National Cancer Institute 5R03CA289646-03

Targeting Oxidized PTP1B for Anticancer Drug Discovery

This award funds research to develop charge-neutral inhibitors targeting the oxidized form of PTP1B, an oncogenic protein tyrosine phosphatase involved in various cancers, aiming to improve drug selectivity and bioavailability for anticancer therapy.

Description

PTP1B, a non-receptor–type oncogenic protein tyrosine phosphatase, is involved in growth factor signaling and is frequently amplified in various cancers, including ovarian, gastric, prostate, and breast cancers. Despite its potential as a therapeutic target, developing inhibitors has been challenging due to low cell permeability and lack of selectivity. This project aims to develop charge-neutral inhibitors that specifically target the oxidized form of PTP1B (PTP1B-ox), which is prevalent in disease states. The approach involves preparing and screening sulfenic acid-reactive libraries to identify compounds that stabilize and target oxidized PTP1B, leveraging innovative chemistry and targeting redox forms of proteins.

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