Cypemycin precursor peptide mutant and application thereof and prepared cypemycin analogues

Abstract

The present invention discloses a cypemycin precursor peptide mutant and an application thereof and prepared cypemycin analogues. The mutant is prepared by mutating one or more threonines in a core peptide to serine, lysine, alanine or leucine; and / or, mutating one or two glutamines in the core peptide to glutamic acid; and / or, mutating serine in the core peptide to alanine or tyrosine; and / or, mutating valine at a 12nd and / or 21st position of a sequence shown in SEQ ID NO.1 to lysine, alanine, isoleucine, or cysteine; and / or, mutating cysteine at a 19th position of the sequence shown in the SEQ ID NO.1 to serine or tyrosine; and / or, mutating cysteine at a 33rd position and / or proline at a 36th position of a sequence shown in SEQ ID NO.2 to alanine. A series of cypemycin analogues can be prepared by using the mutant and provide a basis for screening compounds with higher activity.

Description

technical field

[0001] The invention belongs to the field of biotechnology engineering, and specifically relates to a mutant of a septomycin precursor peptide, an application thereof and a prepared septomycin analogue. Background technique

[0002] Natural products are the material basis for drug discovery and development, and have received great attention from microbiologists and pharmacologists in the past few decades, among which penicillin, streptomycin, and abamectin have been favored by Nobel Prizes one after another. At present, 60% of clinical anticancer drugs and 70% of antibiotics are derived from them. In recent years, with the emergence of various drug-resistant bacteria and super-resistant bacteria, many natural products have good development prospects in the field of new drug research and development in the future because of their good biological activity.

[0003] Cypemycin (Septomycin, also known as Cypemycin) is a "star" compound of the linaridin (linear de...

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