KR100508616B1 - 염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 - Google Patents
염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 Download PDFInfo
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- KR100508616B1 KR100508616B1 KR10-2003-0040018A KR20030040018A KR100508616B1 KR 100508616 B1 KR100508616 B1 KR 100508616B1 KR 20030040018 A KR20030040018 A KR 20030040018A KR 100508616 B1 KR100508616 B1 KR 100508616B1
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- chain
- insulin
- amino acid
- activity
- arginine
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- 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
- C07K14/62—Insulins
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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
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
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- Proteomics, Peptides & Aminoacids (AREA)
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- Organic Chemistry (AREA)
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Abstract
Description
단일사슬인슐린 유사체 | 연결펩티드 서열 | ED50 | |
수용체 결합 활성 | 글루코스 흡수 활성 | ||
인슐린 | - | 0.74 (100)a | 0.332 (100) |
B1 | RRRR APGDV KRR | 2.21 (33.5) | 1.153 (28.8) |
B2 | RRR APGDV KRRR | 2.32 (31.9) | 1.137 (29.2) |
H1 | RRR APGDV KR | 1.33 (55.6) | 0.806 (41.2) |
H2 | RR APGDV KRR | 1.21 (61.2) | 0.768 (43.2) |
H3 | RRR APGDV KRR | 1.20 (61.7) | 0.765 (43.4) |
M1 | RR APGDV KR | 1.47 (50.5) | 0.932 (35.6) |
M2 | RR YPGDV KR | 1.63 (45.5) | 0.932 (35.6) |
M3 | RR HPGDV KR | 1.57 (47.3) | 0.949 (35.1) |
M4 | RR GPG KR | 1.52 (48.8) | 1.06 (31.3) |
M5 | RR GGGGG KR | 1.71 (43.4) | 1.10 (30.2) |
T1 | RR GPG GG | 3.26 (22.8) | 1.95 (17.0) |
T2 | GG GPG KR | 2.68 (27.7) | 1.56 (21.3) |
T3 | RG GPG GR | 2.94 (25.2) | 1.88 (17.7) |
D1 | APGDV | 25.1 (2.96) | 9.38 (3.54) |
D2 | YPGDV | 16.5 (4.50) | 4.05 (8.20) |
D3 | HPGDV | 22.3 (3.32) | 6.23 (5.33) |
D4 | GPG | 60.1 (1.23) | 15.3 (2.17) |
D5 | GGGPGG | 10.2 (7.25) | |
D6 | GG GPG GG | 5.69 (13.0) | - |
프로인슐린 | RR-C peptide-KR | 33.7 (2.20) | 26.5 (1.25) |
des-프로인슐린 | C peptide | 258 (0.29) | - |
인슐린 유사체 | ED50a(nmol/kg) | 인슐린 대비 효능비(%) | ||
1시간후 | 2시간후 | 1시간후 | 2시간후 | |
인슐린 | 1.5 | 1.8 | 100 | 100 |
B1 | 3.3 | 2.8 | 45.8 | 65.2 |
H2 | 2.1 | 2.0 | 71.2 | 92.1 |
M2 | 2.8 | 2.2 | 53.6 | 81.8 |
M4 | 2.4 | 2.4 | 62.5 | 75.0 |
T1 | 4.2 | 4.1 | 35.7 | 43.9 |
D1 | 7.2 | 7.1 | 20.8 | 25.4 |
프로인슐린 | 8.0 | 8.0 | 18.8 | 22.2 |
Claims (4)
- 서열번호: 2의 아미노산 서열을 지닌 B사슬 - L사슬(링커 아미노산 서열을 지닌 사슬) - 서열번호: 1의 아미노산 서열을 지닌 A사슬로 구성된 단일사슬 인슐린 유사체상기식에서 L사슬은 7 내지 12 개의 아미노산 서열을 가지며 하기식(Ⅰ)로 나타낸다.X1 - Y - X2 (I)X1: 아르기닌-아르기닌 또는 아르기닌-아르기닌-아르기닌이고,Y: 3 내지 8 개의 불특정 아미노산 서열이고,X2: 리신-아르기닌 또는 리신-아르기닌-아르기닌이다.
- 제 1항에 있어서, 상기식(I)의 L사슬에 있어서 Y는 3 내지 5 개의 불특정 아미노산으로 구성된 것임을 특징으로 하는 단일사슬 인슐린 유사체
- 삭제
- 제 1항 또는 제 2항의 단일사슬 인슐린 유사체를 유효성분으로 포함하고, 약학적으로 허용되는 담체를 포함하는 당뇨병 치료제
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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KR10-2003-0040018A KR100508616B1 (ko) | 2003-06-20 | 2003-06-20 | 염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 |
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KR10-2003-0040018A KR100508616B1 (ko) | 2003-06-20 | 2003-06-20 | 염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20030063266A KR20030063266A (ko) | 2003-07-28 |
KR100508616B1 true KR100508616B1 (ko) | 2005-08-17 |
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KR10-2003-0040018A KR100508616B1 (ko) | 2003-06-20 | 2003-06-20 | 염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 |
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Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1692168B1 (en) | 2003-12-03 | 2011-07-20 | Novo Nordisk A/S | Single-chain insulin |
JP6584953B2 (ja) * | 2012-11-05 | 2019-10-02 | ケース ウェスタン リザーブ ユニバーシティCase Western Reserve University | 長時間作用型単鎖インスリン類似体 |
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- 2003-06-20 KR KR10-2003-0040018A patent/KR100508616B1/ko active IP Right Grant
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KR20030063266A (ko) | 2003-07-28 |
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