Summary of project PR000344
This data is available at the NIH Common Fund's National Metabolomics Data Repository (NMDR) website, the Metabolomics Workbench, https://www.metabolomicsworkbench.org, where it has been assigned Project ID PR000344. The data can be accessed directly via it's Project DOI: 10.21228/M8KK69 This work is supported by NIH grant, U2C- DK119886.
See: https://www.metabolomicsworkbench.org/about/howtocite.php
Project ID: | PR000344 |
Project DOI: | doi: 10.21228/M8KK69 |
Project Title: | Cloning, expression and derivatization of cytotoxic marine natural product Apratoxin |
Project Summary: | Apratoxin is a hybrid PKS/NRPS secondary metabolite showing potent anticancer activity by inducing G1 phase cell cycle arrest and apoptosis. There have been reported a series of natural apratoxin derivatives with defined chemical modifications in their structures that alter their biological activity. Looking for a better activity, total synthesis of apratoxin has been achieved and a series of synthetic congeners showed increased activity with subnanomolar potency. From the total synthesis point of view, the modification of the polyketide backbone presents a burden for a radical derivatization of apratoxins. We hypothesized that supply the polyketide part naturally by overexpression the corresponding genes it will facilitate the generation of apratoxin congeners by decorating the backbone with a variety of amino acids improving the antitumor activity.Threfore, the apratoxin gene cluster was recovered from a fosmid DNA library. The gene set responsible for the biosynthesis of the polyketide backbone was introduced in E. coli BAP strain and expressed at 30C for 24 hours. Two sets of control and experimental samples with culture broth pH adjusted at 8 and 12 respectively was extracted with ethyl acetate and dried. |
Institute: | University of Florida |
Department: | Medicinal Chemistry |
Last Name: | Luesch |
First Name: | Hendrik |
Address: | Medical Sciences Building, Rm P5-26, 1600 SW Archer Rd., FL32610 |
Email: | luesch@cop.ufl.edu |
Phone: | none |
Summary of all studies in project PR000344
Study ID | Study Title | Species | Institute | Analysis(* : Contains Untargted data) | Release Date | Version | Samples | Download(* : Contains raw data) |
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ST000446 | Heterologous expression and detection of Apratoxins in E. coli | Escherichia coli | University of Florida | MS* | 2017-10-03 | 1 | 12 | Uploaded data (2.8M) |