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Engineered production of cancer targeting peptide (CTP)-containing C-1027 in Streptomyces globisporus and biological evaluation.

Abstract：

:Conjugation of cancer targeting peptides (CTPs) with small molecular therapeutics has emerged as a promising strategy to deliver potent (but typically nonspecific) cytotoxic agents selectively to cancer cells. Here we report the engineered production of a CTP (NGR)-containing C-1027 and evaluation of its activity against selected cancer cell lines. C-1027 is an enediyne chromoprotein produced by Streptomyces globisporus, consisting of an apo-protein (CagA) and an enediyne chromophore (C-1027). NGR is a CTP that targets CD13 in tumor vasculature. S. globisporus SB1026, a recombinant strain engineered to encode CagA with the NGR sequence fused at its C-terminus, directly produces the NGR-containing C-1027 that is equally active as the native C-1027. Our results demonstrate the feasibility to produce CTP-containing enediyne chromoproteins by metabolic pathway engineering and microbial fermentation and will inspire efforts to engineer other CTP-containing drug binding proteins for targeted delivery.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li W,Li X,Huang T,Teng Q,Crnovcic I,Rader C,Shen B

doi

10.1016/j.bmc.2016.04.017

subject

Has Abstract

pub_date

2016-09-01 00:00:00

pages

3887-3892

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30251-6

journal_volume

24

pub_type

杂志文章

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