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Updated: May 22, 2026
Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Beta-testing of PI3-kinase inhibitors: is beta better?
Peter R Shepherd1, William A Denny
1Department of Molecular Medicine and Pathology, School of Medical Sciences, University of Auckland, Auckland, New Zealand.
Abstract:
Although it has been known for some time that PTEN-null tumors require expression of the p110β isoform of phosphoinositide 3-kinase for growth, the corollary demonstration that small-molecule inhibitors of p110β are effective drugs for such tumors has not been shown. This has now been rectified by the demonstration that the TGX221 analogue KIN-193 is effective in mouse xenografts of HCC70 and PC3 human tumor cell lines.
Insights
Small-molecule inhibitors targeting p110β are effective treatments for PTEN-null tumors. KIN-193, a p110β inhibitor, demonstrated efficacy in preclinical models of human cancer cell lines.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- PTEN-null tumors exhibit a dependency on the p110β isoform of phosphoinositide 3-kinase for their growth.
- The therapeutic potential of targeting p110β in these tumors with small-molecule inhibitors remained largely unproven.
Purpose of the Study:
- To demonstrate the efficacy of p110β small-molecule inhibitors as a therapeutic strategy for PTEN-null tumors.
- To evaluate a specific p110β inhibitor, KIN-193, in preclinical cancer models.
Main Methods:
- Utilized mouse xenograft models engrafted with human tumor cell lines (HCC70 and PC3).
- Administered KIN-193, a TGX221 analogue and p110β inhibitor, to assess its anti-tumor effects.
Main Results:
- KIN-193 demonstrated significant efficacy in inhibiting tumor growth in both HCC70 and PC3 xenograft models.
- This study provides the first evidence for the effectiveness of p110β inhibitors in treating PTEN-null tumors.
Conclusions:
- Small-molecule inhibition of p110β is a viable therapeutic approach for PTEN-null cancers.
- KIN-193 represents a promising drug candidate for further clinical development against these tumor types.
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