Prodotti della ricerca

Titolo: Dihydroquinazoline and Triazinedione Derivatives as Prok1 and Prok2 receptor antagonists in HEK-293 transfected cells
Data di pubblicazione: 2015
Abstract: Prokineticin were originally identified as potent agents mediating gut motility, but were later shown to promote angiogenesis in steroidogenic glands, heart and reproductive system. They also modulate neurogenesis, circadian rhythms, nociception, haematopoiesis as well as immune response.[1] Prokineticin are thought to be associated with pathologies of the reproductive systems,[2] myocardial infarction,[3] and tumorigenesis.[4,5] Consequently, antagonism of the prokineticins functions may have utility in the treatment of disorders or diseases including gastrointestinal motility, angiogenesis, haematopoiesis, diabetes and pain. Here we report the identification and pharmacological characterization of a new prototype (KYS-05090) in comparison with our reference prokineticin receptor antagonist (PC-7), [6, 7] (Figure 1). Figure 1. Prokineticin receptor antagonists References [1] Negri, L.; Lattanzi, R.; Giannini, E.; Canestrelli, M.; Nicotra, A.; Melchiorri, P. Bv8/prokineticins and their receptors: a new pronociceptive system. Int. Rev. Neurobiol. 2009, 85, 145-157. [2] Xiao, L.; Zhang, C.; Li, X.; Gong, S.; Hu, R.; Balasubramanian, R.; Crowely, W.F. Jr; Hastings, M.H.; Zhou, Q-Y. Signaling Role of Prokineticin 2 on the Estrous Cycle of Female Mice. PlosOne 2014, 9, e98314. [3] Attramadal, H. Prokineticins and the heart: diverging actions elicited by signaling through prokineticin receptor-1 or -2. Cardiovasc. Res. 2009, 81, 3-4. [4] Monnier, J.; Samson, N. Cytokine properties of prokineticins. FEBS J. 2008, 275, 4014-4021. [5] Shojaei, F.; Wu, X.; Zhong, C.; Yu, L.; Liang, X. H.; Yao, J.; Blanchard D.; Bais, C.; Peale, F. V.; van Bruggen, N.; Ho, C.; Ross, J.; Tan, M.; Carano, R. A.; Meng, Y. G.; Ferrara, N. Bv8 regulates myeloid-cell-dependent tumor angiogenesis. Nature 2007, 450, 825-831. [6] Jang, S.J.; Choi, H.W.; Choi, D.L.; Cho, S.; Rim, H.K.; Choi, H.E.;, Kim, K.S.; Huang, M.; Rhim, H.; Lee, K.T.; Lee J.Y. In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers. Bioorg. Med. Chem Lett. 2013, 23, 6656-6662. [7] Congiu, C.; Onnis, V.; Deplano, A.; Salvadori, S.; Marconi, V.; Maftei, D.; Negri, L.; Lattanzi, R.; Balboni, G. A new convenient synthetic method and preliminary pharmacological characterization of triazinediones as prokineticin receptor antagonists. Eur. J. Med. Chem. 2014, 81, 334-340.
Tipologia:4.1 Contributo in Atti di convegno

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