cas 147900-45-6, Cyclohexanecarboxylicacid, 4-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-, cis-

Articles about 147900-45-6Total 4 be found

Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6
A series of protease activated receptor 2 activating peptide (PAR2-AP) derivatives (1-15) were designed and synthesized. The obtained compounds were tested on a panel of human kallikreins (hKLK1, hKLK2, hKLK5, hKLK6, and hKLK7) and were found completely i
Severino, Beatrice,Fiorino, Ferdinando,Corvino, Angela,Caliendo, Giuseppe,Santagada, Vincenzo,Assis, Diego Magno,Oliveira, Juliana R.,Juliano, Luiz,Manganelli, Serena,Benfenati, Emilio,Frecentese, Francesco,Perissutti, Elisa,Juliano, Maria Aparecida
p. 45 - 52
(2015)
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Discovery of a new phosphotyrosine mimetic for PTP1B using breakaway tethering
Protein tyrosine phosphatases play important roles in many signaling cascades involved in human disease. The identification of druglike inhibitors for these targets is a major challenge, and the discovery of suitable phosphotyrosine (pY) mimetics remains
Erlanson, Daniel A.,McDowell, Robert S.,He, Molly M.,Randal, Mike,Simmons, Robert L.,Kung, Jenny,Waight, Andrew,Hansen, Stig K.
p. 5602 - 5603
(2003)
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Synthesis and Opioid Activity of Dynorphin A-(1-13)NH2 Analogues Containing cis- and trans-4-Aminocyclohexanecarboxylic acid
It has been proposed that the "message" sequence of dynorphin A (Dyn A) exists in an extended conformation in aqueous solution (Schiller, P.W.Int.J.Pept.Protein Res. 1983, 21 307-312).Molecular modeling suggested that trans-4-aminocyclohexanecarboxylic acid (trans-ACCA) might function as a conformationally constrained replacement for Gly2-Gly3 of Dyn A in such an extended conformation.ACCA was synthesized by catalytic hydrogenation of p-aminobenzoic acid, and the cis and trans isomers were separated by fractional recrystallization.Analogues ofDyn A-(1-13)-NH2 containing cis- and trans-ACCA were prepared by solid-phase peptide synthesis using the Fmoc chemical protocol.Results from radioligand binding assays indicated that the peptides have modest affinity for κ opioid receptors (Ki's = 9.1 and 13.4 nM for 2-3>- and 2-3>Dyn A-(1-13)NH2, respectively) and modest κ-receptor selectivity (Ki ratio (κ/μ/δ) = 1/13/210 and 1/21/103, respectively) 2-3>- and 2-3>Dyn A-(1-13)-NH2 are the first reported Dyn A analogues constrained in the "message" sequence that are selective for κ receptors.The cis-ACCA analogue showed very weak opioid activity (IC50 = 4.0 μM) in the guinea pig ileum.
Snyder, Kristin R.,Murray, Thomas F.,DeLander, Gary E.,Aldrich, Jane V.
p. 1100 - 1103
(1993)
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Opioid deltorphin C analogues containing cis- or trans-2- or 3- or 4- aminocyclohexanecarboxylic acid residues
The solid phase synthesis, based on the Fmoc chemical protocol, was used to prepare ten deltorphin C (Del-C; H-Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2) analogues containing cis- and trans- 2 or 3- or 4- aminocyclohexanecarboxylic acid (ACCA) residues at position 2, ACCA-peptides showed high resistance to degradation by plasma or brain enzymes, negligible affinity for the κ- binding site and modest δ- and/or μ-receptor affinities. Both [cis-3- ACCA2]Del-C analogues and one trans isomer are the only deltorphin analogues of this series exhibiting an appreciable δ-affinity and selectivity. These data suggest that the presence of a conformationally constrained ACCA residue in position 2 of the 'message' sequence of deltorphin C is slightly tolerated.
Marastoni, Mauro,Guerrini, Remo,Balboni, Gianfranco,Salvadori, Severo,Fantin, Giancarlo,Fogagnolo, Marco,Lazarus, Lawrence H.,Tomatis, Roberto
p. 6 - 12
(2007/10/03)