Covering: 2009 to 2013. This review covers the 188 novel marine natural products described since 2008, from deep-water (50->5000 m) marine fauna including bryozoa, chordata, cnidaria, echinodermata, microorganisms, mollusca and porifera. The structures of the new compounds and details of the source organism, depth of collection and country of origin are presented, along with any relevant biological activities of the metabolites. Where reported, synthetic studies on the deep-sea natural products have also been included. Most strikingly, 75% of the compounds were reported to possess bioactivity, with almost half exhibiting low micromolar cytotoxicity towards a range of human cancer cell lines, along with a significant increase in the number of microbial deep-sea natural products reported.
Isatin (1H-indole-2,3-dione) and its derivatives demonstrate a diverse array of biological and pharmacological activities including anticonvulsant, antibacterial, antifungal, antiviral and anticancer properties. This broad spectrum of biochemical targets has been facilitated by the synthetic versatility of isatin, which has allowed the generation of a large number of structurally diverse derivatives including analogues derived from substitution of the aryl ring, and/or derivatisation of the isatin nitrogen and C2/C3 carbonyl moieties. The recent FDA approval of the oxindole sunitinib malate, as a kinase inhibitor for the treatment of advanced renal carcinoma and gastrointestinal stromal tumours, underscores the increasing interest in isatins as a new class of antineoplastic agents. In addition to potent kinase inhibition, the mechanism of action of other isatin derivatives includes the inhibition and/or modulation of proteases, translation initiation, neo-vascularisation and tubulin polymerisation. It was therefore the objective of this review to systematically evaluate the cytotoxic and anticancer properties of various substituted isatins and collate these findings to be used as a guide for future structure-activity relationship and mode of action studies. This is the first review to comprehensively discuss the in vitro and in vivo anticancer activities of isatin and its substituted derivatives.
This review covers the 390 novel marine natural products described to date from deep-water (>50 m) marine fauna, with details on the source organism, its depth and country of origin, along with any reported biological activity of the metabolites. Relevant synthetic studies on the deep-sea natural products have also been included.
Upregulation of sialyltransferases—the enzymes responsible for the addition of sialic acid to growing glycoconjugate chains—and the resultant hypersialylation of up to 40–60% of tumour cell surfaces are established hallmarks of several cancers, including lung, breast, ovarian, pancreatic and prostate cancer. Hypersialylation promotes tumour metastasis by several routes, including enhancing immune evasion and tumour cell survival, and stimulating tumour invasion and migration. The critical role of enzymes that regulate sialic acid in tumour cell growth and metastasis points towards targeting sialylation as a potential new anti-metastatic cancer treatment strategy. Herein, we explore insights into the mechanisms by which hypersialylation plays a role in promoting metastasis, and explore the current state of sialyltransferase inhibitor development.
For thousands of years humankind has sought to explore our oceans. Evidence of this early intrigue dates back to 130,000BCE, but the advent of remotely operated vehicles (ROVs) in the 1950s introduced technology that has had significant impact on ocean exploration. Today, ROVs play a critical role in both military (e.g. retrieving torpedoes and mines) and salvage operations (e.g. locating historic shipwrecks such as the RMS Titanic), and are crucial for oil and gas (O&G) exploration and operations. Industrial ROVs collect millions of observations of our oceans each year, fueling scientific discoveries. Herein, we assembled a group of international ROV experts from both academia and industry to reflect on these discoveries and, more importantly, to identify key questions relating to our oceans that can be supported using industry ROVs. From a long list, we narrowed down to the 10 most important questions in ocean science that we feel can be supported (whole or in part) by increasing access to industry ROVs, and collaborations with the companies that use them. The questions covered opportunity (e.g. what is the resource value of the oceans?) to the impacts of global change (e.g. which marine ecosystems are most sensitive to anthropogenic impact?). Looking ahead, we provide recommendations for how data collected by ROVs can be maximised by higher levels of collaboration between academia and industry, resulting in win-win outcomes. What is clear from this work is that the potential of industrial ROV technology in unravelling the mysteries of our oceans is only just beginning to be realised. This is particularly important as the oceans are subject to increasing impacts from global change and industrial exploitation. The coming decades will represent an important time for scientists to partner with industry that use ROVs in order to make the most of these 'eyes in the sea'.
The cyclization of small peptides which do not incorporate turn inducers is often difficult. We have developed a method involving the use of removable turn inducers, in the form of pseudoprolines, for the cyclization of difficult peptide sequences. The pseudoprolines induce a cisoid amide bond in the peptide backbone which facilitates cyclization. They are then readily removed to yield a cyclic peptide that does not contain any turn inducers.
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