Inhibitors of Phosphatidylinositol-specific Phospholipase C wit h Myo-inositol Scaffold

New compounds exhibiting significant inhibitory activity against PI-PLC have been identified. The findings could prove valuable in the development of clinically applicable PI-PLC inhibitors, particularly for the treatment of cancer. Additionally, the myo-inositol derivatives developed demonstrated greater suitability for studying PI-PLC's role in physiological processes in tissue homogenates compared to the maleimide derivative U73122, which is commonly used for this purpose in scientific research. This advantage arises from the fact that U73122 is a non-specific 'pan-assay interference compound' (PAIN).

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Publication Details

Journal
Medicinal Chemistry
Published
2025-05-05
DOI
https://doi.org/10.2174/0115734064384345250415073648
Primary Topic
Biomedical Research and Pathophysiology
Type
article
Field-Weighted Citation Impact
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article

Inhibitors of Phosphatidylinositol-specific Phospholipase C wit h Myo-inositol Scaffold

Matthias Lehr, Walburga Hanekamp, Christoph Arenz, Christian Bierkamp
Medicinal Chemistry
Biomedical Research and Pathophysiology
article

Inhibitors of Phosphatidylinositol-specific Phospholipase C wit h Myo-inositol Scaffold

Matthias Lehr, Walburga Hanekamp, Christoph Arenz, Christian Bierkamp
article en

Abstract

New compounds exhibiting significant inhibitory activity against PI-PLC have been identified. The findings could prove valuable in the development of clinically applicable PI-PLC inhibitors, particularly for the treatment of cancer. Additionally, the myo-inositol derivatives developed demonstrated greater suitability for studying PI-PLC's role in physiological processes in tissue homogenates compared to the maleimide derivative U73122, which is commonly used for this purpose in scientific research. This advantage arises from the fact that U73122 is a non-specific 'pan-assay interference compound' (PAIN).

Medicinal ChemistryVol. 22(2)
University of Münster (DE), Humboldt-Universität zu Berlin (DE)
Openalex Percentile: Top 86%
Biomedical Research and Pathophysiology
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