- Glycopeptide derivatives for the preservation and protection of biological materials and microorganisms
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The present invention relates to a compound of the following formula (I): in which at least one and only one group chosen among R5, R6 and R7 is a group of the following formula: The present invention relates also to uses
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Page/Page column 58; 59; 61
(2018/11/06)
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- Efficient near infrared fluorescence detection of elastase enzyme using peptide-bound unsymmetrical squaraine dye
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Extended wavelength analyte-responsive fluorescent probes are highly desired for the imaging applications owing to their deep tissue penetration, and minimum interference from autofluorescence by biomolecules. Near infra-red (NIR) sensitive and self-quenching fluorescent probe based on the dye-peptide conjugate (SQ 1 PC) was designed and synthesized by facile and efficient one-pot synthetic route for the detection of Elastase activity. In the phosphate buffer solution, there was an efficient quenching of fluorescence of SQ 1 PC (86%) assisted by pronounced dye-dye interaction due to H-aggregate formation. Efficient and fast recovery of this quenched fluorescence of SQ 1 PC (> 50% in 30 s) was observed on hydrolysis of this peptide-dye conjugate by elastase enzyme. Presently designed NIR sensitive self-quenching substrate offers the potential application for the detection of diseases related to proteases by efficient and fast detection of their activities.
- Saikiran, Maryala,Sato, Daisuke,Pandey, Shyam S.,Hayase, Shuzi,Kato, Tamaki
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supporting information
p. 4024 - 4029
(2017/08/23)
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- NEW COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING, AND SYNTHESIS, NANO-STRUCTURE AND USE THEREOF
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The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the f
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Paragraph 0086; 0091
(2016/04/19)
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- DHDMIQK(KAP): A novel nano-delivery system of dihydroxyl-tetrahydro-isoquinoline-3-carboxylic acid and KPAK towards the thrombus
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Vascular thrombosis is a major risk of the onset of stroke and so novel therapeutic candidates have been attracting interest. In this context, here docking based computer assisted screening and mesoscale simulation were used to design N-[(S)-6,7-dihydroxy-1,1-dimethyl-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]-Lys(Pro-Ala-Lys), DHDMIQK(KAP), for inhibiting P-selectin expression. In vitro, 1 nM of DHDMIQK(KAP) effectively down-regulated P-selectin expression. In water, in rat plasma and in the solid state DHDMIQK(KAP) formed nanoparticles of a size capable of suitable delivery in the blood circulation. FT-MS and NOESY 2D NMR spectra showed DHDMIQK(KAP) formed hexamers, identified the intermolecular interactions of the hexamer, and assigned the hexamer a butterfly like conformation. Transmission electron microscopy, scanning electron microscopy and atomic force microscopy (AFM) imaged DHDMIQK(KAP) forming size-suitable nanoparticles for safe delivery in the blood circulation. In particular, AFM images showed that the nanoparticles effectively adhered onto the surfaces of the platelets. In vivo DHDMIQK(KAP) lysed the thrombus and inhibited thrombosis with a minimal effective dose of 0.01 nmol kg-1. FT-MS spectrum analyses defined a specific distribution of DHDMIQK(KAP) in the thrombus, but not in the blood and vital organs. Therefore, DHDMIQK(KAP) should be a novel nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus.
- Feng, Qiqi,Zhao, Ming,Gan, Taiping,Zhu, Haimei,Wang, Yaonan,Zhao, Shurui,Wang, Yuji,Wu, Jianhui,Peng, Shiqi
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p. 5991 - 6003
(2016/09/23)
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- Carboline-3-carboxylic acid modified related sequences of Ala-Arg-Pro-Ala-Lys, their synthesis and use as thromobolytic agent
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The present invention relates to the protected intermediates and the deprotected products of P6A, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-(2-Boc)-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid and the deprotected pseudopeptides, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid benzyl ester, related to the methods for their preparation, and related to their use as the thrombolytic agents.
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Page/Page column 11
(2010/02/11)
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- Solution-phase automated synthesis of tripeptide derivatives
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An improved general method for automated synthesis of tripeptides was developed, in which methanesulfonic acid (MSA) was used in place of trifluoroacetic acid (TFA), thus making it possible to avoid, 1) corrosion of the apparatus by strong acid vapor, 2) formation of emulsions, and 3) use of the restricted solvent, dichloromethane. As an application of the automated synthesis apparatus, 216 fragment tripeptide derivatives were synthesized systematically using the MSA method, in excellent yield and with increased efficiency.
- Kuroda,Hattori,Kitada,Sugawara
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p. 1138 - 1146
(2007/10/03)
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- Synthesis and Biological Properties of New Hexapeptide Substrates for Vitamin K Dependent Carboxylase. Evidence for X-Pro Cis/Trans Amide Bond Interconversions in Prothrombin Precursor Fragment 18-22
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Three hexapeptide analogues, corresponding to sequence 18-23 of bovine prothrombin precursor > have been synthesized and evaluated as substrates for vitamin K dependent carboxylase.These new hexapeptides are moderately good substrates for the ca
- Rich, Daniel H.,Kawai, Megumi,Goodman, Hedda L.,Suttie, John W.
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p. 910 - 916
(2007/10/02)
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