, S.; Georgiou, C.D.; Margiolaki, I. In Quest for Improved Drugs against Diabetes: The Added Value of X-ray Powder Diffraction Methods. Biomolecules 2017, 7, 63.

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