DE4003944A1 - Synthetisches polypeptid: lh - rh -- klh (konjugat aus luteinisierendem hormon-releasing hormon und dem keyhole limpet haemocyanin - Google Patents
Synthetisches polypeptid: lh - rh -- klh (konjugat aus luteinisierendem hormon-releasing hormon und dem keyhole limpet haemocyaninInfo
- Publication number
- DE4003944A1 DE4003944A1 DE19904003944 DE4003944A DE4003944A1 DE 4003944 A1 DE4003944 A1 DE 4003944A1 DE 19904003944 DE19904003944 DE 19904003944 DE 4003944 A DE4003944 A DE 4003944A DE 4003944 A1 DE4003944 A1 DE 4003944A1
- Authority
- DE
- Germany
- Prior art keywords
- hormone
- synthetic polypeptide
- keyhole limpet
- haemocy
- lhrh
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 229920001184 polypeptide Polymers 0.000 title claims abstract description 7
- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract description 7
- 102000004196 processed proteins & peptides Human genes 0.000 title claims abstract description 7
- 210000000481 breast Anatomy 0.000 title abstract description 3
- 239000005556 hormone Substances 0.000 title abstract 4
- 229940088597 hormone Drugs 0.000 title abstract 4
- 206010006187 Breast cancer Diseases 0.000 title 1
- 208000026310 Breast neoplasm Diseases 0.000 title 1
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 title 1
- 241000237988 Patellidae Species 0.000 title 1
- 102100024028 Progonadoliberin-1 Human genes 0.000 title 1
- 206010060862 Prostate cancer Diseases 0.000 title 1
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 title 1
- 201000008275 breast carcinoma Diseases 0.000 title 1
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 title 1
- 201000001514 prostate carcinoma Diseases 0.000 title 1
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 claims abstract description 14
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 claims abstract description 13
- 101000904177 Clupea pallasii Gonadoliberin-1 Proteins 0.000 claims abstract description 12
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 claims abstract description 12
- 230000015572 biosynthetic process Effects 0.000 claims abstract description 6
- 241000239218 Limulus Species 0.000 claims abstract 2
- 108010045069 keyhole-limpet hemocyanin Proteins 0.000 claims abstract 2
- 230000004071 biological effect Effects 0.000 claims description 2
- 108060003552 hemocyanin Proteins 0.000 claims 3
- 108700012941 GNRH1 Proteins 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 abstract description 4
- 238000003786 synthesis reaction Methods 0.000 abstract description 3
- 238000002560 therapeutic procedure Methods 0.000 abstract description 3
- 206010062767 Hypophysitis Diseases 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 239000000262 estrogen Substances 0.000 abstract description 2
- 230000028327 secretion Effects 0.000 abstract description 2
- 229960003604 testosterone Drugs 0.000 abstract description 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000031018 biological processes and functions Effects 0.000 abstract 1
- 230000001456 gonadotroph Effects 0.000 abstract 1
- 239000003688 hormone derivative Substances 0.000 abstract 1
- 230000008105 immune reaction Effects 0.000 abstract 1
- 230000001592 luteinising effect Effects 0.000 abstract 1
- 239000003488 releasing hormone Substances 0.000 abstract 1
- 238000012360 testing method Methods 0.000 description 2
- XQJMXPAEFMWDOZ-UHFFFAOYSA-N 3exo-benzoyloxy-tropane Natural products CN1C(C2)CCC1CC2OC(=O)C1=CC=CC=C1 XQJMXPAEFMWDOZ-UHFFFAOYSA-N 0.000 description 1
- BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 description 1
- 108010069236 Goserelin Proteins 0.000 description 1
- QQXLDOJGLXJCSE-UHFFFAOYSA-N N-methylnortropinone Natural products C1C(=O)CC2CCC1N2C QQXLDOJGLXJCSE-UHFFFAOYSA-N 0.000 description 1
- QIZDQFOVGFDBKW-DHBOJHSNSA-N Pseudotropine Natural products OC1C[C@@H]2[N+](C)[C@H](C1)CC2 QIZDQFOVGFDBKW-DHBOJHSNSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000003388 anti-hormonal effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 238000001794 hormone therapy Methods 0.000 description 1
- 238000002649 immunization Methods 0.000 description 1
- 230000003053 immunization Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000009806 oophorectomy Methods 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 210000003635 pituitary gland Anatomy 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- CYHOMWAPJJPNMW-JIGDXULJSA-N tropine Chemical compound C1[C@@H](O)C[C@H]2CC[C@@H]1N2C CYHOMWAPJJPNMW-JIGDXULJSA-N 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 229940033942 zoladex Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/59—Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g.hCG [human chorionic gonadotropin]; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/26—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against hormones ; against hormone releasing or inhibiting factors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
Description
1. Das genannte Konjugat gehört in den Bereich Impfstoffe
bzw. LH-RH-Analoga/Antagonisten.
2. Die im Haupt- und Unteranspruch genannten synthetischen
Polypeptide antagonisieren durch Induktion von Antikörpern
gegen LH-RH die biologische Wirkung des LH-RH an der
Hypophyse, in der Folge kommt es zum Sistieren der Gonado
tropinsekretion und sekundär zur Verringerung der ovariellen
Östrogenbildung bzw. Testosteronbildung in den Testes.
3. Die Anwendung ist im Humanmedizinischen Bereich in der
Therapie des Rezeptor-positiven Mamma-Ca bzw. des Prostata-
Ca gegeben, auch in der Veterinärmedizin gibt es Aspekte.
4. Die Synthese kann in einem einfachen, bekannten Verfahren
durchgeführt werden. Die beiden Grundstoffe sind auf dem
Markt erhältlich.
5. Bisheriger Stand der antihormonellen Therapie sind Analoga
des LH-RH (Zoladex®), deren Wirkung nachläßt, wenn man
sie absetzt oder die Ovarektomie. Die Immunisierung gegen
LH-RH wäre die billigste und am wenigsten belastende Therapie.
6. Die Anwendung des synthetischen Polypeptids führt über die
Synthese von größeren Mengen über die Zulassungsprüfungen des
BGA zur Ausbietung durch die Pharma-Firma.
Claims (2)
- Hauptanspruch:
Der Hauptanspruch bezieht sich auf das synthetische Polypeptid:
LH-RH-KLH (Konjugat aus Luteinisierendem Hormon releasing Hormon und dem Keyhole Limpet Hämocyanin), dadurch gekennzeichnet, daß nur das synthetische Polypeptid eine spezifische Immunreaktion (spezifische Antikörper) gegen LH-RH beim Menschen auslösen und damit die biologische Wirkung des LH-RH antagonisieren kann. - Unteranspruch:
Der Unteranspruch bezieht sich auf LH-RH-Konjugate mit in der Natur vorkommenden Hämocyaninen (z. B. Limulus-Hämocyanin) dadurch gekennzeichnet, daß auch die anderen artspezifischen Hämocyaninen eine Antikörperbildung gegen LH-RH beim Menschen auslösen können.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19904003944 DE4003944A1 (de) | 1990-02-14 | 1990-02-14 | Synthetisches polypeptid: lh - rh -- klh (konjugat aus luteinisierendem hormon-releasing hormon und dem keyhole limpet haemocyanin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19904003944 DE4003944A1 (de) | 1990-02-14 | 1990-02-14 | Synthetisches polypeptid: lh - rh -- klh (konjugat aus luteinisierendem hormon-releasing hormon und dem keyhole limpet haemocyanin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE4003944A1 true DE4003944A1 (de) | 1991-08-22 |
Family
ID=6399789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19904003944 Withdrawn DE4003944A1 (de) | 1990-02-14 | 1990-02-14 | Synthetisches polypeptid: lh - rh -- klh (konjugat aus luteinisierendem hormon-releasing hormon und dem keyhole limpet haemocyanin |
Country Status (1)
| Country | Link |
|---|---|
| DE (1) | DE4003944A1 (de) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993002706A1 (en) * | 1991-07-26 | 1993-02-18 | Commonwealth Scientific And Industrial Research Organisation | Self-adjuvanting peptide vaccine delivery system and production thereof |
| US6132720A (en) * | 1994-01-27 | 2000-10-17 | Aphton Corp. | Immunogens against gonadotropin releasing hormone |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988000056A1 (en) * | 1986-07-03 | 1988-01-14 | The State Of Victoria | Composition and method for immunological castration and spaying |
-
1990
- 1990-02-14 DE DE19904003944 patent/DE4003944A1/de not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988000056A1 (en) * | 1986-07-03 | 1988-01-14 | The State Of Victoria | Composition and method for immunological castration and spaying |
Non-Patent Citations (3)
| Title |
|---|
| US-Zeitschriften: Chemical Abstracts: Vol. 96, 1982, Ref. Nr. 50332n * |
| Vol. 89, Ref. Nr. 51031, Biosis * |
| Vol.110, 1989, Ref. Nr. 121166g * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993002706A1 (en) * | 1991-07-26 | 1993-02-18 | Commonwealth Scientific And Industrial Research Organisation | Self-adjuvanting peptide vaccine delivery system and production thereof |
| US5955080A (en) * | 1991-07-26 | 1999-09-21 | Commonwealth Scientific And Industrial Research Organisation | Self-adjuvanting peptide vaccine delivery system and production thereof |
| US6132720A (en) * | 1994-01-27 | 2000-10-17 | Aphton Corp. | Immunogens against gonadotropin releasing hormone |
| US6303123B1 (en) | 1994-01-27 | 2001-10-16 | Aphton Corporation | Methods for the treatment of hormone-dependent tumors with immunogens against gonadotropin releasing hormone |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| OM8 | Search report available as to paragraph 43 lit. 1 sentence 1 patent law | ||
| 8141 | Disposal/no request for examination |