Coumarins: old compounds with novel promising therapeutic perspectives.
- M. Riveiro, N. de Kimpe, C. Davio
- Chemistry, BiologyCurrent Medicinal Chemistry
- 1 May 2010
The present review highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anti-cancer agents and the translation of current knowledge into new potential lead compounds and the repositioning of known compounds for the treatment of cancer.
Multidrug Resistance Protein 4 (MRP4/ABCC4) Regulates cAMP Cellular Levels and Controls Human Leukemia Cell Proliferation and Differentiation*
- S. Copsel, Corina I. García, C. Davio
- Biology, ChemistryJournal of Biological Chemistry
- 4 January 2011
It is shown that intracellular cAMP levels not only in U937 cells but also in other acute myeloid leukemia cell lines are also regulated by multidrug resistance-associated proteins (MRPs), particularly MRP4, and provided the first evidence that MRP 4 may represent a new potential target for leukemia differentiation therapy.
Structural insights into hydroxycoumarin-induced apoptosis in U-937 cells.
- M. Riveiro, A. Moglioni, C. Davio
- Chemistry, BiologyBioorganic & Medicinal Chemistry
- 1 March 2008
Histamine modulates the expression of c-fos through cyclic AMP production via the H2 receptor in the human promonocytic cell line U937.
The results indicate that histamine activates several mechanisms involved in the induction of differentiation, such as cAMP and c-fos production, but fails to promote differentiation of U937 cells, apparently due to the rapid desensitization of H2 receptors.
Mepyramine, a Histamine H1 Receptor Inverse Agonist, Binds Preferentially to a G Protein-coupled Form of the Receptor and Sequesters G Protein*
- C. Fitzsimons, F. Monczor, N. Fernández, C. Shayo, C. Davio
- Biology, ChemistryJournal of Biological Chemistry
- 13 August 2004
The present work finds that mepyramine is able to decrease the basal constitutive activity of the guinea pig H1 receptor, to bind with high affinity to a Gq/11 protein-coupled form of the receptor and to reduce G protein availability for other non-related receptors associated with the same signaling pathway.
Toward establishing structure-activity relationships for oxygenated coumarins as differentiation inducers of promonocytic leukemic cells.
- M. Riveiro, Dominick Maes, C. Davio
- Chemistry, BiologyBioorganic & Medicinal Chemistry
- 15 September 2009
Histamine acting on H1 receptor promotes inhibition of proliferation via PLC, RAC, and JNK-dependent pathways.
- C. Notcovich, F. Diez, C. Shayo
- BiologyExperimental Cell Research
- 1 February 2010
Structure-anti-leukemic activity relationship study of ortho-dihydroxycoumarins in U-937 cells: key role of the δ-lactone ring in determining differentiation-inducing potency and selective…
- R. Vazquez, M. Riveiro, C. Davio
- Biology, ChemistryBioorganic & Medicinal Chemistry
- 15 September 2012
Physiological implications of biased signaling at histamine H2 receptors
- Natalia Alonso, C. Zappia, N. Fernández
- BiologyFrontiers in Pharmacology
- 10 March 2015
The findings indicate that while famotidine acts as inverse agonist diminishing cAMP basal levels, it mimics the effects of histamine and the agonist amthamine concerning receptor desensitization and internalization, and support that ligand bias is not only a pharmacological curiosity but has physiological and pharmacological implications on cell metabolism.
The time-course of cyclic AMP signaling is critical for leukemia U-937 cell differentiation.
- C. Shayo, B. L. Legnazzi, C. Davio
- BiologyBiochemical and Biophysical Research…
- 13 February 2004
...
...