AR044857A1 - POLYMERIC CONJUGATES OF CYTOKINES, CHEMIOCINES, GROWTH FACTORS, POLYPEPTIDIC HORMONES AND THEIR ANTAGONISTS WITH CONSERVED ACTIVITY OF UNION TO THE RECEIVER - Google Patents
POLYMERIC CONJUGATES OF CYTOKINES, CHEMIOCINES, GROWTH FACTORS, POLYPEPTIDIC HORMONES AND THEIR ANTAGONISTS WITH CONSERVED ACTIVITY OF UNION TO THE RECEIVERInfo
- Publication number
- AR044857A1 AR044857A1 ARP040102168A AR044857A1 AR 044857 A1 AR044857 A1 AR 044857A1 AR P040102168 A ARP040102168 A AR P040102168A AR 044857 A1 AR044857 A1 AR 044857A1
- Authority
- AR
- Argentina
- Prior art keywords
- conjugates
- receptor binding
- cytokines
- methods
- polypeptide
- Prior art date
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- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
Se suministran métodos para la síntesis de conjugados poliméricos de citoquinas, quimiocinas, factores de crecimiento, hormonas polipeptídicas y sus antagonistas de unión al receptor, conjugados que retienen actividad de unión al receptor inusualmente elevada. La preparación de conjugados poliméricos de acuerdo con los métodos de la presente reduce o evita la inhibición estérica de interacciones receptor-ligando que comúnmente se producen a partir de la unión de polímeros a las regiones de unión al receptor de las citoquinas, quimiocinas, factores de crecimiento y hormonas polipeptídicas, como así también a sus análogos agonistas y antagonistas. Se suministra, además, los conjugados y las composiciones producidos por tales métodos. Los conjugados retienen un nivel de actividad de unión al receptor más alto que el producido por los métodos tradicionales de acoplamiento de polímeros que no se han orientado para evitar los dominios de unión al receptor de citoquinas, quimiocinas, factores de crecimiento y hormonas polipeptídicas. Los conjugados exhiben, además, una vida media extendida in vitro si se compara con las citoquinas, quimiocinas, factores de crecimiento y hormonas polipeptídicas no conjugados, suministra, además, kits que comprenden dichos conjugados y/o composiciones, y métodos de uso de tales conjugados y composiciones en una variedad de aplicaciones diagnósticas, profilácticas, terapéuticas y de procesamiento biológico. Reivindicación 1: Un método para sintetizar conjugados de uno o más polímeros sintéticos solubles en agua con una citoquina, una quimiocina, un factor de crecimiento o una hormona polipeptídica, o uno de sus antagonistas, que conserva más de la potencia de unión al receptor de dicha citoquina, dicha quimiocina, dicho factor de crecimiento o dicha hormona polipeptídica, o su antagonista, que la que se conserva cuando dichos polímeros se acoplan en forma aleatoria, que comprende: (a) seleccionar una citoquina, una quimiocina, un factor de crecimiento o una hormona polipeptídica en la cual el aminoácido amino-terminal se ubica en posición remota respecto de uno o más dominios de unión al receptor de dicha citoquina, dicha quimiocina, dicho factor de crecimiento o dicha hormona polipeptídica, o su antagonista, y (b) acoplar dicho uno o más polímeros en forma selectiva a dicho aminoácido amino-terminal.Methods for the synthesis of polymeric conjugates of cytokines, chemokines, growth factors, polypeptide hormones and their receptor binding antagonists, conjugates that retain unusually high receptor binding activity are provided. The preparation of polymeric conjugates according to the methods herein reduces or prevents steric inhibition of receptor-ligand interactions that commonly occur from the binding of polymers to the receptor binding regions of cytokines, chemokines, growth and polypeptide hormones, as well as their agonist and antagonist analogs. The conjugates and compositions produced by such methods are also supplied. The conjugates retain a higher level of receptor binding activity than that produced by traditional polymer coupling methods that have not been targeted to avoid receptor binding domains of cytokines, chemokines, growth factors and polypeptide hormones. The conjugates also exhibit an extended half-life in vitro when compared to cytokines, chemokines, growth factors and unconjugated polypeptide hormones, also provides kits comprising said conjugates and / or compositions, and methods of use of such conjugates and compositions in a variety of diagnostic, prophylactic, therapeutic and biological processing applications. Claim 1: A method of synthesizing conjugates of one or more water-soluble synthetic polymers with a cytokine, a chemokine, a growth factor or a polypeptide hormone, or one of its antagonists, which retains more than the receptor binding potency of said cytokine, said chemokine, said growth factor or said polypeptide hormone, or its antagonist, that which is conserved when said polymers are randomly coupled, comprising: (a) selecting a cytokine, a chemokine, a growth factor or a polypeptide hormone in which the amino-terminal amino acid is located remotely from one or more receptor binding domains of said cytokine, said chemokine, said growth factor or said polypeptide hormone, or its antagonist, and (b ) coupling said one or more polymers selectively to said amino-terminal amino acid.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47991403P | 2003-06-20 | 2003-06-20 | |
| US10/743,295 US20040136952A1 (en) | 2002-12-26 | 2003-12-23 | Polymer conjugates of cytokines, chemokines, growth factors, polypeptide hormones and antagonists thereof with preserved receptor-binding activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR044857A1 true AR044857A1 (en) | 2005-10-05 |
Family
ID=42778299
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102168 AR044857A1 (en) | 2003-06-20 | 2004-06-22 | POLYMERIC CONJUGATES OF CYTOKINES, CHEMIOCINES, GROWTH FACTORS, POLYPEPTIDIC HORMONES AND THEIR ANTAGONISTS WITH CONSERVED ACTIVITY OF UNION TO THE RECEIVER |
| ARP090103741 AR073408A2 (en) | 2003-06-20 | 2009-09-29 | POLYMERIC CONJUGATES OF CYTOKINES, CHEMIOCINES, GROWTH FACTORS, POLYPEPTIDIC HORMONES AND ITS ANTAGONISTS WITH CONSERVED ACTIVITY OF UNION TO THE RECEIVER |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103741 AR073408A2 (en) | 2003-06-20 | 2009-09-29 | POLYMERIC CONJUGATES OF CYTOKINES, CHEMIOCINES, GROWTH FACTORS, POLYPEPTIDIC HORMONES AND ITS ANTAGONISTS WITH CONSERVED ACTIVITY OF UNION TO THE RECEIVER |
Country Status (1)
| Country | Link |
|---|---|
| AR (2) | AR044857A1 (en) |
-
2004
- 2004-06-22 AR ARP040102168 patent/AR044857A1/en not_active Application Discontinuation
-
2009
- 2009-09-29 AR ARP090103741 patent/AR073408A2/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AR073408A2 (en) | 2010-11-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed, e.g., due to non-payment of fee |