Search Results - "Massey, Andrew J"

A high content, high throughput cellular thermal stability assay for measuring drug-target engagement in living cells by Massey, Andrew J

“…Determining and understanding drug target engagement is critical for drug discovery. This can be challenging within living cells as selective readouts are…”
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Chk1 inhibition as a novel therapeutic strategy for treating triple-negative breast and ovarian cancers by Bryant, Christopher, Rawlinson, Rebecca, Massey, Andrew J

“…Chk1 inhibitors are currently in clinical trials as putative potentiators of cytotoxic chemotherapy drugs. Chk1 inhibitors may exhibit single agent anti-tumor…”
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Multiparametric Cell Cycle Analysis Using the Operetta High-Content Imager and Harmony Software with PhenoLOGIC by Massey, Andrew J

“…High-content imaging is a powerful tool for determining cell phenotypes at the single cell level. Characterising the effect of small molecules on cell cycle…”
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Knockdown of PAK4 or PAK1 inhibits the proliferation of mutant KRAS colon cancer cells independently of RAF/MEK/ERK and PI3K/AKT signaling by Tabusa, Hana, Brooks, Teresa, Massey, Andrew J

“…The p21-activated kinase (PAK) serine/threonine kinases are important effectors of the small GTPases Rac and Cdc42, and play significant roles in controlling…”
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novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells by Massey, Andrew J, Williamson, Douglas S, Browne, Helen, Murray, James B, Dokurno, Pawel, Shaw, Terry, Macias, Alba T, Daniels, Zoe, Geoffroy, Stephanie, Dopson, Melanie, Lavan, Paul, Matassova, Natalia, Francis, Geraint L, Graham, Christopher J, Parsons, Rachel, Wang, Yikang, Padfield, Antony, Comer, Mike, Drysdale, Martin J, Wood, Mike

“…Purpose The anti-apoptotic function of the 70 kDa family of heat shock proteins and their role in cancer is well documented. Dual targeting of Hsc70 and Hsp70…”
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The GPCR adaptor protein Norbin regulates S1PR1 trafficking and the morphology, cell cycle and survival of PC12 cells by Johansen, Valdemar B. I., Hampson, Elizabeth, Tsonou, Elpida, Pantarelli, Chiara, Chu, Julia Y., Crossland, Laraine, Okkenhaug, Hanneke, Massey, Andrew J., Hornigold, David C., Welch, Heidi C. E., Chetwynd, Stephen A.

“…Norbin is an adaptor protein that binds numerous G protein-coupled receptors (GPCRs), is highly expressed in neurons, and is essential for a functioning…”
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ATPases as Drug Targets: Insights from Heat Shock Proteins 70 and 90 by Massey, Andrew J

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Checkpoint Kinase 1 (Chk1) inhibition fails to activate the Stimulator of Interferon Genes (STING) innate immune signalling in a human coculture cancer system by Brooks, Teresa, Wayne, Joanne, Massey, Andrew J.

“…Utilising Checkpoint Kinase 1 (Chk1) inhibitors to increase cytoplasmic DNA may be a potential strategy to increase the sensitivity of tumours to immune…”
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Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800 by Massey, Andrew J, Schoepfer, Joseph, Brough, Paul A, Brueggen, Josef, Chène, Patrick, Drysdale, Martin J, Pfaar, Ulrike, Radimerski, Thomas, Ruetz, Stephan, Schweitzer, Alain, Wood, Mike, Garcia-Echeverria, Carlos, Jensen, Michael Rugaard

“…Heat shock protein 90 (Hsp90) is a ubiquitously expressed molecular chaperone with ATPase activity involved in the conformational maturation and stability of…”
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Targeting DNA damage response pathways to activate the STING innate immune signaling pathway in human cancer cells by Wayne, Joanne, Brooks, Teresa, Landras, Alexandra, Massey, Andrew J.

“…Activating stimulator of interferon genes to turn immunologically refractive cold tumor hot is an exciting therapeutic approach to increase the clinical…”
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Inhibition of ATR-dependent feedback activation of Chk1 sensitises cancer cells to Chk1 inhibitor monotherapy by Massey, Andrew J

“…Abstract The Chk1 and ATR kinases are critical mediators of the DNA damage response pathway and help protect cancer cells from endogenous and oncogene induced…”
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Chk1 inhibition induces a DNA damage bystander effect in cocultured tumour cells by Brooks, Teresa, Wayne, Joanne, Massey, Andrew J.

“…•Chk1 inhibitors induced DNA damage in THP1 and Jurkat cells.•Chk1i treated cells induce a DNA damage bystander effect in untreated co-cultured…”
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Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage by Massey, Andrew J.

“…Chk1 kinase inhibitors are currently under clinical investigation as potentiators of cytotoxic chemotherapy and demonstrate potent activity in combination with…”
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Context-dependent cell cycle checkpoint abrogation by a novel kinase inhibitor by Massey, Andrew J, Borgognoni, Jenifer, Bentley, Carol, Foloppe, Nicolas, Fiumana, Andrea, Walmsley, Lee

“…Checkpoint kinase 1 and 2 (Chk1/Chk2), and the Aurora kinases play a critical role in the activation of the DNA damage response and mitotic spindle…”
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Targeting DYRK1A/B kinases to modulate p21‐cyclin D1‐p27 signalling and induce anti‐tumour activity in a model of human glioblastoma by Massey, Andrew J., Benwell, Karen, Burbridge, Mike, Kotschy, Andras, Walmsley, David Lee

“…The dual‐specificity tyrosine‐regulated kinases DYRK1A and DYRK1B play a key role in controlling the quiescence‐proliferation switch in cancer cells. Serum…”
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Tumour growth environment modulates Chk1 signalling pathways and Chk1 inhibitor sensitivity by Massey, Andrew J.

“…Clinical development of Chk1 inhibitors is currently focussed on evaluating activity as monotherapy and as potentiators of chemotherapy. To aid translation of…”
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γH2AX and Chk1 phosphorylation as predictive pharmacodynamic biomarkers of Chk1 inhibitor-chemotherapy combination treatments by Rawlinson, Rebecca, Massey, Andrew J

“…Chk1 inhibitors are currently in clinical trials in combination with a range of cytotoxic agents and have the potential to potentiate the clinical activity of…”
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Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B by Lee Walmsley, David, Murray, James B, Dokurno, Pawel, Massey, Andrew J, Benwell, Karen, Fiumana, Andrea, Foloppe, Nicolas, Ray, Stuart, Smith, Julia, Surgenor, Allan E, Edmonds, Thomas, Demarles, Didier, Burbridge, Mike, Cruzalegui, Francisco, Kotschy, Andras, Hubbard, Roderick E

“…The serine/threonine kinase DYRK1A has been implicated in regulation of a variety of cellular processes associated with cancer progression, including cell…”
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Inhibition of Chk1 with the small molecule inhibitor V158411 induces DNA damage and cell death in an unperturbed S-phase by Wayne, Joanne, Brooks, Teresa, Massey, Andrew J

“…Chk1 kinase is a critical component of the DNA damage response checkpoint and Chk1 inhibitors are currently under clinical investigation. Chk1 suppresses…”
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Inhibition of the checkpoint kinase Chk1 induces DNA damage and cell death in human Leukemia and Lymphoma cells by Bryant, Christopher, Scriven, Kirsten, Massey, Andrew J

“…Chk1 forms a core component of the DNA damage response and small molecule inhibitors are currently being investigated in the clinic as cytotoxic chemotherapy…”
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