Glycobiology and Drug Design by Anatole A. Klyosov

By Anatole A. Klyosov

In past times a number of years, it has turn into more and more transparent that carbohydrates, which might be specific to express ailments, signify an entire new measurement in drug layout. characterised via a number of phrases - particular reputation, lectins, and molecular range, simply to cite a number of - this new size in line with carbohydrates primarily has brought a brand new language to chemistry, biochemistry, and similar disciplines. Vocabulary has been construction so speedy, actually, that almost all expert chemists (i.e., practitioners who're one of the few who paintings within the sector of carbohydrates) could occasionally think a piece illiterate. This publication might help them and lots of different scientists to raised comprehend the present state-of-the-art and the demanding situations that stay in effectively consummating suits of carbohydrate-based medicinal drugs and the lethal ailments they aim. This e-book contains preclinical experiences and medical trials of carbohydrate-based medications in growth in addition to reading their supply, biocompatibility, clearance, and metabolic pathways. extra, this publication explores a couple of different beneficial properties of carbohydrate medications and their ambitions, reminiscent of the constitution of antibodies with strangely high-affinity for carbohydrates, and protein-glycan interactions and their inhibitors. Galactomannans and thio-, imino-, nitro-, and aminosugars are relatively thought of with appreciate to their structural and useful affects. This quantity won't in basic terms replace current courses on carbohydrate-based drug layout but additionally extra form the rising information and pondering during this new area.

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9% in RA vs. 7% in control. The two polymorphic forms (SNP) of galectin-3 gene were located at rs4644 and rs4652 sites in the DNA. Almost at the same time, another study (22) showed that galectin-3 is present in the inflamed synovium in patients with rheumatoid arthritis, and plays a pathogenic role in the development and progression of antigen-induced arthritis. The authors showed that the joint inflammation and bone erosion in mice were markedly suppressed in galectin-3 null mice as compared with wild-type mice.

The authors concluded that loss of galectin-8 might be an early step in the development of malignant lesions of the bladder and a significant independent predictor of recurrence. Aside from galectin-3 and -8, galectin-1 and -4 have been reported to be clinically significant as colorectal cancer markers (44). These authors showed early on that galectin-1 is over-expressed in colorectal carcinoma (CRC) tissues. In this paper, they showed in 105 CRC patients and 100 healthy volunteers (control) that levels of circulating galectin-1 and -4 reflect the presence of CRC and/or its state of progression.

Furthermore we have shown that the principal mechanism of action of the drug candidate, DAVANAT, which is a modified galactomannan, is the strong blocking of galectin-1 and galectin-3. In other words, DAVANAT is a galectin blocker. In vitro, the binding constant for DAVANAT with isolated and purified galectin-1 and -3 was found to be in the micromolar range (~10 μM), but with a stoichiometry of binding 3 to 6 molecules of galectin-1 to one molecule of DAVANAT (molecular weight of 59 kDa). 8 μg/mL, that is 60-70 nM.

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