Abstract
The Gi protein-associated A3 adenosine receptor (A3AR) is over-expressed in inflammatory cells, and this high expression is also reflected in the peripheral blood mononuclear cells of patients with autoimmune inflammatory diseases such as rheumatoid arthritis, psoriasis, and Crohn's disease. CF101, a selective agonist with high affinity to the A3AR, is known to induce robust anti-inflammatory effect in experimental animal models of adjuvant-, collagen-, and tropomyosin-induced arthritis. The effect is mediated via a definitive molecular mechanism entailing deregulation of the nuclear factor-κB (NF-κB) and the Wnt signal transduction pathways resulting in apoptosis of inflammatory cells. CF101 was found to be safe and well tolerated in all preclinical, phase I, and phase II human clinical studies. In two phase II clinical studies where CF101 was administered to rheumatoid arthritis (RA) patients as a stand-alone drug, a significant anti-rheumatic effect and a direct significant correlation were found between receptor expression at baseline and patients' response to the drug, suggesting that A3AR may be utilized as a predictive biomarker. The A3AR is a promising therapeutic target in rheumatoid arthritis and can be used also as a...Continue Reading
References
Sep 1, 1991·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·J Linden
Apr 1, 1989·International Journal of Cardiology·B Clarke, M Coupe
Jun 9, 1997·FEBS Letters·C L SableE Van Obberghen
Jun 22, 1999·Molecular and Cellular Biology·N FilippaE Van Obberghen
Mar 4, 2000·Biochimica Et Biophysica Acta·Z ZhaoK Ravid
Sep 26, 2001·Experimental Cell Research·P FishmanS Pathak
Dec 24, 2003·Oncogene·Pnina FishmanLea Madi
Nov 2, 2004·International Journal of Clinical Pharmacology and Therapeutics·A R van TroostenburgP Fishman
Mar 2, 2006·Arthritis Research & Therapy·Pnina FishmanEhud Baharav
May 1, 2007·Arthritis and Rheumatism·M Carmen MontesinosBruce N Cronstein
May 12, 2009·Cellular Immunology·A OchaionP Fishman
Oct 29, 2011·Drug Discovery Today·Pnina FishmanKenneth A Jacobson
Citations
Sep 1, 2016·Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology·Bálint BotzZsuzsanna Helyes
Sep 26, 2016·Immunologic Research·Ke DongHui-Zhong Zhang
Nov 11, 2016·Nature Reviews. Rheumatology·Bruce N Cronstein, Michail Sitkovsky
Mar 21, 2017·Journal of Medicinal Chemistry·Dilip K ToshKenneth A Jacobson
Apr 27, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jocelyn StockwellFrancisco S Cayabyab
Mar 25, 2017·International Journal of Molecular Sciences·Annalisa RavaniKatia Varani
Jun 1, 2018·Physiological Reviews·Pier Andrea BoreaKatia Varani
Jan 30, 2019·International Journal of Molecular Sciences·Marta VuerichMaria Serena Longhi
Jul 12, 2019·Current Pharmaceutical Design·Yogendra PalShantanu Bandopadhyay
Jul 25, 2019·Current Pharmaceutical Design·Pobitra BorahPran Kishore Deb
Jan 10, 2018·Oncotarget·Minwen XuLiefeng Wang
Jul 29, 2020·Purinergic Signalling·R Rama SureshKenneth A Jacobson
Aug 18, 2020·ChemMedChem·Veronica Salmaso, Kenneth A Jacobson
Jul 7, 2017·Zeitschrift für Rheumatologie·D Redelstein, M Fleck
Dec 14, 2017·International Journal of Molecular Sciences·Yu Ri WooHyun Jeong Park
May 18, 2018·Mediators of Inflammation·F MorandiF Malavasi
Sep 26, 2020·Pharmaceuticals·Giulia Magni, Stefania Ceruti
Feb 10, 2019·International Journal of Molecular Sciences·Luc RochetteCatherine Vergely
Jan 7, 2021·Therapeutic Advances in Musculoskeletal Disease·Julien BlaessRenaud Felten
Jan 7, 2018·Biochemical Pharmacology·Lizi XiaLaura H Heitman
Jun 24, 2021·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Lisa EhlersTimo Gaber
Jul 9, 2021·Psoriasis : Targets and Therapy·Hakim Ben AbdallahLars Iversen
Jun 13, 2021·European Journal of Pharmacology·Krishna YadavManju Rawat Singh
Jul 25, 2021·International Journal of Molecular Sciences·Silvia PasquiniKatia Varani
Nov 19, 2019·Journal of Medicinal Chemistry·Maria João MatosFernanda Borges
Sep 4, 2019·Immunology Letters·Jean L G da SilvaDaniela B R Leal
Dec 20, 2017·Journal of Medicinal Chemistry·Riccardo PetrelliLoredana Cappellacci
Aug 28, 2021·International Journal of Molecular Sciences·Rebecca SohnZsuzsa Jenei-Lanzl
Apr 21, 2018·Oncology Research·Pedro FongLi R Meng