p53 PEPTIDOMIMETIC MACROCYCLES Russian patent published in 2018 - IPC C07K14/47 C07K7/08 C07K7/64 C07K7/54 C07K1/113 A61K38/12 A61K38/10 A61K38/03 A61K38/17 A61P35/00 

Abstract RU 2642299 C2

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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RU 2 642 299 C2

Authors

Gerlave Vensan

Elkin Karl

Nesh Khyu M.

Sojer Tomi K.

Grejvz Bredford Dzh.

Fefan Erik

Dates

2018-01-24Published

2013-02-14Filed