SHP2 inhibition sensitizes diverse oncogene-addicted solid tumors to re-treatment with targeted therapy

A Drilon, MR Sharma, ML Johnson, TA Yap, S Gadgeel… - Cancer discovery, 2023 - AACR
… A SHP2 inhibitor is unlikely to work on its own, however. FIH trials of the first SHP2
inhibitors … to the characterization of combinations with a novel SHP2 inhibitor (PF-07284892/ARRY-…

Recent advances of SHP2 inhibitors in cancer therapy: current development and clinical application

X Yuan, H Bu, J Zhou, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
… date, four SHP2 allosteric inhibitors have entered clinical trials for the treatment of solid
tumors… This review will provide a summary of the physiological and biological functions of SHP2

Shp1 in solid cancers and their therapy

A Varone, D Spano, D Corda - Frontiers in Oncology, 2020 - frontiersin.org
… represents a promising anti-cancer strategy to inhibit tumor growth and induce apoptosis in
… Although a similar mechanism has not yet been reported for solid tumors, we cannot exclude …

[HTML][HTML] Strategies to overcome drug resistance using SHP2 inhibitors

M Liu, S Gao, RM Elhassan, X Hou, H Fang - Acta Pharmaceutica Sinica B, 2021 - Elsevier
… mutations found in leukemia and solid tumors and exhibited 20-fold increase in the basal
phosphatase activity 6 , 34 . NS is an autosomal dominant genetic disease. Germline mutations …

Initial results from a dose finding study of TNO155, a SHP2 inhibitor, in adults with advanced solid tumors.

I Brana, G Shapiro, ML Johnson, HA Yu, D Robbrecht… - 2021 - ascopubs.org
… with on-target effects of SHP2 inhibition. The most common treatment-… of SHP2 inhibition,
as measured by change in DUSP6 expression by qPCR in paired pre- vs. on-treatment tumor

Abstract LB001: Anti-tumor activity and tolerability of the SHP2 inhibitor RMC-4630 as a single agent in patients with RAS-addicted solid cancers

M Koczywas, E Haura, PA Janne, JM Pacheco… - Cancer Research, 2021 - AACR
RMC-4630 is a potent, selective, orally bioavailable allosteric inhibitor of SHP2, a central
node regulating RAS signaling. Consistent with preclinical observations, initial data from a …

Tyrosine phosphatase PTPN11/SHP2 in solid tumors - bull's eye for targeted therapy?

X Chen, SJ Keller, P Hafner, AY Alrawashdeh… - Frontiers in …, 2024 - frontiersin.org
… of SHP2 expression and function in different solid tumor entities, … of clinical trials with allosteric
SHP2-inhibitors we discuss the … protein tyrosine phosphatase for treatment of solid tumors. …

SHP2 Inhibition as a Promising Anti-cancer Therapy: Function in Tumor Cell Signaling and Immune Modulation

J Wang, L Zhang, CA Pratilas… - Journal of Cancer …, 2021 - scientificarchives.com
solid tumor malignancies. One recent study demonstrates that combined pharmacologic
inhibition of SHP2 … NF1-deficient malignant peripheral nerve sheath tumors (MPNST). This article…

Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors

AM Taylor, BR Williams, F Giordanetto… - Journal of Medicinal …, 2023 - ACS Publications
… Our interests in targeting SHP2 were two-fold: 1) to create a SHP2 inhibitorSHP2 inhibition
in different cancer contexts, including in combination with other signaling pathway inhibitors; …

Allosteric inhibition of SHP2 stimulates antitumor immunity by transforming the immunosuppressive environment

E Quintana, CJ Schulze, DR Myers, TJ Choy, K Mordec… - Cancer research, 2020 - AACR
… effect of the SHP2 inhibitor on T cells in vivo, and further, the impact of SHP2 inhibition on
the … The potential for SHP2 inhibitors to provide therapeutic benefit in solid tumors bearing …