CAS: 67869-62-9; (S)-1-((S)-2-((S)-1-(2-Aminoacetyl)Pyrrolidine-2-Carboxamido)-5-Guanidinopentanoyl)Pyrrolidine-2-Carboxylic Acid

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📜叔丁氧羰基-脯氨酰-琥珀酰亚胺置于盐酸,Sodium Hydroxide,Tea,1-羟基苯并三唑,N,N'-二环己基碳二亚胺体系中,用 乙酸乙酯 作为反应溶剂,化学反应生成 H-甘氨酸-脯氨酸-精氨酸-脯氨酸-Oh乙酸盐
参考文献:Synthesis Of Modified Fragments Of Fibrinogen And Their Effect On The Activity Of Proteolytic Enzymes
标题:Synthesis Of Modified Fragments Of Fibrinogen And Their Effect On The Activity Of Proteolytic Enzymes
摘要:New Analogues Of The Gly-Pro-Arg And Arg-Gly-Asp Fragments Of Fibrinogen Were Synthesized: Gly-Pro-Arg-Pro (1),Gly-Pro-Arg-Pro-Met-We (11),Gly-Pro-Arg-Pro-Phe (111),Gly-Pro-Arg-Pro-Asp (Iv),Gly-Pro-Arg-Pro-Glu (V),And Arg-Asn-Trp-Asp (Vi). Their Effect On The Activity Of Proteases Of Various Types Was Studied With The Method Of Lysis Of Fibrin Plates. All The Peptides Were Found To Inhibit Plasmin Activity (By 60-85%) And The Gamma-Subunit Of Nerve Growth Factor (By 55-93%). Tetrapeptide (Vi) Proved To Be An Effective Inhibitor Of Tissue Activator Of Plasminogen And The 7-Subunit Of Nerve Growth Factor (By 96 And 93%,Respectively). The Peptides Exerted Practically No Effect On The Activity Of Urokinase And Moderately Inhibited The Activity Of Streptokinase [(Iii),Iv),And (Vi)],Papain [(I),(II),Iv),And (Vi)],Subtilisin [(V) And (Vi)],(X-Chymotrypsin [(Iii),(V),And Vi)],And Bacillus Subtilis Metalloprotease (Vi). They Inhibit Trypsin [except For (1) And (111)] When Applied On Fibrin Plates At A Concentration Of I X 10(-2) M,While,At The Concentration Of I X 10(-3) M,(1) And (11) Induced An Increase In Proteolytic Activity By 35 And 47%,Respectively.
DOI:10.1134/s106816200602004X

专利信息

专利号:US-7153933-B2
优先权日:2001-12-07
标 题 :Solid phase method for synthesis peptide-spacer-lipid conjugates, conjugates synthesized thereby and targeted liposomes containing the same
发明人：WU SHIH-KWANG; CHANG TING-GUNG; TSENG CHIN-LU; CHEN LI-JUNG; SHIH KAE-SHYANG
权利人:DEV CENTER BIOTECHNOLOGY
摘要:A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.

专利号:US-5814460-A
优先权日:1990-02-14
标题:Method for generating and screening useful peptides
发明人：VENTON DUANE L; HOPFINGER ANTON J; LEBRETON GUY
权利人:DIATIDE INC
摘要:PCT No. PCT/US93/08231 Sec. 371 Date Feb. 21, 1995 Sec. 102(e) Date Feb. 21, 1995 PCT Filed Aug. 9, 1993 PCT Pub. No. WO94/04558 PCT Pub. Date Mar. 3, 1994The invention allows the generation and screening of a large population of peptides for the presence of peptides which bind a particular macromolecule or macromolecular complex with high affinity, and further allows the favored net synthesis of analyzable quantities of such peptides, by using is the 'trap' a macromolecule or macromolecular complex for which binding of the peptide is desired. The starting mixture is preferably spiked with a peptide having some affinity for the target macromolecule so that mutation of the spike or 'lead' peptide is favored. The development of improved binding peptides through scrambling may be dynamically monitored by initially binding the target with an insolubilized ligand, and then looking for an increase in the concentration of the target in the soluble phase as a result of the displacement of the reference ligand by scrambled peptides.

专利号:ES-2403154-T3
优先权日:1997-04-11
标 题 :Methods and compositions for the synthesis of long chain polyunsaturated fatty acids in plants

专利号:JP-2004189617-A
优先权日:2002-12-06
标题 :Solid-phase method for synthesis of peptide/spacer/lipid conjugate, conjugate synthesized thereby, and objective liposome containing the conjugate

专利号:WO-9846763-A1
优先权日:1997-04-11
标题:Methods and compositions for synthesis of long chain polyunsaturated fatty acids

专利号:US-5366862-A
优先权日:1990-02-14
标题 :Method for generating and screening useful peptides
发明人：VENTON DUANE L; HOPFINGER ANTON J; LE BRETON GUY
权利人:RECEPTOR LAB INC
摘要:The invention allows the generation and screening of a large population of peptides for the presence of peptides which bind a particular macromolecule or macromolecular complex with high affinity, and further allows the favored net synthesis of analyzable quantities of such peptides, by using as the 'trap' a macromolecule or macromolecular complex for which binding of the peptide is desired. The starting mixture is preferably spiked with a peptide having some affinity for the target macromolecule so that mutation of the spike or 'lead' peptide is favored. The development of improved binding peptides through scrambling may be dynamically monitored by initially binding the target with an insolubilized ligand, and then looking for an increase in the concentration of the target in the soluble phase as a result of the displacement of the reference ligand by scrambled peptides.