Next Article in Journal
3-Vinylazetidin-2-Ones: Synthesis, Antiproliferative and Tubulin Destabilizing Activity in MCF-7 and MDA-MB-231 Breast Cancer Cells
Next Article in Special Issue
Developments in Carbohydrate-Based Cancer Therapeutics
Previous Article in Journal
TRP Channels and Migraine: Recent Developments and New Therapeutic Opportunities
Previous Article in Special Issue
Chain-Branched Polyhydroxylated Octahydro-1H-Indoles as Potential Leads against Lysosomal Storage Diseases
Open AccessReview

Strategies for the Development of Glycomimetic Drug Candidates

Molecular Pharmacy, Dept. Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland
Pharmaceuticals 2019, 12(2), 55;
Received: 15 March 2019 / Revised: 3 April 2019 / Accepted: 9 April 2019 / Published: 11 April 2019
(This article belongs to the Special Issue Carbohydrates 2018)
Carbohydrates are a structurally-diverse group of natural products which play an important role in numerous biological processes, including immune regulation, infection, and cancer metastasis. Many diseases have been correlated with changes in the composition of cell-surface glycans, highlighting their potential as a therapeutic target. Unfortunately, native carbohydrates suffer from inherently weak binding affinities and poor pharmacokinetic properties. To enhance their usefulness as drug candidates, ‘glycomimetics’ have been developed: more drug-like compounds which mimic the structure and function of native carbohydrates. Approaches to improve binding affinities (e.g., deoxygenation, pre-organization) and pharmacokinetic properties (e.g., limiting metabolic degradation, improving permeability) have been highlighted in this review, accompanied by relevant examples. By utilizing these strategies, high-affinity ligands with optimized properties can be rationally designed and used to address therapies for novel carbohydrate-binding targets. View Full-Text
Keywords: carbohydrate; glycomimetic; drug development; lectin; lead optimization; binding affinity carbohydrate; glycomimetic; drug development; lectin; lead optimization; binding affinity
Show Figures

Figure 1

MDPI and ACS Style

Hevey, R. Strategies for the Development of Glycomimetic Drug Candidates. Pharmaceuticals 2019, 12, 55.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

Back to TopTop