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Guaianolide sesquiterpenes from Pulicaria crispa (Forssk.) Oliv.
- M. Stavri, K. T. Mathew, Andrew Gordon, S. Shnyder, R. Falconer, S. Gibbons
- Biology, Medicine
- 1 June 2008
A phytochemical study of the asteraceous herb Pulicaria crispa (Forssk.) Oliv resulted in the characterisation of three guaianolide sesquiterpenes, which exhibited weak antimycobacterial activity against Mycobacterium phlei and cytotoxicity in a human bladder carcinoma cell line, EJ-138. Expand
Pharmacological Inhibition of polysialyltransferase ST8SiaII Modulates Tumour Cell Migration
ST8SiaII can be considered a druggable target with the potential for interfering with a critical mechanism in tumour cell dissemination in metastatic cancers, and is demonstrated for the first time that a polysialyltransferase inhibitor can modulate migration in ST8SIAII-expressing tumour cells. Expand
Polysialyltransferase: a new target in metastatic cancer.
- R. Falconer, R. Errington, S. Shnyder, P. Smith, L. Patterson
- Biology, Medicine
- Current cancer drug targets
- 30 September 2012
The demonstration that polyST knock-down negates events associated with tumour cell dissemination indicates that PST and STX are validated targets and presents a therapeutic opportunity to inhibit tumour invasion and metastasis. Expand
Synthesis of C-terminal glycopeptides from resin-bound glycosyl azides via a modified Staudinger reaction.
The solid-phase synthesis of glycopeptides containing the sugar at the C-terminus is reported, generally applicable to most peptide sequences and is compatible with both Boc- and Fmoc- synthetic strategies on a variety of resins. Expand
Progress towards a clinically-successful ATR inhibitor for cancer therapy
This review focuses on the biology of ATR, its functional role in cancer development and treatment, and the rationale behind inhibition of this target as a therapeutic approach, including evaluation of the progress and current status of development of potent and specific ATR inhibitors that have emerged in recent decades. Expand
Membrane type 1-matrix metalloproteinase (MT1-MMP) targeted antitumor agents
2453 Matrix metalloproteinase (MMP) activity is required for tumour growth and metastasis. This study assessed the expression of membrane-type MMP1 (MT1-MMP) in human Non Small Cell Lung Cancer… Expand
Development of novel tumor-targeted theranostic nanoparticles activated by membrane-type matrix metalloproteinases for combined cancer magnetic resonance imaging and therapy.
- Celina Ansari, G. Tikhomirov, +10 authors H. Daldrup-Link
- Materials Science, Medicine
- 1 February 2014
These findings demonstrate proof of concept for a new nanotemplate that integrates tumor specificity, drug delivery and in vivo imaging into a single TNP entity through attachment of enzyme-activated prodrugs onto magnetic nanoparticles. Expand
Novel liposaccharide conjugates for drug and peptide delivery.
- B. Drouillat, A. Hillery, G. Dékány, R. Falconer, K. Wright, I. Toth
- Chemistry, Medicine
- Journal of pharmaceutical sciences
These preliminary experiments have demonstrated the ability of the liposaccharides to form particulate systems per se and also their ability to be incorporated into conventional liposomal systems. Expand
Development of a novel tumor-targeted vascular disrupting agent activated by membrane-type matrix metalloproteinases.
The design and characterization of a novel VDA, ICT2588, that is nontoxic until activated specifically in the tumor by membrane-type 1 matrix metalloproteinase (MT1-MMP) is described, which achieves selective VDA targeting based on MT-M MP activation in the tumors microenvironment. Expand
Design, synthesis and biological evaluation of novel lipoamino acid-based glycolipids for oral drug delivery.
A series of lipoamino acid-based glycolipids were synthesised and conjugated to monosaccharides to yield novel O-, N, S- and C-linked glycolIPids in good yields, with potential to improve the oral absorption of piperacillin. Expand