CAS: 7298-84-2; (S)-2-((S)-2-Amino-4-Methylpentanamido)Propanoic Acid

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📜N--L-Alanin-Benzylester置于palladium(II) Oxide Hydrate 氢气体系中,用 甲醇,溶剂黄146 作为反应溶剂,化学反应生成 L-亮氨酸-L-丙氨酸
参考文献:Synthesis Of L-Leucyl-L-Alanyl-L-Valyl-L-Glutamic Acid And Intermediate Peptides1
标题:Synthesis Of L-Leucyl-L-Alanyl-L-Valyl-L-Glutamic Acid And Intermediate Peptides1
摘要:
DOI:10.1021/jo01065A039

专利信息

专利号:US-7829669-B2
优先权日:1999-06-28
标 题:Catalytically active recombinant memapsin and methods of use thereof
发明人：KOELSCH GERALD; TANG JORDAN J N; HONG LIN; GHOSH ARUN K; LIN XINLI
权利人:OKLAHOMA MED RES FOUND; UNIV ILLINOIS
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

专利号:US-2015328616-A1
优先权日:2014-05-13
标题:Surface mediated synthesis of polynucleotides, polypeptides and polysaccharides and related materials, methods and systems
发明人：GETHERS MATTHEW; GODDARD III WILLIAM A; WEISS PAUL S; RANDALL JOHN
权利人:CALIFORNIA INST OF TECHN
摘要:Surface mediated polymer synthesizing methods and related systems and materials are described where monomers are attached to monomer binding regions on a surface and subsequently form chemical bonds with adjacent monomers on the surface to form linear polymers selected from polynucleotide, polypeptides and polysaccharides.

专利号:US-2002049303-A1
优先权日:1999-06-28
标 题 :Catalytically active recombinant memapsin and methods of use thereof
发明人：TANG JORDAN J N; LIN XINLI; KOELSCH GERALD; HONG LIN
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogs including isosteres at the sites of the critical amino acid residues were developed and the substrate analogs, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

专利号:US-2010292439-A1
优先权日:2006-07-05
标 题 :Use of Functionalized Onium Salts for Peptide Synthesis
发明人：VAULTIER MICHEL; ROCHE CELINE; GMOUH SAID; COMMERCON ALAIN
权利人:CENTRE NAT RECH SCIENT; UNIV RENNES
摘要:A subject of the invention is the use of a salt with a dedicated task of formula (I): n A + -L-R—OY, X − n as soluble support for peptide synthesis, in which:n X − represents a functional or non-functional anion, Y represents either a hydrogen atom, or a —COOR 1 group, R 1 representing in particular an alkyl group comprising 1 to 20 carbon atoms, A + represents a cationic entity, L represents an arm, in particular an alkyl group of 3 to 20 carbon atoms, R represents in particular a group of formula —C(R a )(R b )—, R a and R b representing independently of one another in particular a hydrogen or an alkyl group, comprising 1 to 20 carbon atoms.

专利号:US-8273403-B2
优先权日:2002-05-10
标题 :Generation of surface coating diversity
发明人：BARDEN MICHAEL C; KAMBOURIS PETER A
权利人:BARDEN MICHAEL C; KAMBOURIS PETER A; BIO LAYER PTY LTD
摘要:This invention relates to a surface discovery system and high-throughput combinatorial synthesis methods for generating large numbers of diverse surface coatings on solid substrates. The system is built upon a synthon which comprises at least three elements: a chemical backbone coating on the solid substrate that comprises a copolymer (B) of at least one passive constituent (P) and at least one active constituent (A); a spacer unit (S) separating the backbone from a functional group; and a functional group (F). The methods comprise the following steps: 1) selecting a plurality of synthons so that each synthon has at least two points of diversity selected from P, A, S and F; 2) applying copolymer B onto a substrate; and 3) attaching a combination of S and F to constituent A of copolymer B. Steps 2) and 3) are performed such that different synthons are generated on localized regions of the substrate.

专利号:US-5762918-A
优先权日:1992-03-23
标题:Methods of using steroid-polyanionic polymer-based conjugated targeted to vascular endothelial cells
发明人：THORPE PHILIP E
权利人:UNIV TEXAS
摘要:This invention discloses new targeted conjugates for the delivery of a compound, and particularly, a steroid, to vascular endothelial cells. The conjugates comprise two components, preferably linked by a selectively-hydrolyzable bond, such as an acid-labile bond or enzyme-sensitive bond. The first component, a polyanionic polymer, and preferably, a polysulphated polymer such as a heparin-derivative, specifically directs the conjugate to vascular endothelial cells. The second component is a selected agent, such as a steroid, which exerts a specific effect on the target cell following its release. In particular, the present invention provides novel conjugated angiogenesis inhibitors, for use in the treatment of pathogenic conditions including cancer, arthritis, and diabetic blindness. An inhibitor comprising a heparin derivative and the anti-angiogenic steroid, cortisol, is herein shown to be markedly acid-labile, to suppress DNA synthesis and cell migration in human umbilical vein endothelial cells, to retard or abolish (depending pending on the route of injection) the vascularization of sponges in vivo and to retard lung tumor growth in mice by 65%. No adverse effects of the conjugate were detected, and equivalent treatments with a mixture of heparin plus cortisol were significantly less effective in all cases.