MX339993B - Inhibidores dimericos de alta afinidad de psd-95 como neuroprotectores eficientes contra daño isquemico cerebral y para el tratamiento de dolor. - Google Patents
Inhibidores dimericos de alta afinidad de psd-95 como neuroprotectores eficientes contra daño isquemico cerebral y para el tratamiento de dolor.Info
- Publication number
- MX339993B MX339993B MX2013013146A MX2013013146A MX339993B MX 339993 B MX339993 B MX 339993B MX 2013013146 A MX2013013146 A MX 2013013146A MX 2013013146 A MX2013013146 A MX 2013013146A MX 339993 B MX339993 B MX 339993B
- Authority
- MX
- Mexico
- Prior art keywords
- peptide
- analogue
- inhibitors
- psd
- linker
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 5
- 208000002193 Pain Diseases 0.000 title abstract 2
- 238000011282 treatment Methods 0.000 title abstract 2
- 230000006931 brain damage Effects 0.000 title 1
- 231100000874 brain damage Toxicity 0.000 title 1
- 208000029028 brain injury Diseases 0.000 title 1
- 230000000302 ischemic effect Effects 0.000 title 1
- 239000004090 neuroprotective agent Substances 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 8
- 108010051109 Cell-Penetrating Peptides Proteins 0.000 abstract 2
- 102000020313 Cell-Penetrating Peptides Human genes 0.000 abstract 2
- 108700019745 Disks Large Homolog 4 Proteins 0.000 abstract 2
- 102000047174 Disks Large Homolog 4 Human genes 0.000 abstract 2
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 abstract 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 abstract 1
- 102100022397 Nitric oxide synthase, brain Human genes 0.000 abstract 1
- 101710111444 Nitric oxide synthase, brain Proteins 0.000 abstract 1
- 125000003275 alpha amino acid group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 231100000318 excitotoxic Toxicity 0.000 abstract 1
- 230000003492 excitotoxic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente invención se refiere a nuevos inhibidores potentes del complejo de proteína ternario de NNOS, PSD-95 y el receptor NMDA y composiciones farmacéuticas que comprenden los inhibidores para profilaxis y/o tratamiento de enfermedad relacionada a excitotoxicidad y condiciones de dolor crónico en un sujeto. Los inhibidores son inhibidores de PSD-95 diméricos que comprenden un primer péptido o análogo peptídico enlazado a un segundo péptido o análogo peptídico por un ligador, en donde el primero y el segundo péptido o análogo peptídico comprenden al menos cuatro residuos unidos a amida que tiene una secuencia YTXV o YSXV, en donde a. Y se selecciona de entre E, Q, y A, y un análogo de los mismos, y b. X se selecciona de entre A, Q, D, N, N-Me-A, N-Me--Q, N-Me-D, y N-Me-N o un análogo de estos, y en donde un péptido penetrador de célula (CPP) se enlaza al ligador o a una cadena lateral de amino del primero y el segundo péptido o análogo peptídico. El ligador puede ser un ligador de PEG o de NPEG.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161485898P | 2011-05-13 | 2011-05-13 | |
| EP11165994 | 2011-05-13 | ||
| PCT/EP2012/058762 WO2012156308A1 (en) | 2011-05-13 | 2012-05-11 | High-affinity, dimeric inhibitors of psd-95 as efficient neuroprotectants against ischemic brain damage and for treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013013146A MX2013013146A (es) | 2014-05-27 |
| MX339993B true MX339993B (es) | 2016-06-21 |
Family
ID=51360100
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013013146A MX339993B (es) | 2011-05-13 | 2012-05-11 | Inhibidores dimericos de alta afinidad de psd-95 como neuroprotectores eficientes contra daño isquemico cerebral y para el tratamiento de dolor. |
Country Status (2)
| Country | Link |
|---|---|
| US (1) | US9139615B2 (es) |
| MX (1) | MX339993B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3074032T3 (pl) * | 2013-12-01 | 2019-06-28 | University Of Copenhagen | Pochodne kwasów tłuszczowych dimerycznych inhibitorów psd-95 |
| CN110386962A (zh) * | 2019-07-04 | 2019-10-29 | 苏州强耀生物科技有限公司 | 一种阿霉素偶联靶向多肽的合成方法 |
| CN110627877A (zh) * | 2019-09-25 | 2019-12-31 | 成都奥达生物科技有限公司 | 一种psd-95抑制剂 |
| WO2021194257A1 (ko) * | 2020-03-25 | 2021-09-30 | (주) 업테라 | 세포 투과성 펩티드 이량체, 이의 제조방법 및 이를 이용한 카고 전달 시스템 |
| CN119390848A (zh) * | 2023-09-07 | 2025-02-07 | 湖南中晟全肽生物科技股份有限公司 | 具有神经保护作用的肽及其应用 |
| CN119039462A (zh) * | 2023-09-07 | 2024-11-29 | 湖南中晟全肽生物科技股份有限公司 | 兴奋性神经毒性相关损伤的治疗肽 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7510824B2 (en) | 1999-06-02 | 2009-03-31 | Nono Inc. | Method of screening peptides useful in treating traumatic injury to the brain or spinal cord |
| US20090285780A1 (en) | 2006-05-24 | 2009-11-19 | Chyi Lee | Peg linker compounds and biologically active conjugates thereof |
| JP5746468B2 (ja) | 2006-07-11 | 2015-07-08 | ノノ インコーポレイテッド | 発熱を伴う脳卒中を処置する方法および組成物 |
| DK2320927T3 (en) | 2008-07-09 | 2015-09-14 | Univ Copenhagen | Modified peptides as potent inhibitors of the PSD-95 / NMDA receptor interaction |
-
2012
- 2012-05-11 MX MX2013013146A patent/MX339993B/es active IP Right Grant
- 2012-05-11 US US14/116,862 patent/US9139615B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9139615B2 (en) | 2015-09-22 |
| MX2013013146A (es) | 2014-05-27 |
| US20140094415A1 (en) | 2014-04-03 |
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