Journal ArticleDOI
Microbial natural products: molecular blueprints for antitumor drugs
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TLDR
This review describes only a handful of exemplary natural products and their derivatives as well as those that have served as elegant blueprints for the development of novel synthetic structures that are either currently in use or in clinical or preclinical trials together with some of their earlier analogs in some cases whose failure to proceed aided in the derivation of later compounds.Abstract:
Microbes from two of the three domains of life, the Prokarya, and Eukarya, continue to serve as rich sources of structurally complex chemical scaffolds that have proven to be essential for the development of anticancer therapeutics. This review describes only a handful of exemplary natural products and their derivatives as well as those that have served as elegant blueprints for the development of novel synthetic structures that are either currently in use or in clinical or preclinical trials together with some of their earlier analogs in some cases whose failure to proceed aided in the derivation of later compounds. In every case, a microbe has been either identified as the producer of secondary metabolites or speculated to be involved in the production via symbiotic associations. Finally, rapidly evolving next-generation sequencing technologies have led to the increasing availability of microbial genomes. Relevant examples of genome mining and genetic manipulation are discussed, demonstrating that we have only barely scratched the surface with regards to harnessing the potential of microbes as sources of new pharmaceutical leads/agents or biological probes.read more
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Natural product discovery: past, present, and future
Leonard Katz,Richard H. Baltz +1 more
TL;DR: Advances in bioinformatics, mass spectrometry, proteomics, transcriptomics, metabolomics and gene expression are driving the new field of microbial genome mining for applications in natural product discovery and development.
Journal Article
Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization.:II. FERMENTATION, ISOLATION AND CHARACTERIZATION
TL;DR: Rapamycin is a new antifungal antibiotic produced by Streptomyces hygroscopicus and can be classified as a triene, highly active against various Candida species, especially Candida albicans.
Journal ArticleDOI
Metabolite induction via microorganism co-culture: A potential way to enhance chemical diversity for drug discovery
TL;DR: Co-culture studies that aim to increase the diversity of metabolites obtained from microbes, with a special emphasis on the multiple methods of performing co-culture experiments, are focused on.
Journal ArticleDOI
A Review of the Microbial Production of Bioactive Natural Products and Biologics.
Janette V. Pham,Mariamawit A. Yilma,Adriana Feliz,Murtadha T. Majid,Nicholas Maffetone,Jorge R. Walker,Eunji Kim,Hyo Je Cho,Jared M. Reynolds,Myoung Chong Song,Sung Ryeol Park,Sung Ryeol Park,Yeo Joon Yoon +12 more
TL;DR: The structures and diverse biological activities of natural products and recombinant proteins that have been exploited as valuable molecules in medicine, agriculture and insect control are introduced and suggested to inspire the development of new therapeutic agents in academia and industry.
Journal ArticleDOI
Marine-sourced anti-cancer and cancer pain control agents in clinical and late preclinical development.
David J. Newman,Gordon M. Cragg +1 more
TL;DR: This review shows the compounds derived from marine sources that are currently in clinical trials against cancer and the use of marine-derived agents to ameliorate the pain from cancers in humans, and to act as an adjuvant in immunological therapies.
References
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Journal ArticleDOI
Total Synthesis of Bryostatin 3 This work was supported by the Ministry of Education, Science, Sports, and Culture (Japan). K.O. is grateful to JSPS for a predoctoral fellowship. The authors thank Dr. G. N. Chmurny (NIH) for providing them with (1)H and (13)C NMR spectra of bryostatin 3 and for helpful discussions.
Journal ArticleDOI
The Potential of Natural Products in the Discovery of Pharma Leads: A Case for Reassessment
Patent
Sequences for fk228 biosyntnesis and methods of synthesizing fk228 and fk228 analogs
TL;DR: In this paper, the polypeptides involved in biosynthesis of FK 228 and those involved in synthesis of a novel FK228 analog, thailandepsin are disclosed.
Journal ArticleDOI
4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
Cristina Rossi,Christopher I. Fincham,Piero D’Andrea,Marina Porcelloni,Alessandro Ettorre,Sandro Mauro,Mario Bigioni,Monica Binaschi,Carlo Alberto Maggi,Federica Nardelli,Massimo Parlani,Daniela Fattori +11 more
TL;DR: The second part of the strategy used in the research group to find a new class of HDAC inhibitors is reported, namely the SAR study for the compounds bearing a sulfonyl group on the piperidine nitrogen, which has considered both sulfonamides and sulfonyL ureas.
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