- Rapid, effective deprotection of tert-butoxycarbonyl (Boc) amino acids and peptides at high temperatures using a thermally stable ionic liquid
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A method for high temperature Boc deprotection of amino acids and peptides in a phosphonium ionic liquid is described. The ionic liquid had low viscosity, high thermal stability and demonstrated a beneficial effect. The study extended the possibility for extraction of water soluble polar organic molecules using ionic liquids. Trace water significantly improved product purity and yield, while only 2 equiv. TFA led to deprotection within 10 min. The trityl group was also deprotected.
- Bhawal, Sumit S.,Patil, Rahul A.,Armstrong, Daniel W.
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p. 95854 - 95856
(2015/11/24)
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- Synthesis of dendritic oligo(aryl sulfone)s as supports for synthesis
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A short, divergent route to G1 oligo(aryl sulfone)s and a G 2 oligo(aryl sulfone) dendrimer using nucleophilic aromatic substitution reactions is described. A range of tetrasubstituted pentasulfones are proposed for applications as homogeneous supports for synthesis. Key to achieving selectivity in the syntheses is the activation of leaving groups by sulfide to sulfone oxidation. Preparation of the G2 oligo(aryl sulfone) is low-yielding due to competition from SET processes that are interesting from a mechanistic point of view. The utility of the supports is exemplified with a four step synthesis of a dipeptide and by 'react and release' synthesis of amides.
- Taylor, Paul C.,Wall, Michael D.,Woodward, Peter R.
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p. 12314 - 12322
(2007/10/03)
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- Cancerous metastasis inhibitor
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A chimeric protein wherein HI-8 which is the C-terminal domain of human urinary trypsin inhibitor (UTI) having a cancer cell metastasis inhibitory effect, is linked to a peptide containing the G domain of urokinase binding specifically to urokinase receptor expressed in a large amount in cancer cells.
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- Polypeptide, DNA fragment encoding the same, drug composition containing the same and process for producing the same
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This invention particularly provides a novel polypeptide having high protease-inhibiting activity, preferably FXa-inhibiting activity, which comprises, at least as a part of the polypeptide, an amino acid sequence resulting from substitution of an amino acid for at least one amino acid in the following amino acid sequence (1), wherein the amino acid substitution is at least one substitution selected from the following substitution means (i) to (iii). It also provides a process for the production of the polypeptide, a novel DNA fragment encoding the polypeptide and a drug composition containing the same. Amino acid sequence (1) STR1 (i) Substitution of 15 position Gln counting from the N-terminus by an amino acid other than Gln. (ii) Substitution of 42 position Tyr counting from the N-terminus by an amino acid other than Tyr. (iii) Substitution of 7 position Arg counting from the N-terminus by an amino acid other than Arg.
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- Polypeptide, DNA fragment encoding the same, drug composition containing the same and process for producing the same
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This invention particularly provides a novel polypeptide having high protease-inhibiting activity, preferably FXa-inhibiting activity, which comprises, at least as a part of the polypeptide, an amino acid sequence resulting from substitution of an amino acid for at least one amino acid in the following amino acid sequence (1), wherein the amino acid substitution is at least one substitution selected from the following substitution means (i) to (iii). It also provides a process for the production of the polypeptide, a novel DNA fragment encoding the polypeptide and a drug composition containing the same. ______________________________________Amino acid sequence (1)______________________________________Cys Asn Leu Pro Ile Val Arg Gly Pro CysArg Ala Phe Ile Gln Leu Trp Ala Phe AspAla Val Lys Gly Lys Cys Val Leu Phe ProTyr Gly Gly Cys Gln Gly Asn Gly Asn LysPhe Tyr Ser Glu Lys Glu Cys Arg Glu TyrCys______________________________________ (i) Substitution of 15 position Gln counting from the N-terminus by an amino acid other than Gln. (ii) Substitution of 42 position Tyr counting from the N-terminus by an amino acid other than Tyr. (iii) Substitution of 7 position Arg counting from the N-terminus by an amino acid other than Arg.
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