CN1826353A - 新的黑皮质素受体模板、肽及其用途 - Google Patents
新的黑皮质素受体模板、肽及其用途 Download PDFInfo
- Publication number
- CN1826353A CN1826353A CNA2004800211952A CN200480021195A CN1826353A CN 1826353 A CN1826353 A CN 1826353A CN A2004800211952 A CNA2004800211952 A CN A2004800211952A CN 200480021195 A CN200480021195 A CN 200480021195A CN 1826353 A CN1826353 A CN 1826353A
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- CN
- China
- Prior art keywords
- phe
- peptide
- arg
- sequence
- dphe
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- 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
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
- C07K14/68—Melanocyte-stimulating hormone [MSH]
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Toxicology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Description
化合物 | EC50(nM) | |||
mMC1R | mMC3R | mMC4R | mMC5R | |
hAGRP(109-118) | 5,120±3,040 | >100,000 | pA2=6.8±0.24 | >100,000 |
α-MSH | 0.55±0.09 | 0.79±0.14 | 5.37±0.62 | 0.44±0.09 |
NDP-MSH | 0.038±0.012 | 0.098±0.013 | 0.21±0.03 | 0.071±0.012 |
MTII | 0.020±0.003 | 0.16±0.03 | 0.087±0.008 | 0.16±0.03 |
SEQ ID NO:1 | 61.3±17.9 | 轻微激动剂>100,000 | 部分激动剂pA2=6.1±0.2 | 238.7±100 |
SEQ ID NO:2 | >100,000 | >100,000 | >100,000 | >100,000 |
化合物 | EC50(nM) | |||
mMC1R | mMC3R | mMC4R | mMC5R | |
SEQ ID NO:3 | 1,730±310 | pA2=5.7±0.2 | pA2=5.9±0.2 | >100,000 |
SEQ ID NO:4 | 13,500±3,100 | >100,000 | 部分激动剂15,900±7,300 | >100,000 |
SEQ ID NO:5 | 6,120±2,300 | 轻微激动剂 | 10,900±2,900 | 2,220±1,100 |
SEQ ID NO:6 | 19,700±4,300 | 轻微激动剂 | 13,400±400 | 3,900±1,800 |
SEQ ID NO:7 | 4,850±1,450 | 轻微激动剂 | 450±160 | 124±25 |
SEQ ID NO:8 | 13,300±1,700 | 轻微激动剂 | >100,000 | 100,000 |
SEQ ID NO:9 | 59.5±16.7 | 309±120 | 57.1±4.4 | 90.0±22.0 |
SEQ ID NO:10 | 0.21±0.09 | 0.99±0.34 | 0.18±0.04 | 0.55±0.14 |
SEQ ID NO:11 | 1,960±500 | pA2=6.2±0.3 | pA2=6.2±0.1 | >100,000 |
SEQ ID NO:12 | >100,000 | >100,000 | >100,000 | >100,000 |
SEQ ID NO:13 | 部分激动剂19,900±5,100 | >100,000 | >100,000 | >100,000 |
SEQ ID NO:14 | 部分激动剂7,220±2,200 | 部分激动剂20,500±6,800 | >100,000 | 部分激动剂24,400±6,700 |
SEQ ID NO:15 | 59.9±8.1 | 480±49 | 930±120 | 327±118 |
SEQ ID NO:16 | 轻微激动剂 | >100,000 | >100,000 | 轻微激动剂 |
SEQ ID NO:17 | 7.28±0.76 | 6,210±990 | 轻微激动剂 | 450±110 |
SEQ ID NO:18 | 3,630±320 | >100,000 | >100,000 | 轻微激动剂 |
SEQ ID NO:19 | >100,000 | >100,000 | >100,000 | >100,000 |
SEQ ID NO:20 | 部分激动剂38,300±8,700 | >100,000 | >100,000 | >100,000 |
SEQ ID NO:21 | >100,000 | >100,000 | >100,000 | >100,000 |
SEQ ID NO:22 | 440±49 | 14,400±3,700 | 5,000±900 | 3,600±200 |
SEQ ID NO:23 | 2,630±830 | 轻微激动剂 | >100,000 | 轻微激动剂 |
SEQ ID NO:24 | 7.20±2.89 | 29.0±7.5 | 0.36±0.07 | 0.46±0.18 |
SEQ ID NO:25 | 14000±1700 | 部分激动剂30300±1400 | 14700±1000 | 690±98 |
SEQ ID NO:26 | 66.5±26.8 | 23800±18900 | 32.5±16.7 | 2.06±0.67 |
SEQ ID NO:27 | 350±160 | 13500±3700 | 710±170 | 50.1±9.6 |
SEQ ID NO:28 | 22.1±18 | 部分激动剂pA2=7.2±0.2 | 0.63±0.20 | 7.16±0.22 |
SEQ ID NO:29 | 6.04±1.36 | 部分激动剂pA2=7.2±0.6 | 0.64±0.17 | 3.15±1.38 |
SEQ ID NO:30 | 690±150 | pA2=6.4±0.2 | 115±26 | 440±230 |
SEQ ID NO:31 | 10300±3200 | 13200±3400 | 16700±1300 | 7900±4000 |
SEQ ID NO:32 | 0.30±0.05 | pA2=8.9±0.1 | 部分激动剂pA2=9.4±0.4 | 2.33±0.96 |
SEQ ID NO:33 | 5.56±3.40 | pA2=8.3±0.2 | 部分激动剂pA2=9.3±0.1 | 22.3±10.6 |
SEQ ID NO:34 | 9.20±0.97 | 320±250 | 0.57±0.08 | 3.13±1.89 |
化合物 | EC50(nM) | |||
mMC1R | mMC3R | mMC4R | mMC5R | |
SEQ ID NO:35 | 3.87±0.85 | 33.0±21.3 | 0.57±0.07 | 5.27±2.12 |
SEQ ID NO:36 | 990±290 | 17300±290 | 4300±1900 | 3200±2400 |
SEQ ID NO:37 | 680±82 | 30800±4200 | 8600±2200 | 800±120 |
SEQ ID NO:38 | 1000±170 | 39200±13200 | 7200±1800 | 700±110 |
SEQ ID NO:39 | 0.53±0.13 | 5.56±2.72 | 0.27±0.12 | 1.93±1.10 |
SEQ ID NO:40 | 0.20±0.05 | 6.50±1.87 | 0.67±0.25 | 0.95±0.40 |
SEQ ID NO:41 | 11.6±3.5 | 450±130 | 42.6±9.7 | 3.43±0.90 |
SEQ ID NO:42 | 21.6±10.3 | 3400±1200 | 260±99 | 42.7±10.0 |
SEQ ID NO:43 | 2.61±0.14 | 14.0±1.8 | 0.66±0.20 | 4.87±2.29 |
Claims (27)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10/602,394 | 2003-06-23 | ||
US10/602,394 US7084111B2 (en) | 2003-06-23 | 2003-06-23 | Melanocortin receptor templates, peptides, and use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1826353A true CN1826353A (zh) | 2006-08-30 |
CN100497373C CN100497373C (zh) | 2009-06-10 |
Family
ID=33518084
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2004800211952A Expired - Fee Related CN100497373C (zh) | 2003-06-23 | 2004-06-22 | 新的黑皮质素受体模板、肽及其用途 |
Country Status (5)
Country | Link |
---|---|
US (4) | US7084111B2 (zh) |
JP (1) | JP2007537976A (zh) |
CN (1) | CN100497373C (zh) |
CA (1) | CA2530027A1 (zh) |
WO (1) | WO2005000877A2 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106536542A (zh) * | 2014-05-13 | 2017-03-22 | 凯尔格恩有限公司 | 具有改善色素减退及抑制脂肪形成的功效的肽及其的用途 |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7910101B2 (en) | 2004-10-25 | 2011-03-22 | Centocor, Inc. | Melanocortin receptor binding mimetibodies, compositions, methods and uses |
PT2236151E (pt) | 2005-07-08 | 2012-07-02 | Ipsen Pharma | Ligandos do receptor de melanocortina |
EP1915168A4 (en) | 2005-07-08 | 2010-03-31 | Ipsen Pharma | LIGANDS OF MELANOCORTIN RECEPTORS |
WO2007123839A2 (en) * | 2006-04-18 | 2007-11-01 | University Of Florida Research Foundation, Inc. | Peptides with efficacy in rescuing melanocortin-4 receptor polymorphic agonist signaling |
NZ590254A (en) | 2008-06-09 | 2012-07-27 | Palatin Technologies Inc | Melanocortin receptor-specific cyclic peptides for treatment of sexual dysfunction |
TW201002340A (en) * | 2008-06-09 | 2010-01-16 | Palatin Technologies Inc | Melanocortin receptor-specific peptides for treatment of obesity |
EP2440572B1 (en) | 2009-06-08 | 2017-04-05 | Palatin Technologies, Inc. | Lactam-bridged melanocortin receptor-specific peptides |
UY32690A (es) | 2009-06-08 | 2011-01-31 | Astrazeneca Ab | Péptidos específicos para receptores de melanocortina |
JP5805632B2 (ja) | 2009-06-08 | 2015-11-04 | パラティン テクノロジーズ, インコーポレイテッドPalatin Technologies, Inc. | メラノコルチン受容体に特異的なペプチド |
GB0918579D0 (en) * | 2009-10-22 | 2009-12-09 | Imp Innovations Ltd | Gadd45beta targeting agents |
EA201290295A1 (ru) * | 2009-11-23 | 2013-01-30 | Палатин Текнолоджиз, Инк. | Специфичные к рецептору меланокортина-1 линейные пептиды |
BR112012011787B1 (pt) | 2009-11-23 | 2022-03-03 | Palatin Technologies, Inc | Peptídeo cíclico e composição farmacêutica |
US9441013B2 (en) | 2011-05-17 | 2016-09-13 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Melanocortin 1 receptor ligands and methods of use |
US9290539B2 (en) | 2011-05-17 | 2016-03-22 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Melanotropin ligands for skin care |
US9402877B2 (en) * | 2011-11-04 | 2016-08-02 | Xion Pharmaceuticals Corporation | Methods and compositions for oral administration of melanocortin receptor agonist compounds |
US9499586B2 (en) * | 2012-10-16 | 2016-11-22 | Hong Kong Baptist University | Anticancer and anti-obesity cyclic peptide agents |
KR101632948B1 (ko) * | 2014-05-13 | 2016-06-27 | (주)케어젠 | 항염증, 골 형성 및 발모 촉진 활성을 갖는 펩타이드 및 이의 용도 |
US9814755B2 (en) | 2014-06-10 | 2017-11-14 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Methods for the treatment of depression and anxiety |
US9821023B2 (en) | 2014-06-10 | 2017-11-21 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Methods for the treatment of central nervous system (CNS) disorders and mood disorders |
US20170022252A1 (en) | 2014-06-10 | 2017-01-26 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Novel modulators of melanocortin receptors |
US10550157B2 (en) | 2015-10-16 | 2020-02-04 | Arizona Board Of Regent On Behalf Of The University Of Arizona | Compositions and methods for treating central nervous system (CNS) disorders and mood disorders |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6350430B1 (en) | 1997-10-27 | 2002-02-26 | Lion Bioscience Science Ag | Melanocortin receptor ligands and methods of using same |
GB9808229D0 (en) | 1998-04-17 | 1998-06-17 | Quadrant Holdings Cambridge | Melanocortin receptor ligands |
WO1999055679A1 (en) | 1998-04-28 | 1999-11-04 | Trega Biosciences, Inc. | Isoquinoline compound melanocortin receptor ligands and methods of using same |
EP1125579A3 (en) | 2000-01-18 | 2003-01-02 | Pfizer Products Inc. | Uses of agrp-melanocortin receptor binding modulating compounds |
US6600015B2 (en) | 2000-04-04 | 2003-07-29 | Hoffmann-La Roche Inc. | Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity |
ES2280393T3 (es) | 2000-08-30 | 2007-09-16 | F. Hoffmann-La Roche Ag | Peptidos ciclicos que tienen actividad agonista para el receptor de melanocortin-4. |
IL159797A0 (en) | 2001-07-11 | 2004-06-20 | Palatin Technologies Inc | Linear and cyclic melanocortin receptor-specific peptides |
-
2003
- 2003-06-23 US US10/602,394 patent/US7084111B2/en not_active Expired - Fee Related
-
2004
- 2004-06-22 CA CA002530027A patent/CA2530027A1/en not_active Abandoned
- 2004-06-22 JP JP2006517632A patent/JP2007537976A/ja not_active Withdrawn
- 2004-06-22 CN CNB2004800211952A patent/CN100497373C/zh not_active Expired - Fee Related
- 2004-06-22 WO PCT/US2004/020329 patent/WO2005000877A2/en active Application Filing
-
2006
- 2006-07-24 US US11/491,596 patent/US7582610B2/en not_active Expired - Fee Related
-
2008
- 2008-01-08 US US11/970,708 patent/US20080146496A1/en not_active Abandoned
- 2008-01-08 US US11/970,722 patent/US20080146779A1/en not_active Abandoned
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106536542A (zh) * | 2014-05-13 | 2017-03-22 | 凯尔格恩有限公司 | 具有改善色素减退及抑制脂肪形成的功效的肽及其的用途 |
CN106536542B (zh) * | 2014-05-13 | 2019-07-30 | 凯尔格恩有限公司 | 具有改善色素减退及抑制脂肪形成的功效的肽及其的用途 |
Also Published As
Publication number | Publication date |
---|---|
US7582610B2 (en) | 2009-09-01 |
US20080146496A1 (en) | 2008-06-19 |
JP2007537976A (ja) | 2007-12-27 |
US20060258590A1 (en) | 2006-11-16 |
US7084111B2 (en) | 2006-08-01 |
US20080146779A1 (en) | 2008-06-19 |
US20040260063A1 (en) | 2004-12-23 |
WO2005000877A3 (en) | 2005-08-11 |
CN100497373C (zh) | 2009-06-10 |
CA2530027A1 (en) | 2005-01-06 |
WO2005000877A2 (en) | 2005-01-06 |
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