A5029079820- Dendrimers and Hyperbranched Polymers
- RNA Interference and Gene Delivery
- Traditional and Medicinal Uses of Annonaceae
- Protein Kinase Regulation and GTPase Signaling
- Carbohydrate Chemistry and Synthesis
- Computational Drug Discovery Methods
- Enzyme Structure and Function
- Chemical Synthesis and Analysis
- Cellular transport and secretion
- Marine Sponges and Natural Products
- Complementary and Alternative Medicine Studies
- Advanced biosensing and bioanalysis techniques
- Phytochemical compounds biological activities
- Click Chemistry and Applications
- Herbal Medicine Research Studies
- Ubiquitin and proteasome pathways
- Plant biochemistry and biosynthesis
- Biochemical and Structural Characterization
- Inhalation and Respiratory Drug Delivery
- Nanoparticle-Based Drug Delivery
- Plant-derived Lignans Synthesis and Bioactivity
- Cancer-related Molecular Pathways
- Phytochemistry and Biological Activities
- Glycosylation and Glycoproteins Research
- Immunotherapy and Immune Responses
Starpharma (Australia)
2013-2025
The University of Queensland
2025
Magic Leap (United States)
2023
University of Hertfordshire
2023
Emerald Group Publishing (United Kingdom)
2023
University of Nottingham
2023
University of Utah
1998-2010
Monash University
2000-2009
The University of Melbourne
2008-2009
Commonwealth Scientific and Industrial Research Organisation
2009
The systemic delivery of drugs via the inhaled route is an attractive, needle-free means improving exposure molecules such as peptides and proteins that are poorly absorbed after oral administration. Directed into lungs also provides a increasing drug concentrations at site action for lung-specific disease states pulmonary infections lung cancer. current study has examined potential utility PEGylated polylysine dendrimers agents in particular sought to explore relationship between dendrimer...
Abstract Dual Bcl-2/Bcl-x L inhibitors are expected to deliver therapeutic benefit in many haematological and solid malignancies, however, their use is limited by tolerability issues. AZD4320, a potent dual inhibitor, has shown good efficacy however had dose limiting cardiovascular toxicity preclinical species, coupled with challenging physicochemical properties, which prevented its clinical development. Here, we describe the design development of AZD0466, drug-dendrimer conjugate, where...
Total synthesis of the anticancer 1,4-dioxane containing natural products silvestrol (1) and episilvestrol (2) is described by an approach based on proposed biosynthesis these novel compounds. The key steps included oxidative rearrangement protected d-glucose derivative 11 to afford 12, which could be elaborated coupling partner 5 a photochemical [3 + 2]-cycloadditon between 3-hydroxyflavone 27 methyl cinnamate followed base-induced α-ketol reduction give cyclopentabenzofuran core 33. (−)-6...
PEGylated polylysine dendrimers show promise as novel drug delivery systems with the potential to direct site specific deposition patterns and reduce toxicity at nontarget sites. Here activity profiles of a generation 5 dendrimer 50% surface conjugation PEG1100 doxorubicin (via an acid labile 4-hydrazinosulfonyl benzoic linker) have been compared in Walker 256 rat tumor model human MDA-MB231 xenograft mice. A comparison was also made liposomal formulation solution. In both mouse breast...
The current study sought to explore whether the subcutaneous administration of lymph targeted dendrimers, conjugated with a model chemotherapeutic (methotrexate, MTX), was able enhance anticancer activity against node metastases. lymphatic pharmacokinetics and antitumor PEGylated polylysine dendrimers MTX [D-MTX(OH)] via tumor-labile hexapeptide linker examined in rats compared similar system where α-carboxyl O-tert-butylated [D-MTX(OtBu)]. latter has previously been shown exhibit longer...
Dendrimers are branched macromolecular structures that useful nanocarriers for small-molecule drugs, such as cancer therapeutics. Their small size permits penetration into solid tumors, coupled with functionalization a low-fouling PEG coating minimizes transient cellular interactions and enhances plasma circulation time. While PEGylated dendrimers show significant promise anticancer therapeutics, there is potential to increase tumor cell specificity drive uptake of drugs cells by conjugating...
Sugar and spice…︁ The total synthesis of the rare but potent anticancer natural product (−)-episilvestrol its 5′′′ epimer (−)-silvestrol was accomplished from D-glucose, naringenin, methyl cinnamate (see scheme). key steps sequence were inspired by possible biogenesis these compounds. Supporting information for this article is available on WWW under http://www.wiley-vch.de/contents/jc_2002/2007/z702700_s.pdf or author. Please note: publisher not responsible content functionality any...
A generation 5 PEGylated (PEG 1100) polylysine dendrimer, conjugated via a stable amide linker to OtBu protected methotrexate (MTX), was previously shown have circulatory half-life of 2 days and target solid tumors in both rats mice. Here, we show that deprotection MTX substitution the with matrix metalloproteinase (MMP) 9 cleavable (PVGLIG) dramatically increased plasma clearance promoted deposition liver spleen (50-80% dose recovered 3 post dose). Similar rapid also seen using scrambled...
PEGylation typically improves the systemic exposure and tumor biodistribution of polymeric drug delivery systems, but may also restrict enzyme access to peptide-based linkers. The impact dendrimer generation (G4 vs G5) PEG length (570 1100 Da) on pharmacokinetics, biodistribution, release kinetics, anticancer activity a series PEGylated polylysine dendrimers conjugated with doxorubicin via cathepsin-B cleavable valine-citrulline linker was therefore investigated in rodents. Although smallest...
The contributions to catalysis of the conserved catalytic aspartate (Asp149) in phosphorylase kinase subunit (PhK; residues 1−298) have been studied by kinetic and crystallographic methods. Kinetic studies solvents different viscosity show that PhK, like cyclic AMP dependent protein kinase, exhibits a mechanism which chemical step phosphoryl transfer is fast rate-limiting release products, ADP phosphoprotein, possibly viscosity-dependent conformational changes. Site-directed mutagenesis...
For the study of biological signal transduction, access to correctly lipidated proteins is utmost importance. Furthermore, bioconjugates that embody correct structure protein but may additionally carry different lipid groups or labels (i.e., fluorescent tags) by which can be traced in systems, could provide invaluable reagents. We report here development techniques for synthesis a series modified Ras proteins. These number different, natural and non-natural residues, process was extended...
An induced circular dichroism (CD) spectrum is observed for 1,1',3,3,3',3'-hexamethyl-9-phenyl-indocarbocyanine, 1,1'-diethyl-2,2'-cyanine, 1,1'-di-(3,5-di-tert-butyl)benzyl-2,2'-cyanine, or 1,1'-di-(4-tert-butyl)benzyl-2,2'-cyanine when penetrated into a chiral cavity of either spirobi[(2-methyl)borataxanthene] spirobi[(3-methyl)borataxanthene]. Within the ion pair, cyanine dye exists in two (or more) interconverting conformations unequal energy. Solid-state structural evidence suggests...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT2,5-Dithiacyclopentylideneketene and ethenedithione, S:C:C:S, generated by flash vacuum pyrolysisCurt Wentrup, Peter Kambouris, Richard A. Evans, David Owen, Graham Macfarlane, Josselin Chuche, Jean Claude Pommelet, Abdelhamid Ben Cheikh, Michel Plisnier, Robert FlammangCite this: J. Am. Chem. Soc. 1991, 113, 8, 3130–3135Publication Date (Print):April 1, 1991Publication History Published online1 May 2002Published inissue 1 April...
Type II diabetes mellitus is a chronic metabolic disorder that can lead to serious cardiovascular, renal, neurologic, and retinal complications. While several drugs are currently prescribed treat type diabetes, their efficacy limited by mechanism-related side effects (weight gain, hypoglycemia, gastrointestinal distress), inadequate for use as monotherapy, the development of tolerance agents. Consequently, combination therapies frequently employed effectively regulate blood glucose levels....