| Added by | mollevi |
|---|---|
| Group name | PlateformePCC |
| Item Type | Journal Article |
| Title | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7?-OBz-11?(R)-OTHP-5?-pregnanedione in K562/R7 and H295R cell xenografts |
| Creator | Alameh et al. |
| Author | Ghina Alameh |
| Author | Agnès Emptoz-Bonneton |
| Author | Marc Rolland de Ravel |
| Author | Eva L. Matera |
| Author | Elisabeth Mappus |
| Author | Patrick Balaguer |
| Author | Luc Rocheblave |
| Author | Thierry Lomberget |
| Author | Charles Dumontet |
| Author | Marc Le Borgne |
| Author | Michel Pugeat |
| Author | Catherine Grenot |
| Author | Claude Y. Cuilleron |
| Abstract | Synthetic progesterone and 5?/?-pregnane-3,20-dione derivatives were evaluated as in vitro and in vivo modulators of multidrug-resistance (MDR) using two P-gp-expressing human cell lines, the non-steroidogenic K562/R7 erythroleukaemia cells and the steroidogenic NCI-H295R adrenocortical carcinoma cells, both resistant to doxorubicin. The maximal effect in both cell lines was observed for 7?-O-benzoyloxy,11?(R)-O-tetrahydropyranyloxy-5?-pregnane-3,20-dione 4. This modulator co-injected with doxorubicin significantly decreased the tumour size and increased the survival time of immunodeficient mice xenografted with NCI-H295R or K562/R7 cells. |
| Publication | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Volume | 34 |
| Issue | 1 |
| Pages | 684-691 |
| Date | Dec 2019 |
| Journal Abbr | J Enzyme Inhib Med Chem |
| Language | eng |
| DOI | 10.1080/14756366.2019.1575825 |
| ISSN | 1475-6374 |
| Library Catalog | PubMed |
| Extra | PMID: 30777494 PMCID: PMC6383615 |
| Tags | Animals, Antineoplastic Agents, Cell Proliferation, Cell Survival, Dose-Response Relationship, Drug, Drug Resistance, Multiple, Drug Resistance, Neoplasm, Drug Screening Assays, Antitumor, Female, Humans, Mice, Mice, SCID, Molecular Conformation, Multidrug resistance, Neoplasms, Experimental, non-steroidogenic and steroidogenic cell lines, original, P-glycoprotein, pregnane modulators, Pregnanes, Structure-Activity Relationship, Tumor Cells, Cultured, xenografts |
| Date Added | 2019/06/04 - 17:03:54 |
| Date Modified | 2019/06/05 - 11:04:16 |
Institut de Recherche en Cancérologie de
