Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds -> Monitor Keywords

Site News |

Monitor Keywords |

Monitor Archive |

Organizer |

Account Info |

05/11/06 - USPTO Class 514 | 104 views | #20060100130 | Prev - Next | About this Page

Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds

Title: Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20060100130, Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds.

1. The use of a compound as inhibitor of a secondary amide peptide bond-specific cis/trans isomerase (APIase) which assumes the structure and conformation of a peptide motif R.sub.2--R.sub.3 if it is bound as a substrate to the active centre of this isomerase, wherein R.sub.2 comprises all natural amino acids and R.sub.3 comprises the amino acids methionine, alanine, serine, glutamic acid, leucine, lysine, isoleucine and/or glycine or their mimetics.

2. The use according to claim 1, wherein the residues flanking the peptide motif are characterised on the one side by hydrophobic properties and on the other side by hydrophobic or positively charged residues, wherein these flanking residues are in contact with the active centre of the isomerase.

3. The use according to claim 1, wherein the compound is a peptide, an oligopeptide or a peptide mimetic.

4. The use according to claim 3 with an inhibition constant of 100 micro molar or less.

5. The use according to claim 2, wherein the peptide, oligopeptide or peptide mimetic can be linear or cyclic.

6. The use according to claim 1, wherein the inhibitor represents a peptide and/or a peptide mimetic with the basic structure X.sub.a--R.sub.2--R.sub.3X.sub.b, wherein X comprises any L-amino or D-amino acid, R.sub.2 comprises any L-amino acid or mimetics thereof and R.sub.3 comprises the following amino acids: methionine, alanine, serine, glutamic acid, leucine, lysine, isoleucine and glycine or mimetics thereof and wherein a and b represent the number of flanking amino acids and are selected so that, while maintaining the structure R.sub.2--R.sub.3, the length of the peptide is larger than 2 amino acids or the corresponding amino acid mimetics and shorter than 10 amino acids or the corresponding amino acid mimetics.

7. The use according to claim 6, wherein the compound has a molecular weight of 200 to a maximum of 2,000.

8. The use according to claim 6, wherein single amino acids or mimetics thereof have a molecular weight of not less than 75 and of not more than 500 and are combined in such a way that either only each of the terminal residues Xa, Xb individually or both of them or at least one of the neighbouring R2-R3 amino acids or amino acid mimetics or several of the neighbouring R2-R3 amino acids or amino acid mimetics have a hydrophilic functional group either formed by --OH, --SH, --NH, or NH.sub.2 or by acid groups such as phosphatyl, sulfatyl or carboxyl.

9. A peptide or peptide mimetic with the general basic structure Y--R.sub.2--R.sub.3 wherein Y is a saturated or unsaturated, linear or branched chain fatty acid which is linked to the amino acid or the amino acid mimetic R.sub.2 by a C(O)NH bond and wherein the amino acid or the amino acid mimetic R.sub.3, via its amino group, is linked to R.sub.2 by a C(O)NH bond, wherein R.sub.2 and R.sub.3 have the meanings as indicated above.

10. The compounds according to claim 6, wherein the peptide mimetic R.sub.3 consists of at least 5 and not more than 29 atoms and has to be able to form a chemical bond with R2 which corresponds to the structure of a peptide bond, wherein the basic structure of R3 is described as H.sub.2N--R-Z, wherein Z represents a functional group selected from nitro, sulfoxy, phospho, amino, carboxy, sulfhydryl, wherein R represents a linear or branched hydrocarbon chain, whose length is a maximum of 14 carbon atoms and a minimum of 1 carbon atom, wherein the distance between H.sub.2N---Z via R is a maximum of 4 carbon atoms and a minimum of 1 carbon atom, wherein R itself can optionally have one or up to three hydroxyl, carboxylic acid, carboxylic acid ester, amide, aldehyde, ether, iminoether, hydrazide, izidoether, thiol or sulfoxime groups.

11. The compound according to claim 9, wherein the fatty acid has 8 to 24 carbon atoms.

12. The compound according to claim 9, wherein the fatty acid has 14 to 16 carbon atoms.

13. The compound according to claim 9, wherein the fatty acid is mono-hydroxylated.

14. The compound according to claim 9, wherein the fatty acid is poly-hydroxylated.

15. The embodiment according to claim 6, wherein the amino acid mimetics R2 and R3 are the same or different and have up to 34 carbon atoms and a linear structure, which can optionally be branched, a C5- to C34-carbycyclic structure or a heterocyclic structure, containing S, N and O as hetero atoms and having ring sizes of 5 to 8, wherein these structures can be completely saturated or can have mono- or poly-unsaturated carbon moieties.

16. The embodiment according to claim 15, wherein R2 and R3 include benzoic or non-benzoic aromatic compounds which can optionally be mono- or poly-substituted with functional groups selected from nitro, sulfoxy, phospho, amino, carboxy, sulflhydryl groups.

17. The embodiment according to claim 15, wherein R2 and R3 are mono- or poly-halogenated, wherein halogen is selected from fluoro, chloro, bromine or iodine.

18. The compound according to claim 9, wherein Y is a saturated fatty acid.

19. The compound according to claim 9, wherein Y is an unsaturated fatty acid.

20. The compound according to claim 18, wherein the saturated fatty acid is selected from: propionic acid, butyric acid, iso butyric acid, valeric acid, iso-valeric acid, caproic acid, enanthic acid, caprylic acid, pelargonic acid, capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, stearic acid, nonadecanoic acid, iso tuberculostearic acid, arachic acid, behenic acid, lignoceric acid, cerotic acid and melissic acid.

21. The compound according to claim 19, wherein the unsaturated fatty acid is selected from: acrylic acid, crotonic acid, palmitoleic acid, oleic acid, erucic acid, sorbic acid, elaeosteric acid, arachidonic acid, clupanodonic acid, docosahexaenoic acid, elaidic acid, linolic acid and linolenic acid.

22. The embodiment according to claim 6, wherein R2 and R3 together represent a peptide mimetic.

23. The compound according to claim 9, with the formula:

24. The embodiment according to claim 6, wherein the inhibitor has an inhibition constant of 100 micro molar or less.

25. Mixtures comprising an inhibitor according to claim 1 and optionally a pharmaceutical acceptable carrier.

26. A method for inhibiting cell growth by inhibiting a APIase activity by contacting the corresponding cells with an effective amount of an inhibitor according to claim 1.

27. A method for inhibiting the formation of incorrectly folded proteins, wherein the specific APIase which catalyses this folding is inhibited with an effective amount of an inhibitor according to claim 1.

28. The method according to claim 26, wherein the specific APIase is DnaK.

29. The use of an inhibitor according to claim 1 for the preparation of a pharmaceutical composition for inhibiting APIase.

30. The use of claim 29, wherein the APIase is DnaK.

31. The use according to claim 29 for inhibiting the cell growth of hyperplastic or neoplastic disease processes.

32. The method according to claim 26, wherein the cells are eukaryotic cells.

33. The method according to claim 26, wherein the cells are selected from the following group: mammalian cells, yeast cells, fungal cells.

34. The method according to claim 27, wherein the incorrect folding of proteins leads to diseases.

35. A method for identifying an inhibitor of a secondary amide peptide bond-specific cis/trans isomerase (APIase) comprising the following steps: a. preparing a library of compounds with the sequence X.sub.1X.sub.2X.sub.3R3-R4X.sub.4X.sub.5X.sub.6, wherein in each peptide X represents an amino acid; b. adding an APIase of choice to the library indicated under a) for a corresponding time and under such conditions which are sufficient for binding the APIase to peptides; c. determining the amino acid sequence of the peptide bound to the APIase; d. synthesizing the peptide found under c; and e. determining the inhibitor constant of the peptide, wherein an inhibition constant of 100 micro molar or less shows an inhibitor of this APIase.

36. A method for locating an inhibitor of a secondary amide peptide bond-specific cis/trans isomerase (APIase) comprising the following steps: a. preparing a secondary amide peptide bond-specific cis/trans isomerase (APIase), b. mixing the APIase with: i. a possible inhibitor molecule and ii. a specific APIase substrate of this enzyme in order to iii. obtain a mixture of APIase, possible inhibitor molecule and substrate, c. incubating this mixture under conditions which are necessary for the APIase to catalyse the cis/trans isomerisation of the substrate; and d. determining the inhibitor constant of the peptide, wherein a Ki of 100 micro molar or less shows an inhibitor of this APIase.

Brief Patent Description - Full Patent Description - Patent Claims

Click on the above for other options relating to this Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds patent application.
###

How KEYWORD MONITOR works... a FREE service from FreshPatents
1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored.
3. Each week you receive an email with patent applications related to your keywords.
Start now! - Receive info on patent apps like Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds or other areas of interest.
###

Previous Patent Application:
Foam control agents for water-based printing inks and coatings
Next Patent Application:
Compositions and methods for modifying toxic effects of proteinaceous compounds
Industry Class:
Drug, bio-affecting and body treating compositions

###

Design/code © 2009 FreshContext LLC/Freshpatents.com. Website Terms and Conditions - Also read: About this Page
Patent data source: patents published by the United States Patent and Trademark Office (USPTO)
Information published here is for research/educational purposes only (and in conjunction with our Keyword Monitor) and is not meant to be used in place of the full USPTO patent document/images or a comprehensive patent archive search. Complete official applications are on file at the USPTO and often contain additional data/images (Freshpatents is currently text-only). FreshPatents.com is not affiliated with or endorsed by the USPTO or firms/individuals or products/designs/ideas related to listed patents.

FreshPatents.com Support
Thank you for viewing the Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds patent info.
IP-related news and info

Results in 0.09869 seconds

Other interesting Feshpatents.com categories:
Accenture , Agouron Pharmaceuticals , Amgen , AT&T , Bausch & Lomb , Callaway Golf 174

* Protect your Inventions
* US Patent Office filing

Provisional Patent
Utility Patent

PATENT INFO