FIELD: biotechnology.
SUBSTANCE: stable cross-linked p53 peptidomimetic macrocycle, a method for its preparation and its use are proposed. The p53 peptidomimetic macrocycle has a structure represented in the formula, and interferes with binding of p53 to MDM2 and/or p53 to MDMX. The P53 peptidomimetic macrocycle can be used to prepare pharmaceutical compositions for treatment of cancer characterized by undesirably low or low p53 activity and/or for the treatment of cancer characterized by undesirably high levels of MDM2 or MDMX activity.
EFFECT: proposed cross-linked p53 macrocycle has cell permeability that is at least twice as high as that of the corresponding macrocycle without cross-links.
50 cl, 7 dwg, 9 tbl, 22 ex
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Authors
Dates
2018-01-24—Published
2013-02-14—Filed