WO1997002340A3 - Methods for inhibiting factor xiii activity - Google Patents
Methods for inhibiting factor xiii activity Download PDFInfo
- Publication number
- WO1997002340A3 WO1997002340A3 PCT/US1996/011182 US9611182W WO9702340A3 WO 1997002340 A3 WO1997002340 A3 WO 1997002340A3 US 9611182 W US9611182 W US 9611182W WO 9702340 A3 WO9702340 A3 WO 9702340A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- factor xiii
- approach
- designed
- methods
- designed based
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/1025—Acyltransferases (2.3)
- C12N9/104—Aminoacyltransferases (2.3.2)
- C12N9/1044—Protein-glutamine gamma-glutamyltransferase (2.3.2.13), i.e. transglutaminase or factor XIII
Abstract
Methods for inhibiting Factor XIII activity feature a ligand that forms at least one contact, at a distance of about 5 Å or less, with at least one amino acid residue of a Factor XIII monomer. Factor XIII inhibitors are selected or designed using the three-dimensional structure of Factor XIII as a guide. In one approach, inhibitory ligands are selected or designed based on the Factor XIII b-sandwich:core interface. In a second approach, inhibitors are selected or designed based on the catalytic site of Factor XIII. In a third approach, inhibitory ligands are selected or designed based on the Factor XIII dimer interface. In a fourth approach, inhibitory molecules were designed to occupy the Factor XIII binding site, and include an electrophilic moiety susceptible to nucleophilic displacement by the reactive Cys-314.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73095P | 1995-06-30 | 1995-06-30 | |
| US60/000,730 | 1995-06-30 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO1997002340A2 WO1997002340A2 (en) | 1997-01-23 |
| WO1997002340A3 true WO1997002340A3 (en) | 1997-03-06 |
Family
ID=21692769
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1996/011182 WO1997002340A2 (en) | 1995-06-30 | 1996-06-28 | Methods for inhibiting factor xiii activity |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO1997002340A2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2949782B1 (en) * | 2009-09-04 | 2015-10-16 | Isp Investments Inc | TRANSGLUTAMINASE ACTIVATOR PEPTIDE AND COSMETIC OR PHARMACEUTICAL COMPOSITION CONTAINING SAME. |
-
1996
- 1996-06-28 WO PCT/US1996/011182 patent/WO1997002340A2/en active Application Filing
Non-Patent Citations (6)
| Title |
|---|
| A A NAGY ET AL.: "Inhibition of the fibrin stabilizing factor by amino acid and peptide derivatives", PEPTIDES 1990. PROCEEDINGS OF THE XXI EUROPEAN PEPTIDE SYMPOSIUM, SEPTEMBER 2-8, 1990, PLATJA D'ARO, SPAIN, 1991, ESCOM, LEIDEN, pages 777 - 778, XP002023122 * |
| BIOCH. SOC. TRANS., vol. 18, no. 6, 1990, pages 1318 - 1320 * |
| CHEMICAL ABSTRACTS, vol. 113, no. 21, 19 November 1990, Columbus, Ohio, US; abstract no. 187093z, P M DOYLE ET AL.: "peptides incorporating electrophilic glutamine analogs as potential transglutaminase inhibitors" page 308; XP002023124 * |
| D LUKACOVA ET AL.: "Inhibition of Factor XIII activation by an anti-peptide monoclonal antibody", BIOCHEMISTRY, vol. 30, no. 42, 22 November 1991 (1991-11-22), EASTON, PA US, pages 10164 - 10170, XP000229792 * |
| J J GROOTJANS ET AL.: "Substrate requirements for transglutaminases", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 270, no. 39, 29 September 1995 (1995-09-29), MD US, pages 22855 - 22858, XP002023123 * |
| K E ACHYUTHAN ET AL.: "Factor XIIIa-derived peptides inhibit transglutaminase activity", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 268, no. 28, 5 October 1993 (1993-10-05), MD US, pages 21284 - 21292, XP000568750 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO1997002340A2 (en) | 1997-01-23 |
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