Search Results - "Flanagan, Jack U"

Glutathione transferases by HAYES, John D, FLANAGAN, Jack U, JOWSEY, Ian R

“…This review describes the three mammalian glutathione transferase (GST) families, namely cytosolic, mitochondrial, and microsomal GST, the latter now…”
Get full text

Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed by Yosaatmadja, Yuliana, Silva, Shevan, Dickson, James M., Patterson, Adam V., Smaill, Jeff B., Flanagan, Jack U., McKeage, Mark J., Squire, Christopher J.

“…The discovery of genetic drivers of lung cancer in patient sub-groups has led to their use as predictive biomarkers and as targets for selective drug therapy…”
Get full text

Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality by Chan, Denise A, Sutphin, Patrick D, Nguyen, Phuong, Turcotte, Sandra, Lai, Edwin W, Banh, Alice, Reynolds, Gloria E, Chi, Jen-Tsan, Wu, Jason, Solow-Cordero, David E, Bonnet, Muriel, Flanagan, Jack U, Bouley, Donna M, Graves, Edward E, Denny, William A, Hay, Michael P, Giaccia, Amato J

“…Identifying new targeted therapies that kill tumor cells while sparing normal tissue is a major challenge of cancer research. Using a high-throughput chemical…”
Get more information

Inhibitors of Discoidin Domain Receptor (DDR) Kinases for Cancer and Inflammation by Denny, William A, Flanagan, Jack U

“…The discoidin domain receptor tyrosine kinases DDR1 and DDR2 are distinguished from other kinase enzymes by their extracellular domains, which interact with…”
Get full text

Diverse mechanisms activate the PI 3-kinase/mTOR pathway in melanomas: implications for the use of PI 3-kinase inhibitors to overcome resistance to inhibitors of BRAF and MEK by Tran, Khanh B, Kolekar, Sharada, Jabed, Anower, Jaynes, Patrick, Shih, Jen-Hsing, Wang, Qian, Flanagan, Jack U, Rewcastle, Gordon W, Baguley, Bruce C, Shepherd, Peter R

“…The PI 3-kinase (PI3K) pathway has been implicated as a target for melanoma therapy. Given the high degree of genetic heterogeneity in melanoma, we sought to…”
Get full text

A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types by Jamieson, Stephen, Flanagan, Jack U, Kolekar, Sharada, Buchanan, Christina, Kendall, Jackie D, Lee, Woo-Jeong, Rewcastle, Gordon W, Denny, William A, Singh, Ripudaman, Dickson, James, Baguley, Bruce C, Shepherd, Peter R

“…Genetic alterations in PI3K (phosphoinositide 3-kinase) signalling are common in cancer and include deletions in PTEN (phosphatase and tensin homologue deleted…”
Get more information

Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions by Tomek, Petr, Palmer, Brian D., Flanagan, Jack U., Sun, Chuanwen, Raven, Emma L., Ching, Lai-Ming

“…High expression of the immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO1) for a broad range of malignancies is associated with poor patient…”
Get full text

Influence of Aldo-keto Reductase 1C3 in Prostate Cancer - A Mini Review by Karunasinghe, Nishi, Masters, Jonathan, Flanagan, Jack U, Ferguson, Lynnette R

“…Aldo-keto reductase 1C3 (AKR1C3) is an important oxidoreductase with multiple substrates, that are involved in producing extra-testicular androgens. Its…”
Get more information

Structure, function and inhibition of the phosphoinositide 3-kinase p110α enzyme by Flanagan, Jack U, Shepherd, Peter R

“…The PI3K (phosphoinositide 3-kinase) p110α isoform is activated by oncogenic mutations in many cancers. This has stimulated intense interest in identifying…”
Get more information

Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2 by Tijono, Sofian M, Palmer, Brian D, Tomek, Petr, Flanagan, Jack U, Henare, Kimiora, Gamage, Swarna, Braun, Lukas, Ching, Lai-Ming

“…Indoleamine 2, 3-dioxygenase 1 (IDO1) is commonly expressed by cancers as a mechanism for evading the immune system. Preclinical and clinical studies have…”
Get full text

Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3 by Flanagan, Jack U, Yosaatmadja, Yuliana, Teague, Rebecca M, Chai, Matilda Z L, Turnbull, Andrew P, Squire, Christopher J

“…Aldo-keto reductase 1C3 (AKR1C3) catalyses the NADPH dependent reduction of carbonyl groups in a number of important steroid and prostanoid molecules. The…”
Get full text

Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3) by Brooke, Darby G., van Dam, Ellen M., Watts, Colin K.W., Khoury, Amanda, Dziadek, Marie A., Brooks, Hilary, Graham, Lisa-Jane K., Flanagan, Jack U., Denny, William A.

“…High-throughput screening of a small-molecule library identified a 5-triazolo-2-arylpyridazinone as a novel inhibitor of the important glycolytic enzyme…”
Get full text

Inhibition of NMDA receptor function with an anti-GluN1-S2 antibody impairs human platelet function and thrombosis by Green, Taryn N., Hamilton, Justin R., Morel-Kopp, Marie-Christine, Zheng, Zhaohua, Chen, Ting-Yu T., Hearn, James I., Sun, Peng P., Flanagan, Jack U., Young, Deborah, Barber, P. Alan, During, Matthew J., Ward, Christopher M., Kalev-Zylinska, Maggie L.

“…GluN1 is a mandatory component of N-methyl-D-aspartate receptors (NMDARs) best known for their roles in the brain, but with increasing evidence for relevance…”
Get full text

DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular by Buchanan, Christina M, Shih, Jen-Hsing, Astin, Jonathan W, Rewcastle, Gordon W, Flanagan, Jack U, Crosier, Philip S, Shepherd, Peter R

“…The flavone acetic acid derivative DMXAA [5,6-dimethylXAA (xanthenone-4-acetic acid), Vadimezan, ASA404] is a drug that displayed vascular-disrupting activity…”
Get more information

SAR studies of 4-pyridyl heterocyclic anilines that selectively induce autophagic cell death in von Hippel-Lindau-deficient renal cell carcinoma cells by Bonnet, Muriel, Flanagan, Jack U., Chan, Denise A., Lai, Edwin W., Nguyen, Phuong, Giaccia, Amato J., Hay, Michael P.

“…We recently identified a class of pyridyl aniline thiazoles (PAT) that displayed selective cytotoxicity for von Hippel-Lindau (VHL) deficient renal cell…”
Get full text

Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1 by Trevarton, AlexanderJ, Zhou, Yan, Yang, Dehua, Rewcastle, Gordon W., Flanagan, Jack U., Braithwaite, Antony, Shepherd, Peter R., Print, Cristin G., Wang, Ming-Wei, Lasham, Annette

“…We have previously shown that high expression of the nucleic acid binding factor YB-1 is strongly associated with poor prognosis in a variety of cancer types…”
Get full text

Small-molecule CSF1R kinase inhibitors; review of patents 2015-present by Denny, William A, Flanagan, Jack U

“…Colony stimulating factor 1 receptor (CSF-1R, also known as c-FMS kinase) is in the class III receptor tyrosine kinase family, along with c-Kit, Flt3 and…”
Get more information

Residues Glutamate 216 and Aspartate 301 Are Key Determinants of Substrate Specificity and Product Regioselectivity in Cytochrome P450 2D6 by Paine, Mark J.I., McLaughlin, Lesley A., Flanagan, Jack U., Kemp, Carol A., Sutcliffe, Michael J., Roberts, Gordon C.K., Wolf, C. Roland

“…Cytochrome P450 2D6 (CYP2D6) metabolizes a wide range of therapeutic drugs. CYP2D6 substrates typically contain a basic nitrogen atom, and the active-site…”
Get full text

Evidence That GRIN2A Mutations in Melanoma Correlate with Decreased Survival by D'mello, Stacey Ann N, Flanagan, Jack U, Green, Taryn N, Leung, Euphemia Y, Askarian-Amiri, Marjan E, Joseph, Wayne R, McCrystal, Michael R, Isaacs, Richard J, Shaw, James H F, Furneaux, Christopher E, During, Matthew J, Finlay, Graeme J, Baguley, Bruce C, Kalev-Zylinska, Maggie L

“…Previous whole-exome sequencing has demonstrated that melanoma tumors harbor mutations in the GRIN2A gene. GRIN2A encodes the regulatory GluN2A subunit of the…”
Get full text

A Structure‐Activity Investigation of the Fungal Metabolite (−)‐TAN‐2483B: Inhibition of Bruton's Tyrosine Kinase by McCone, Jordan A. J., Teesdale‐Spittle, Paul H., Flanagan, Jack U., Harvey, Joanne E.

“…The natural product (−)‐TAN‐2483B is a fungal secondary metabolite which displays promising anti‐cancer and immunomodulatory activity. Our previous syntheses…”
Get full text