Human interferon alpha derivatives and preparation and use of pegylated products thereof

A technology of pegylation and interferon alpha, applied in the field of biomedicine, can solve the problems of fast plasma clearance, limitation, poor stability, etc., and achieve the effect of treating or preventing viral infections or tumor diseases
CN101671390BActive Publication Date: 2012-10-03BEIJING SIHUAN PHARMA +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING SIHUAN PHARMA
Publication Date
2012-10-03

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Abstract

The invention relates to human interferon alpha derivatives and preparation and use of pegylated products thereof. The human interferon alpha derivatives are formed by bonding three amino acids to N terminals of human interferon alpha and have a structural formula of R3-R2-R1-interferon, wherein the interferon is the human interferon alpha, and a first position amino acid R1 bonded to the N terminals of the human interferon alpha is a sculpture amino acid or glycine; the second position amino R2 is an aromatic amino acid or glycine; and the third position amino acid R3 is an acidic amino acidor glycine. The invention also provides pegylated derivatives of the human interferon alpha derivatives, a preparation method thereof and use thereof in the preparation of medicaments for treating and preventing viral infection or lung cancer. The human interferon alpha derivatives have the advantages of high specific activity and high pegylation rate. The pegylated derivatives of the human interferon alpha derivatives have the characteristics of high biological activity and no non-N terminal modified isomers and have the advantages of prolonging in-vivo half-life, reducing plasma clearance and the like.
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Description

technical field

[0001] The invention relates to the technical field of biomedicine, in particular to the preparation and application of human interferon alpha derivatives and their pegylated modifications. Background technique

[0002] Human interferon (IFN for short) is a kind of active protein with broad-spectrum anti-virus, anti-proliferation and immunoregulatory functions existing in the body. It is one of the earliest cytokines used in clinical treatment. Human interferon can be divided into three types: Types, namely human interferon-α, human interferon-β, and human interferon-γ, can be further divided into several subtypes according to the amino acid sequence of each type of IFN. A large number of clinical studies have proved that human interferon-α is an important anti-tumor and anti-viral drug. At present, the most widely used clinically in my country is mainly recombinant human interferon α-1a, α-2a and α-1b.

[0003] It has been found that the type I family of h...

Claims

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