Lexitropsin

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Two groups of lexitropsins
Structures of semi-synthetic lexitropsin analogues Script error: No such module "Unsubst".

Lexitropsins are members of a family of semi-synthetic DNA-binding ligands.[1] They are structural analogs of the natural antibiotics netropsin and distamycin. Antibiotics of this group can bind in the minor groove of DNA with different sequence-selectivity.[2][3] Lexitropsins form a complexes with DNA with stoichiometry 1:1 and 2:1. Based on the 2:1 complexes were obtained ligands with high sequence-selectivity.[4] This property is due to their selectivity towards AT-rich regions.[5]

File:Carbocyclilc lexitropsin analogues.png
Synthetic carbocyclic analogues synthesised by Drozdowska et. al[6]

Recently, carbocyclic derivatives based on pentamidine were shown to exhibit in vivo antiproliferative effects on human breast cancer cells, possibly because of their ability to inhibit topoisomerase activity.[7][5][8]

See also

References

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