TPC2 targeting evolution: Leveraging therapeutic opportunities for cancer
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Updated: Oct 23, 2025

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Abeer F Alharbi1, John Parrington2
1Department of Pharmacology, University of Oxford, Oxford, UK; Pharmaceutical Sciences Department, College of Pharmacy, King Saud Bin Abdul-Aziz University for Health Sciences, Riyadh, Saudi Arabia.
Abstract:
Growing evidence implicates a vital role for TPC2/Ca2+ signaling in pathophysiological processes attributed to cancer, raising questions regarding the utility of TPC2 as a cancer therapeutic target. In this issue of Cell Chemical Biology, Müller et al. (2021) develop TPC2 inhibitors, SG005 and SG-094, exhibiting anti-tumor effects with potential translational relevance.
Insights
New TPC2 inhibitors, SG005 and SG-094, show anti-tumor effects. These findings suggest TPC2 calcium signaling could be a viable therapeutic target for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Growing evidence links TPC2/calcium (Ca2+) signaling to cancer pathophysiology.
- The role of TPC2 in cancer raises questions about its potential as a therapeutic target.
Purpose of the Study:
- To develop novel TPC2 inhibitors.
- To evaluate the anti-tumor efficacy of these inhibitors.
Main Methods:
- Development of TPC2 inhibitors, specifically SG005 and SG-094.
- Assessment of the anti-tumor effects of SG005 and SG-094 in relevant models.
Main Results:
- The developed TPC2 inhibitors, SG005 and SG-094, demonstrated significant anti-tumor effects.
- The findings indicate potential translational relevance for TPC2-targeted cancer therapy.
Conclusions:
- TPC2 inhibitors represent a promising therapeutic strategy for cancer treatment.
- Targeting TPC2/Ca2+ signaling offers a potential avenue for novel anti-cancer drug development.
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