Search Results - "Kendall, Jackie D"
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A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types
Published in Biochemical journal (15-08-2011)“…Genetic alterations in PI3K (phosphoinositide 3-kinase) signalling are common in cancer and include deletions in PTEN (phosphatase and tensin homologue deleted…”
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2
Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo
Published in Biochemical journal (15-02-2012)“…In in vitro studies class-I PI3Ks (phosphoinositide 3-kinases), class-II PI3Ks and mTOR (mammalian target of rapamycin) have all been described as having roles…”
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3
Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling
Published in Biochemical journal (15-06-2007)“…Recent genetic knock-in and pharmacological approaches have suggested that, of class IA PI3Ks (phosphatidylinositol 3-kinases), it is the p110alpha isoform…”
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4
Potential global fire monitoring from EOS-MODIS
Published in Journal of Geophysical Research, Washington, DC (27-12-1998)“…The National Aeronautic and Space Administration (NASA) plans to launch the moderate resolution imaging spectroradiometer (MODIS) on the polarorbiting Earth…”
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5
Oncogenic mutations of p110α isoform of PI 3-kinase upregulate its protein kinase activity
Published in PloS one (01-08-2013)“…In addition to lipid kinase activity, the class-I PI 3-kinases also function as protein kinases targeting regulatory autophosphorylation sites and exogenous…”
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6
Synthesis and Biological Evaluation of Novel Analogues of the Pan Class I Phosphatidylinositol 3-Kinase (PI3K) Inhibitor 2-(Difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474)
Published in Journal of medicinal chemistry (27-10-2011)“…A structure–activity relationship (SAR) study of the pan class I PI 3-kinase inhibitor…”
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7
Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474
Published in Bioorganic & medicinal chemistry (15-04-2019)“…[Display omitted] Replacing one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety of sulfonamide-linked…”
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Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474
Published in Bioorganic & medicinal chemistry (15-10-2017)“…[Display omitted] Replacement of one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 (1) with sulfonamide containing…”
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9
Formation of fluorophores from the kynurenine pathway metabolite N-formylkynurenine and cyclic amines involves transamidation and carbon–carbon bond formation at the 2-position of the amine
Published in Biochimica et biophysica acta (01-09-2015)“…Tryptophan catabolism along the kynurenine pathway is associated with a number of pathologies including cataract formation and cancer. Whilst the chemical…”
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10
Combining properties of different classes of PI3Kα inhibitors to understand the molecular features that confer selectivity
Published in Biochemical journal (01-07-2017)“…Phosphoinositide 3-kinases (PI3Ks) are major regulators of many cellular functions, and hyperactivation of PI3K cell signalling pathways is a major target for…”
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11
Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-01-2017)“…[Display omitted] As part of our investigation into pyrazolo[1,5-a]pyridines as novel p110α selective PI3 kinase inhibitors, we report a range of analogues…”
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12
Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors
Published in Oncotarget (18-07-2017)“…Multiple therapeutic agents have been developed to target the phosphatidylinositol 3-kinase (PI3K) signaling pathway, which is frequently dysregulated in…”
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13
Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR
Published in Bioorganic & medicinal chemistry (01-01-2012)“…Structure–activity relationship studies of the pyrazolo[1,5-a]pyridine class of PI3 kinase inhibitors show that substitution off the hydrazone nitrogen and…”
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14
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
Published in Bioorganic & medicinal chemistry (01-01-2012)“…We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class…”
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15
Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474)
Published in European journal of medicinal chemistry (01-06-2013)“…A range of 4-substituted derivatives of the pan class I PI 3-kinase inhibitor 2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole…”
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16
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors
Published in Bioorganic & medicinal chemistry (15-12-2007)“…A novel series of sulfonohydrazides were synthesised and evaluated for inhibition of isoforms of PI3K, and inhibition of cell proliferation. Molecular…”
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17
Phosphoinositide-3-kinase (PI3K) inhibitors: Identification of new scaffolds using virtual screening
Published in Bioorganic & medicinal chemistry letters (15-10-2009)“…In the present work, we used virtual screening (VS) of the ZINC database of 2.5 million compounds to seek new PI3K inhibitory scaffolds. The VS flowchart…”
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18
Synthesis and 1H, 13C and 15N NMR characterisation of substituted Pyrazolo[4,3-c]quinolines and related compounds
Published in Tetrahedron (31-05-2018)“…A wide range of novel and known alkyl substituted pyrazolo[4,3-c]quinolines and related compounds were synthesized. Some of these compounds can undergo…”
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19
Synthesis and Biological Evaluation of Novel Analogues of the Pan Class I Phosphatidylinositol 3-Kinase (PI3K) Inhibitor 2-(Difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1 H -benzimidazole (ZSTK474)
Published in Journal of medicinal chemistry (27-10-2011)Get full text
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20
Oncogenic Mutations of p110[alpha] Isoform of PI 3-Kinase Upregulate Its Protein Kinase Activity
Published in PloS one (01-08-2013)“…In addition to lipid kinase activity, the class-I PI 3-kinases also function as protein kinases targeting regulatory autophosphorylation sites and exogenous…”
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