Bromo Tryptophan Based Antisickling Peptides: Design, Synthesis and Evaluation

2001 
The polymerisation of deoxy sickle cell Haemoglobin (HbS) within the erythrocytes is the primary molecular event responsible for the patho-physiology of the sickle cell disease. From our theoretical analysis [1], we have found that deoxy sickle haemoglobin exhibits the potential for a limited number of small molecules binding sites in conformity with experimental results. From our theoretical binding studies we designed tripeptide analogs with increased flexibility as well as rigidity (Figure 1). These peptides were synthesised and the oxygen affinity and polymerisation of HbS in the presence of these compounds were measured.
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