A5008957279- Synthetic Organic Chemistry Methods
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- Asymmetric Synthesis and Catalysis
- Marine Sponges and Natural Products
- Oxidative Organic Chemistry Reactions
- Microbial Natural Products and Biosynthesis
- Chemical synthesis and alkaloids
- Synthesis of Organic Compounds
- Synthesis and Catalytic Reactions
- Fluorine in Organic Chemistry
- Synthesis and Reactions of Organic Compounds
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Protein Kinase Regulation and GTPase Signaling
- Melanoma and MAPK Pathways
- Synthesis and biological activity
- Advanced Synthetic Organic Chemistry
- Analytical Chemistry and Chromatography
- Catalytic C–H Functionalization Methods
- Traditional and Medicinal Uses of Annonaceae
- Porphyrin and Phthalocyanine Chemistry
- Sesquiterpenes and Asteraceae Studies
- Phosphorus compounds and reactions
- Click Chemistry and Applications
University of Dundee
2003-2024
University of Canterbury
2020-2024
University of Glasgow
2011-2022
Xi’an Jiaotong-Liverpool University
2015-2018
Glasgow Life
2014-2015
Syngenta (United Kingdom)
2011
University of Bath
2011
Pfizer (United Kingdom)
2011
Syngenta (Switzerland)
2007
MRC Protein Phosphorylation and Ubiquitylation Unit
2007
We detected a protein in rabbit skeletal muscle extracts that was phosphorylated rapidly by SGK1 (serum- and glucocorticoid-induced kinase 1), but not Bα, identified it as NDRG2 (N-myc downstream-regulated gene 2). at Thr330, Ser332 Thr348in vitro. All three residues were from wild-type mice, mice do express SGK1. also the related NDRG1 isoform Thr328, Ser330 Thr346 (equivalent to Thr348 of NDRG2), well Thr356 Thr366. Residues Thr346, Thr366 are located within identical decapeptide sequences...
The compound BIRB796 inhibits the stress-activated protein kinases p38alpha and p38beta is undergoing clinical trials for treatment of inflammatory diseases. Here we report that also activity activation SAPK3/p38gamma. This occurs at higher concentrations than those inhibit lower JNK isoforms. We show these concentrations, blocks stress-induced phosphorylation scaffold SAP97, further establishing this a physiological substrate Our results demonstrate BIRB796, in combination with SB203580,...
Following macrolactonization, a Sonogashira coupling leads efficiently from 1 and 2 to the aglycon of structurally unique cytotoxic macrolide callipeltoside A, isolated in tiny quantities lithistid sponge Callipelta sp. Key steps preparation precursor include boron-mediated anti-aldol (A) tandem with Yamamoto's vinylogous aldol reaction (B). TES=triethylsilyl.
FFA2 is a G protein-coupled receptor that responds to short chain fatty acids and has generated interest as therapeutic target for metabolic inflammatory conditions. However, definition of its functions been slowed by dearth selective ligands can distinguish it from the closely related FFA3. At present, only described suffer poor potency, altered signaling due allosteric modes action, or lack function at non-human orthologs receptor. To address need novel ligands, we synthesized two...
AbstractVX-680, also known as MK-0457, is a member of diverse group small molecules that inhibit the Aurora kinases, and has shown significant potential an anti-cancer agent. In keeping with many protein kinase inhibitors, this compound not monospecific agent, its cellular specificity remains largely unknown. cells, VX-680 blocks mitotic Histone H3 phosphorylation induces polyploidy apoptosis, consistent inhibition B. study, we have investigated effects in proliferating human cancer...
Aberrant mitogen/extracellular signal-regulated kinase 5 (MEK5)–extracellular protein (ERK5)-mediated signalling has been implicated in a number of tumour types including prostate cancer (PCa). The molecular basis ERK5-driven carcinogenesis and its clinical relevance remain to be fully characterised. Modulation ERK5 expression or function human PCa PC3 PC3–ERK5 (stably transfected with ERK5) cells was performed using siRNA-mediated knockdown the MEK inhibitor PD18435 respectively. In vitro...
Abnormal expression of the hepatic gluconeogenic genes (glucose-6-phosphatase [G6Pase] and PEPCK) contributes to hyperglycemia. These are repressed by insulin, but this process is defective in diabetic subjects. Protein kinase B (PKB) implicated action insulin. An inhibitor PKB, Akt (Akti)-1/2, was recently reported; however, specificity efficacy against insulin-induced PKB not reported. Our aim characterize Akti-1/2 cells exposed insulin then establish whether inhibition sufficient prevent...
A highly stereocontrolled total synthesis of the cytotoxic macrolide (−)-callipeltoside has been achieved in 23 steps (4.8% overall). Notable features include a novel asymmetric vinylogous aldol reaction to install C13 stereocenter and (E)-trisubstituted alkene, an anti-selective addition, Sonogashira coupling, and, last, Schmidt-type glycosylation attach sugar unit.
The biomimetic synthesis of the bicyclic core novel immunosuppresants SNF4435C and SNF4435D is reported. framework was efficiently generated from all-trans tetraene precursor in one step good yield.
ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTRegiocontrolled Rearrangement of IsobenzofuransBen A. Egan†, Michael Paradowski‡, Lynne H. Thomas§, and Rodolfo Marquez†∥View Author Information WestCHEM, University Glasgow, Joseph Black Building, Avenue, Glasgow G12 8QQ, United Kingdom, Pfizer Global R&D, Sandwich, Kent CT13 9NJ, Department Chemistry, Bath, Bath BA2 7AY, Kingdom[email protected]†University Glasgow.‡Pfizer R&D.§University Bath.∥Ian Sword Reader Organic Chemistry EPSRC Leadership...
The malaria-causing blood stage of Plasmodium falciparum requires extracellular pantothenate for proliferation. parasite converts into coenzyme A (CoA) via five enzymes, the first being a kinase (PfPanK). Multiple antiplasmodial analogues, including pantothenol and CJ-15,801, kill by targeting CoA biosynthesis/utilisation. Their mechanism action, however, remains unknown. Here, we show that parasites pressured with or CJ-15,801 become resistant to these analogues. Whole-genome sequencing...
The biomimetic synthesis of the bisesquiterpene lactones (±)-biatractylolide 1 and (±)-biepiasterolide 2 via dimerization captodative stabilized radical 8 is reported. Atractylon 7 has also been shown to be a possible intermediate during biosynthesis biatractylolide 1, biepiasterolide 2, atractylolide 3, hydroxyatractylolide 4.
We present a new facet of isobenzofuran chemistry which allows for its efficient manipulation to generate biologically relevant entities. This methodology has been successfully applied toward the synthesis ajudazol A.
The nonaldol aldol process developed in our laboratories has been applied to the synthesis of a C1−C11 fragment 22 novel macrocyclic cytotoxic agents tedanolide and 13-deoxytedanolide 1 2. commercially available hydroxy ester 7 was converted 24 steps into compound using two reactions.
Abstract Background Hepatic expression of several gene products involved in glucose metabolism, including phosphoenolpyruvate carboxykinase (PEPCK), glucose-6-phosphatase (G6Pase) and insulin-like growth factor binding protein-1 (IGFBP-1), is rapidly completely inhibited by insulin. This inhibition mediated through the regulation a DNA element present each these promoters, that we call T hymine-rich I nsulin R esponse E lement (TIRE). The insulin signalling pathway results promoters requires...
[reaction: see text] A fast, flexible, and efficient approach for the stereocontrolled synthesis of enamides has been developed starting from lactams amides through use imides. This new provides access to enamide systems not easily or currently accessible other approaches.
Novel azido- and amino-functionalised fluorescent probes based on the BODIPY framework have been developed. The can be easily cheaply synthesised, exhibit highly desirable properties, are amenable to 'click' peptide chemistry methodologies. These provide a stable readily available tool for visualisation of both solution solid supported events.