Publications by authors named "Brad Carte"

5 Publications

  • Page 1 of 1

Marinocyanins, cytotoxic bromo-phenazinone meroterpenoids from a marine bacterium from the streptomycete clade MAR4.

Tetrahedron 2017 Apr 6;73(16):2234-2241. Epub 2017 Mar 6.

Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, La Jolla, CA, 92093-0204, USA.

Six cytotoxic and antimicrobial metabolites of a new bromo-phenazinone class, the marinocyanins A-F (-), were isolated together with the known bacterial metabolites 2-bromo-1-hydroxyphenazine (), lavanducyanin ( WS-9659A) and its chlorinated analog WS-9659B (). These metabolites were purified by bioassay-guided fractionation of the extracts of our MAR4 marine actinomycete strains CNS-284 and CNY-960. The structures of the new compounds were determined by detailed spectroscopic methods and marinocyanin A () was confirmed by crystallographic methods. The marinocyanins represent the first bromo-phenazinones with an -isoprenoid substituent in the skeleton. Marinocyanins A-F show strong to weak cytotoxicity against HCT-116 human colon carcinoma and possess modest antimicrobial activities against and amphotericin-resistant .
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http://dx.doi.org/10.1016/j.tet.2017.03.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5555602PMC
April 2017

Investigations of the marine flora and fauna of the Fiji Islands.

Nat Prod Rep 2012 Dec 14;29(12):1424-62. Epub 2012 Sep 14.

Centre for Drug Discovery and Conservation, Institute of Applied Sciences, The University of the South Pacific, Suva, Fiji.

Over the past 30 years, approximately 140 papers have been published on marine natural products chemistry and related research from the Fiji Islands. These came about from studies starting in the early 1980s by the research groups of Crews at the University of California Santa Cruz, Ireland at the University of Utah, Gerwick from the Scripps Institution of Oceanography, the University of California at San Diego and the more recent groups of Hay at the Georgia Institute of Technology (GIT) and Jaspars from the University of Aberdeen. This review covers both known and novel marine-derived natural products and their biological activities. The marine organisms reviewed include invertebrates, plants and microorganisms, highlighting the vast structural diversity of compounds isolated from these organisms. Increasingly during this period, natural products chemists at the University of the South Pacific have been partners in this research, leading in 2006 to the development of a Centre for Drug Discovery and Conservation (CDDC).
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http://dx.doi.org/10.1039/c2np20055dDOI Listing
December 2012

Identification of novel small-molecule inhibitors for human transketolase by high-throughput screening with fluorescent intensity (FLINT) assay.

J Biomol Screen 2004 Aug;9(5):427-33

S*BIO, Singapore.

The metabolic enzyme transketolase (TK) plays a crucial role in tumor cell nucleic acid synthesis, using glucose through the elevated nonoxidative pentose phosphate pathway (PPP). Identification of inhibitors specifically targeting TK and preventing the nonoxidative PPP from generating the RNA ribose precursor, ribose-5-phosphate, provides a novel approach for developing effective anticancer therapeutic agents. The full-length human transketolase gene was cloned and expressed in Escherichia coli and the recombinant human transketolase protein purified to homogeneity. A fluorescent intensity (FLINT) assay was developed and optimized. Library compounds were screened in a high-throughput screening (HTS) campaign using the FLINT assay. Fifty-four initial hits were identified. Among them, 2 scaffolds with high selectivity, ideal physiochemical properties, and low molecular weight were selected for lead optimization studies. These compounds specifically inhibited in vitro TK enzyme activity and suppressed tumor cell proliferation in at least 3 cancer cell lines: SW620, LS174T, and MIA PaCa-2. Identification of these active scaffolds represents a good starting point for development of drugs specifically targeting TK and the nonoxidative PPP for cancer therapy.
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http://dx.doi.org/10.1177/1087057104263913DOI Listing
August 2004

Three new pyridoacridine type alkaloids from a singaporean ascidian.

J Nat Prod 2002 Aug;65(8):1198-200

Centre for Natural Product Research, Institute of Molecular and Cell Biology, Singapore Science Park, 128041, Singapore.

Two new pyridoacridine alkaloids, kuanoniamines E and F, and a new ring-opened pyridoacridine alkaloid, subarine, were isolated from a Singaporean ascidian. Also isolated were known pyridoacridine alkaloids ascididemin and kuanoniamines A and D. The structures of the alkaloids were determined by spectroscopic methods.
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http://dx.doi.org/10.1021/np010629vDOI Listing
August 2002

Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.

J Nat Prod 2002 Apr;65(4):628-9

Department of Drug Discovery, Millennium Pharmaceuticals Inc., 75-5 Sidney Street, Cambridge, Massachusetts 02139-1562, USA.

As part of a search for novel inhibitors of cathepsin K, the MeOH extract of a Micronesian sponge of the order Haplosclerida was shown to be active. Bioassay-guided fractionation of the extract yielded halitoxins, tryptamine, and a novel tryptamine-derived alkaloid, haploscleridamine (1). The tetrahydro-beta-carboline structure of haploscleridamine (1) was elucidated through spectral techniques. Haploscleridamine (1) was found to be an inhibitor of cathepsin K with an IC(50) of 26 microM.
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http://dx.doi.org/10.1021/np010500lDOI Listing
April 2002