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Inhibition of phospholipase D by agents that inhibit cell growth.
Anticancer Res. 1993 Jul-Aug; 13(4):1239-44.AR

Abstract

The phospholipases are an important class of enzymes for growth factor and oncogene intracellular signalling. The anti-tumor drug suramin was found to inhibit phosphatidylcholine hydrolysis and trans-phosphatidylation by solubilized rat brain phospholipase D (PLD) with an IC50 of 15 microM. An azo analogue of suramin, which is a considerably more potent inhibitor of phosphatidylinositol phospholipase C (PIPLC) than suramin, inhibited PLD with and IC50 of 58 microM. D-609, a xanthogenate compound with in vitro antitumor activity, inhibited PLD with an IC50 of 820 microM. The cytotoxic aminosteroid compound U-73, 122 was a weaker inhibitor of PLD with an IC50 of 78 microM. However, U-73, 122 was a more potent inhibitor of PLD in fibroblast membranes with an IC50 of 25 microM, while suramin was less active with an IC50 of 4.2 mM. The antitumor ether lipid drug ET-18-OCH3 did not inhibit solubilized or membrane PLD although it is a potent inhibitor of PIPLC. The results of the study show that the compounds tested have different abilities to inhibit PIPLC and PLD. Access of hydrophilic drugs to membrane PLD may be a limiting factor to their inhibitory activity.

Authors+Show Affiliations

Arizona Cancer Center, University of Arizona Health Sciences Center, Tucson 85724.No affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

8352550

Citation

Gratas, C, and G Powis. "Inhibition of Phospholipase D By Agents That Inhibit Cell Growth." Anticancer Research, vol. 13, no. 4, 1993, pp. 1239-44.
Gratas C, Powis G. Inhibition of phospholipase D by agents that inhibit cell growth. Anticancer Res. 1993;13(4):1239-44.
Gratas, C., & Powis, G. (1993). Inhibition of phospholipase D by agents that inhibit cell growth. Anticancer Research, 13(4), 1239-44.
Gratas C, Powis G. Inhibition of Phospholipase D By Agents That Inhibit Cell Growth. Anticancer Res. 1993 Jul-Aug;13(4):1239-44. PubMed PMID: 8352550.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of phospholipase D by agents that inhibit cell growth. AU - Gratas,C, AU - Powis,G, PY - 1993/7/1/pubmed PY - 1993/7/1/medline PY - 1993/7/1/entrez SP - 1239 EP - 44 JF - Anticancer research JO - Anticancer Res VL - 13 IS - 4 N2 - The phospholipases are an important class of enzymes for growth factor and oncogene intracellular signalling. The anti-tumor drug suramin was found to inhibit phosphatidylcholine hydrolysis and trans-phosphatidylation by solubilized rat brain phospholipase D (PLD) with an IC50 of 15 microM. An azo analogue of suramin, which is a considerably more potent inhibitor of phosphatidylinositol phospholipase C (PIPLC) than suramin, inhibited PLD with and IC50 of 58 microM. D-609, a xanthogenate compound with in vitro antitumor activity, inhibited PLD with an IC50 of 820 microM. The cytotoxic aminosteroid compound U-73, 122 was a weaker inhibitor of PLD with an IC50 of 78 microM. However, U-73, 122 was a more potent inhibitor of PLD in fibroblast membranes with an IC50 of 25 microM, while suramin was less active with an IC50 of 4.2 mM. The antitumor ether lipid drug ET-18-OCH3 did not inhibit solubilized or membrane PLD although it is a potent inhibitor of PIPLC. The results of the study show that the compounds tested have different abilities to inhibit PIPLC and PLD. Access of hydrophilic drugs to membrane PLD may be a limiting factor to their inhibitory activity. SN - 0250-7005 UR - https://www.unboundmedicine.com/medline/citation/8352550/Inhibition_of_phospholipase_D_by_agents_that_inhibit_cell_growth_ DB - PRIME DP - Unbound Medicine ER -