Patent · US Active

Bis-thioether stapled peptides as inhibitors of PRC2 function

US11345725B2 · kind B2 · utility

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3References

2Claims

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Assignee

RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK · US

Inventors

Guillermo Gerona-Navarro · New York, US
Gan Zhang · Boulder, US
Flavia Barragan · Berlin, DE

Key dates

Filing date	Sep 16, 2020
Grant date	May 31, 2022
Priority date	—
Expiry date	Sep 16, 2040

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07K14/4748
WIPO fieldBiotechnology
WIPO sectorChemistry

Abstract

This disclosure describes three novel bisthioether stapled peptides as allosteric inhibitors of Polycomb Repressive Complex 2 (PRC2) catalytic function with demonstrated cell permeability, potent activity in physiological conditions, and strong antiproliferative effects on cancer cells. These inhibitors target, for the first time, two protein interfaces in PRC2 that are crucial for its proper assembling and thus for its histone methyltransferase activity.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.