Search Results - "Smaill, B."

New Promise and Opportunities for Allosteric Kinase Inhibitors by Lu, Xiaoyun, Smaill, Jeff B., Ding, Ke

“…Drugs that function through allosteric inhibition of kinase signaling represent a promising approach for the targeted discovery of therapeutics. The majority…”
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Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry by Lu, Xiaoyun, Yu, Lei, Zhang, Zhang, Ren, Xiaomei, Smaill, Jeff B., Ding, Ke

“…Both the first‐generation reversible epidermal growth factor receptor (EGFR) inhibitors gefitinib and erlotinib and the second‐generation covalent epidermal…”
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Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects by Lu, Xiaoyun, Chen, Hao, Patterson, Adam V, Smaill, Jeff B, Ding, Ke

“…Hepatocellular carcinoma (HCC) is a lethal disease with limited therapeutic options and a particularly poor prognosis. Aberrant fibroblast growth factor 19…”
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TAS‐120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure by Kalyukina, Maria, Yosaatmadja, Yuliana, Middleditch, Martin J., Patterson, Adam V., Smaill, Jeff B., Squire, Christopher J.

“…1‐[(3S)‐3‐[4‐Amino‐3‐[2‐(3,5‐dimethoxyphenyl)ethynyl]‐1H‐pyrazolo[3,4‐d]pyrimidin‐1‐yl]‐1‐pyrrolidinyl]‐2‐propen‐1‐one (TAS‐120) is an irreversible inhibitor…”
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Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes by Estrada-Bernal, Adriana, Le, Anh T, Doak, Andrea E, Tirunagaru, Vijaya G, Silva, Shevan, Bull, Matthew R, Smaill, Jeff B, Patterson, Adam V, Kim, Chul, Liu, Stephen V, Doebele, Robert C

“…Approved therapies for exon 20, mutations, and fusions are currently lacking for non-small cell lung cancer and other cancers. Tarloxotinib is a prodrug that…”
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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…”
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Tumour Hypoxia-Mediated Immunosuppression: Mechanisms and Therapeutic Approaches to Improve Cancer Immunotherapy by Fu, Zhe, Mowday, Alexandra M, Smaill, Jeff B, Hermans, Ian F, Patterson, Adam V

“…The magnitude of the host immune response can be regulated by either stimulatory or inhibitory immune checkpoint molecules. Receptor-ligand binding between…”
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Nitroreductase gene-directed enzyme prodrug therapy: insights and advances toward clinical utility by Williams, Elsie M, Little, Rory F, Mowday, Alexandra M, Rich, Michelle H, Chan-Hyams, Jasmine V E, Copp, Janine N, Smaill, Jeff B, Patterson, Adam V, Ackerley, David F

“…This review examines the vast catalytic and therapeutic potential offered by type I (i.e. oxygen-insensitive) nitroreductase enzymes in partnership with…”
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Hypoxia-activated prodrugs and (lack of) clinical progress: The need for hypoxia-based biomarker patient selection in phase III clinical trials by Spiegelberg, Linda, Houben, Ruud, Niemans, Raymon, de Ruysscher, Dirk, Yaromina, Ala, Theys, Jan, Guise, Christopher P., Smaill, Jeffrey B., Patterson, Adam V., Lambin, Philippe, Dubois, Ludwig J.

“…•Hypoxia-activated prodrugs have yielded promising results up to phase II trials.•Implementation of hypoxia-activated prodrugs in the clinic has not been…”
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Electrophysiology and 3D-imaging reveal properties of human intracardiac neurons and increased excitability with atrial fibrillation by Ashton, J L, Prince, B, Sands, G, Argent, L, Anderson, M, Smith, J E G, Tedoldi, A, Ahmad, A, Baddeley, D, Pereira, A G, Lever, N, Ramanathan, T, Smaill, B H, Montgomery, Johanna M

“…Altered autonomic input to the heart plays a major role in atrial fibrillation (AF). Autonomic neurons termed ganglionated plexi (GP) are clustered on the…”
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Structural Evaluation of a Nitroreductase Engineered for Improved Activation of the 5-Nitroimidazole PET Probe SN33623 by Sharrock, Abigail V, Mumm, Jeff S, Williams, Elsie M, Čėnas, Narimantas, Smaill, Jeff B, Patterson, Adam V, Ackerley, David F, Bagdžiūnas, Gintautas, Arcus, Vickery L

“…Bacterial nitroreductase enzymes capable of activating imaging probes and prodrugs are valuable tools for gene-directed enzyme prodrug therapies and targeted…”
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Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents by Omran, Ziad, Guise, Chris P., Chen, Linwei, Rauch, Cyril, Abdalla, Ashraf N., Abdullah, Omeima, Sindi, Ikhlas A., Fischer, Peter M., Smaill, Jeff B., Patterson, Adam V., Liu, Yuxiu, Wang, Qingmin

“…Phenanthroindolizidines, such as antofine and tylophorine, are a family of natural alkaloids isolated from different species of Asclepiadaceas. They are…”
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Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling by Jackson-Patel, Victoria, Liu, Emily, Bull, Matthew R, Ashoorzadeh, Amir, Bogle, Gib, Wolfram, Anna, Hicks, Kevin O, Smaill, Jeff B, Patterson, Adam V

“…Hypoxia-activated prodrugs are bioactivated in oxygen-deficient tumour regions and represent a novel strategy to exploit this pharmacological sanctuary for…”
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Subcellular Location of Tirapazamine Reduction Dramatically Affects Aerobic but Not Anoxic Cytotoxicity by Guise, Chris P, Abbattista, Maria R, Anderson, Robert F, Li, Dan, Taghipouran, Rana, Tsai, Angela, Lee, Su Jung, Smaill, Jeff B, Denny, William A, Hay, Michael P, Wilson, William R, Hicks, Kevin O, Patterson, Adam V

“…Hypoxia is an adverse prognostic feature of solid cancers that may be overcome with hypoxia-activated prodrugs (HAPs). Tirapazamine (TPZ) is a HAP which has…”
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The third generation AKR1C3-activated prodrug, ACHM-025, eradicates disease in preclinical models of aggressive T-cell acute lymphoblastic leukemia by Toscan, Cara E., McCalmont, Hannah, Ashoorzadeh, Amir, Lin, Xiaojing, Fu, Zhe, Doculara, Louise, Kosasih, Hansen J., Cadiz, Roxanne, Zhou, Anthony, Williams, Sarah, Evans, Kathryn, Khalili, Faezeh, Cai, Ruilin, Yeats, Kristy L., Gifford, Andrew J., Pickford, Russell, Mayoh, Chelsea, Xie, Jinhan, Henderson, Michelle J., Trahair, Toby N., Patterson, Adam V., Smaill, Jeff B., de Bock, Charles E., Lock, Richard B.

“…T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy that expresses high levels of the enzyme aldo-keto reductase family 1…”
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Restoring Tumour Selectivity of the Bioreductive Prodrug PR-104 by Developing an Analogue Resistant to Aerobic Metabolism by Human Aldo-Keto Reductase 1C3 by Abbattista, Maria R, Ashoorzadeh, Amir, Guise, Christopher P, Mowday, Alexandra M, Mittra, Rituparna, Silva, Shevan, Hicks, Kevin O, Bull, Matthew R, Jackson-Patel, Victoria, Lin, Xiaojing, Prosser, Gareth A, Lambie, Neil K, Dachs, Gabi U, Ackerley, David F, Smaill, Jeff B, Patterson, Adam V

“…PR-104 is a phosphate ester pre-prodrug that is converted in vivo to its cognate alcohol, PR-104A, a latent alkylator which forms potent cytotoxins upon…”
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Interrogation of the Structure-Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications by Ashoorzadeh, Amir, Mowday, Alexandra M, Guise, Christopher P, Silva, Shevan, Bull, Matthew R, Abbattista, Maria R, Copp, Janine N, Williams, Elsie M, Ackerley, David F, Patterson, Adam V, Smaill, Jeff B

“…PR-104A is a dual hypoxia/nitroreductase gene therapy prodrug by virtue of its ability to undergo either one- or two-electron reduction to its cytotoxic…”
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Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations by Lu, Xiaoyun, Smaill, Jeff B, Ding, Ke

“…Clinically acquired resistance to small molecule kinase inhibitors (SMKIs) has become a major “unmet clinical need” in cancer therapy. To date, there are six…”
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Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor:  4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions by Smaill, Jeff B, Rewcastle, Gordon W, Loo, Joseph A, Greis, Kenneth D, Chan, O. Helen, Reyner, Eric L, Lipka, Elke, Showalter, H. D. Hollis, Vincent, Patrick W, Elliott, William L, Denny, William A

“…4-Anilinoquinazoline- and 4-anilinopyrido[3,2-d]pyrimidine-6-acrylamides substituted with solubilizing 7-alkylamine or 7-alkoxyamine side chains were prepared…”
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Successful induction of oestrus, ovulation and pregnancy in adult ewes and ewe lambs out of the breeding season using a GnRH+progesterone oestrus synchronisation protocol by Martinez, M.F., McLeod, B., Tattersfield, G., Smaill, B., Quirke, L.D., Juengel, J.L.

“…•A GnRH+P4-based protocol successfully induced ovulation in anoestrous sheep.•This protocol reduces the length of treatment from 12 to 7 days.•It was shown to…”
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