摘要:
A catalytically active peptide comprising an imidazole function in position i flanked by at least one functional group to be amidated in position i+3+4k, where k is an integer equal to or higher than -1 or in position i-4-4n, wherein n is an integer equal to or higher than 0, characterized in that it also comprises at least one activating group in position i+4+4n or i-3-4n, respectively, wherein n is as above.
摘要:
The invention is directed to methods and compositions for aqueous-compatible solid phase chemical ligation. The methods and compositions of the invention involve the chemical ligation of first and second polymers, where the first polymer is attached to a support through a displaceable linker. The displaceable linker can be cleaved or otherwise displaced under aqueous conditions compatible with subsequent removal of the ligation product from the solid support. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides on a solid support. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate ligated polymers including peptides, polypeptides and other amino acid containing polymers.
摘要:
The invention is directed to methods and compositions for aqueous-compatible solid phase chemical ligation. The methods and compositions of the invention involve the chemical ligation of first and second polymers, where the first polymer is attached to a support through a displaceable linker. The displaceable linker can be cleaved or otherwise displaced under aqueous conditions compatible with subsequent removal of the ligation product from the solid support. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides on a solid support. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate ligated polymers including peptides, polypeptides and other amino acid containing polymers.
摘要:
The invention concerns a multiplex polymer ligation method involving water-soluble polymeric protecting groups, compositions and methods of use. The method involves synthesis of a first compound bearing one or more water-soluble polymeric protecting groups followed by replacing one or more of the water-soluble protecting groups with a chemical adduct of interest. Multiple different compounds derived from the first compound can be readily prepared by splitting the first compound into first and second reaction systems, followed by replacing one or more of the water-soluble polymeric protecting groups of the first reaction system with a first chemical adduct, and replacing one or more of the water-soluble polymeric protecting groups of the second reaction system with a second chemical adduct of interest, where the first and second chemical adducts are different. Also provided are kits useful for carrying out the multiplex polymer ligation methods of the invention.
摘要:
Disclosed are novel polypeptides consisting of a four helix bundle formed of two dimerized helix-loop-helix motifs, wherein either both have a sequence according to SEQ. ID. No. 1, SEQ. ID. No. 2, SEQ. ID. No. 3, SEQ. ID. No. 4, SEQ. ID. No. 5 or SEQ. ID. No. 7, or one has a sequences according to SEQ. ID. No. 6, and the other one has a sequence according to SEQ. ID. No. 1, SEQ. ID. No. 2, SEQ. ID. No. 3, SEQ. ID. No. 4, SEQ. ID. No. 5 or SEQ. ID. No. 7. Also disclosed is a method for site-selective acylation of a folded polypeptide or protein based on the use of a four helix bundle formed of two dimerized helix-loop-helix motifs folded in an antiparallel mode, said helix-loop-helix motifs comprising amino acid residues in a heptad repeat pattern a b c d e fgn, wherein all but 1-3 of said amino acid residues in positions a and d are non-polar and wherein said 1-3 amino acid residues in positions a and d that are non-polar, are selected from the group consisting of lysine, ornithine, diaminobutyric acid and homolysine, wherein said amino acid residues in positions a and d form a hydrophobic core, wherein the polypeptide and/or protein to be acylated is placed in an aqueous solution and an acylation agent is added. Furthermore, use of said method is disclosed.
摘要:
Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.
摘要:
Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.
摘要:
A catalytically active peptide comprising an imidazole function in position i flanked by at least one functional group to be amidated in position i+3+4k, where k is an integer equal to or higher than -1 or in position i-4-4n, wherein n is an integer equal to or higher than 0, characterized in that it also comprises at least one activating group in position i+4+4n or i-3-4n, respectively, wherein n is as above.
摘要:
Highly repetitive proteins which are relatively insoluble in water are chemically modified to increase solubility. The protein is reacted with a functionalizing agent to introduce additional polar functionalities and disrupt the order of the protein. The solubility of the protein in water is increased by the chemical modification, while adhesive and surfactant properties are retained.
摘要:
Protéine basique isolée de venin de serpent de la famille des Elapidés notamment d'un serpent Naja et plus particulièrement de Naja nigricollis et/ou de Naja mossambica pallida, dénommée phospholipase A2 (PLA2), fragments et dérivés de ladite protéine, leurs procédés d'obtention, des compositions pharmaceutiques utilisables en médecine humaine et/ou vétérinaire, ainsi que des agents de diagnostic contenant ladite protéine et/ou ses dérivés et/ou ses fragments. Ladite protéine comprend 118 amino-acides, son poids moleculaire est de l'ordre de 13 300 Daltons et son point isoélectrique est de l'ordre de 8,6. Les dérivés de ladite protéine sont modifiés au niveau de l'une des histidines par fixation d'un groupe alkyle de formule R-CH₂-X. Application à la détection de cellules tumorales.