Title : Phenyl-substituted aminomethylene-bisphosphonates inhibit human P5C reductase and show antiproliferative activity against proline-hyperproducing tumour cells.

Pub. Date : 2021 Dec

PMID : 34107832






4 Functional Relationships(s)
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Protein Name
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1 In certain cancers, such as breast, prostate and some lung and skin cancers, the gene for the enzyme catalysing the second and last step in proline synthesis, delta1-pyrroline-5-carboxylate (P5C) reductase, has been found upregulated. Proline pyrroline-5-carboxylate reductase 1 Homo sapiens
2 This leads to a higher proline content that exacerbates the effects of the so-called proline-P5C cycle, with tumour cells effectively using this method to increase cell survival. Proline pyrroline-5-carboxylate reductase 1 Homo sapiens
3 This leads to a higher proline content that exacerbates the effects of the so-called proline-P5C cycle, with tumour cells effectively using this method to increase cell survival. Proline pyrroline-5-carboxylate reductase 1 Homo sapiens
4 The actual occurrence in vivo of enzyme inhibition was assessed on myelogenous erythroleukemic K562 and epithelial breast cancer MDA-MB-231 cell lines, whose growth was progressively impaired by concentrations of the dibromo derivative ranging from 10-6 to 10-4 M. Interestingly, growth inhibition was not relieved by the exogenous supply of proline, suggesting that the effect relies on the interference with the proline-P5C cycle, and not on proline starvation. Proline pyrroline-5-carboxylate reductase 1 Homo sapiens