Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers(516 views) Pérez de Vega MJ, García-López MT, Zaccaro L, Royo M, Albericio F, Fernández-Carvajal A, Ferrer-Montiel A, González-Muñiz R
Instituto de Química Médica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain
Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain
IBMC-UMH, Ed. Torregaitán, Av. de la Universidad s/n, 03202 Elche, Spain
Instituto de Qu mica M dica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
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Bonache, M.A., García-Martínez, C., García De Diego, L., Carreno, C., Pérez De Vega, M.J., García-López, M.T., Ferrer-Montiel, A., González-Muñiz, R., Old molecule for new receptors: Trp(Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
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Levine, J. D., Alessandri-Haber, N., TRP channels: Targets for the relief of pain (2007) Biochim. Biophys. Acta, 1772, pp. 989-100
Gunthorpe, M. J., Chizh, B. A., Clinical development of TRPV1 antagonists: Targeting a pivotal point in the pain pathway (2009) Drug Discov. Today, 14, pp. 56-67
Garc a-Mart nez, C., Morenilla-Palao, C., Planells-Cases, R., Merino, J. M., Ferrer-Montiel, A., Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties (2000) J. Biol. Chem., 275, pp. 32552-32558
Garc a-L pez, M. T., Herranz, R., Gonz lez-Mu iz, R., Naranjo, J. R., De Ceballos, M., Del R o, J., Antinociceptive effects in rodents of the dipeptide Lys-Trp (Nps) and related compounds (1986) Peptides, 7, pp. 39-43
Bonache, M. A., Garc a-Mart nez, C., Garc a De Diego, L., Carreno, C., P rez De Vega, M. J., Garc a-L pez, M. T., Ferrer-Montiel, A., Gonz lez-Mu iz, R., Old molecule for new receptors: Trp (Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
Szardenings, A. K., Burtoth, T. S., Look, G. C., Campbell, D. A. A., Reductive alkylation procedure applicable to both solution- and solid-phase syntheses of secondary amines (1996) J. Org. Chem., 61, pp. 6720-6722
Shey, J. -Y., Sun, C. -M., Soluble polymer supported synthesis of N, N-di (Boc) -protected guanidines (1998) Synlett, pp. 1423-1425
Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers
Trp(Nps)-Lys-NH(2) derivatives, bearing alkyl or guanidine groups either at the N-terminus or on the Lys side-chain or at both positions were conveniently prepared on solid-phase and evaluated as TRPV1 channel antagonists.
Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers
No results.
Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers