专利号:US-10427126-B2 优先权日:2015-10-28 标题 :System and method for longitudinal analysis of peptide synthesis 发明人:Bannen Ryan; Barilovits Sarah; PATEL JIGAR; SULLIVAN ERIC; TAN JOHN 权利人:ROCHE SEQUENCING SOLUTIONS INC 摘要:The present invention provides a system and method for assessing a synthetic peptide population including interrogating a population of peptide features in the presence of a receptor having an affinity for a binder sequence. The population of peptide features is synthesized over a plurality of synthesis periods and includes a plurality of control peptide features synthesized to have an amino acid sequence including the binder sequence. The control peptide features include a first feature synthesized beginning with a first one of the synthesis periods, and a second feature synthesized beginning after the first one of the synthesis periods such that synthesis of the second control peptide feature is delayed by at least one synthesis period. The method further includes detecting a signal output characteristic of an interaction of the receptor with the control peptide features, the signal output indicative of the fidelity of synthesis of the population of peptide features.
专利号:US-2023272006-A1 优先权日:2021-08-31 标题:Peptidomimetics and method of synthesis thereof 发明人:NEFZI ADEL 权利人:NEFZI ADEL; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides compounds, peptidomimetics, and methods of synthesis thereof. The subject invention provides the synthesis and use of guanidino acids and/or poly guanidino acids not only as vehicles for drug delivery but as toolbox for drug discovery. The peptidomimetic of the subject invention comprises oligo(guanidino acid)s or poly(guanidino acid)s with guanidines as peptide bond surrogates. The incorporation of the guanidine as amide bond surrogates offers significant differences in polarity, hydrogen bonding capability, and acid-base character.
专利号:WO-9101724-A1 优先权日:1989-07-27 标题 :Renal-selective prodrugs for the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
专利号:US-5948693-A 优先权日:1994-09-01 标题:Solid phase synthesis of immunosuppressive agents 发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
专利号:US-8227571-B2 优先权日:2007-12-11 标题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R; ROCHE PALO ALTO LLC 摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybridâ€?) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counteparts.
专利号:US-9346892-B2 优先权日:2011-03-18 标题 :Methods for synthesis of an oligopeptide microarray 发明人:ALBERT TOM; RICHMOND TODD; RODESCH MATTHEW; STENGELE KLAUS-PETER; BUEHLER JOCHEN; OTT MARKUS 权利人:ALBERT TOM; RICHMOND TODD; RODESCH MATTHEW; STENGELE KLAUS-PETER; BUEHLER JOCHEN; OTT MARKUS; ROCHE NIMBLE GEN INC 摘要:An oligopeptide microarray and methods for the synthesis thereof are presented. Further presented is a microarray on a solid support comprising at least about 10,000 oligopeptide features per cm 2 and preferably at least about 50,000 oligopeptide features per cm 2 .
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合成参考文献
参考文献:10.1007/s12033-011-9402-x 摘要:Thiele A, Stangl GI, Schutkowski M. Deciphering enzyme function using peptide arrays. Mol Biotechnol. 2011 Nov;49(3):283–305. doi: 10.1007/s12033-011-9402-x. 参考文献:10.1007/s11306-016-1141-3|10.1007/s11306-017-1190-2 摘要:Pharmacometabolomic signature links simvastatin therapy and insulin resistance: an addition to the topical collection “Recent Advances in Pharmacometabolomics: Enabling Tools for Precision Medicine”. Metabolomics. 2017 Mar 17;13(5):57. doi: 10.1007/s11306-017-1190-2.