Chirality and drug targeting: pros and cons.
The theoretical basis of stereoselectivity in drug targeting in terms of eudismic ratio and quantitative structure-activity relationship has been presented. Specific examples of the advantages of using the correct stereoisomers (eutomers) rather than the distomers or racemic mixtures have been discussed. With the recent development of new methods of chiral synthesis and chiral analysis, it is not longer justifiable to continue to use racemic mixtures as therapeutic agents, unless it can be proven to be safe to do so. In the area of using peptides, proteins, glycoproteins and polysaccharides as therapeutic agents, mother nature has been very selective in choosing the optically active starting materials (Bradley, 1994), it is a necessity to design and test the proper optical isomer when a mimetic or antagonist compound is contemplated as a therapeutic agent.
Lien
E J
EJ
Department of Pharmaceutical Sciences, University of Southern California, School of Pharmacy, Los Angeles 90033, USA.
D003198:Computer Simulation; D006023:Glycoproteins / Q000737:chemistry / Q000493:pharmacokinetics; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics; D011134:Polysaccharides / Q000737:chemistry / Q000493:pharmacokinetics; D011506:Proteins / Q000737:chemistry / Q000493:pharmacokinetics; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013792:Thalidomide / Q000737:chemistry / Q000633:toxicity
D006023:Glycoproteins; D010455:Peptides; D011134:Polysaccharides; D011506:Proteins; D013792:Thalidomide