Search Results - "Waddell, Ian D."

Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides by Waszkowycz, Bohdan, Smith, Kate M, McGonagle, Alison E, Jordan, Allan M, Acton, Ben, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, James, Dominic I, Jones, Clifford D, Jones, Stuart, Mould, Daniel P, Small, Helen F, Stowell, Alexandra I. J, Tucker, Julie A, Waddell, Ian D, Ogilvie, Donald J

“…DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The…”
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Toxoflavins and Deazaflavins as the First Reported Selective Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase II by Raoof, Ali, Depledge, Paul, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hopkins, Gemma V, Jordan, Allan M, Maguire, Laura A, McGonagle, Alison E, Mould, Daniel P, Rushbrooke, Mathew, Small, Helen F, Smith, Kate M, Thomson, Graeme J, Turlais, Fabrice, Waddell, Ian D, Waszkowycz, Bohdan, Watson, Amanda J, Ogilvie, Donald J

“…The recently discovered enzyme tyrosyl-DNA phosphodiesterase 2 (TDP2) has been implicated in the topoisomerase-mediated repair of DNA damage. In the clinical…”
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Stimulation of Hepatocyte Glucose Metabolism by Novel Small Molecule Glucokinase Activators by BROCKLEHURST, Katy J, PAYNE, Victoria A, AGIUS, Loranne, DAVIES, Rick A, CARROLL, Debra, VERTIGAN, Helen L, WIGHTMAN, Heather J, ALSTON, Susan, WADDELL, Ian D, LEIGHTON, Brendan, COGHLAN, Matthew P

“…Stimulation of Hepatocyte Glucose Metabolism by Novel Small Molecule Glucokinase Activators Katy J. Brocklehurst 1 , Victoria A. Payne 2 , Rick A. Davies 1 ,…”
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An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells [version 2; peer review: 2 approved] by James, Dominic I, Durant, Stephen, Eckersley, Kay, Fairweather, Emma, Griffiths, Louise A, Hamilton, Nicola, Kelly, Paul, O'Connor, Mark, Shea, Kerry, Waddell, Ian D, Ogilvie, Donald J

“…After a DNA damage signal multiple polymers of ADP ribose attached to poly(ADP) ribose (PAR) polymerases (PARPs) are broken down by the enzyme poly(ADP) ribose…”
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IncucyteDRC: An R package for the dose response analysis of live cell imaging data [version 1; peer review: 2 approved] by Chapman, Philip J, James, Dominic I, Watson, Amanda J, Hopkins, Gemma V, Waddell, Ian D, Ogilvie, Donald J

“…We present IncucyteDRC, an R package for the analysis of data from live cell imaging cell proliferation experiments carried out on the Essen Biosciences…”
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An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells by James, Dominic I, Durant, Stephen, Eckersley, Kay, Fairweather, Emma, Griffiths, Louise A, Hamilton, Nicola, Kelly, Paul, O'Connor, Mark, Shea, Kerry, Waddell, Ian D, Ogilvie, Donald J

“…After a DNA damage signal multiple polymers of ADP ribose attached to poly(ADP) ribose (PAR) polymerases (PARPs) are broken down by the enzyme poly(ADP) ribose…”
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Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade by Watson, Amanda J., Hopkins, Gemma V., Hitchin, Samantha, Begum, Habiba, Jones, Stuart, Jordan, Allan, Holt, Sarah, March, H. Nikki, Newton, Rebecca, Small, Helen, Stowell, Alex, Waddell, Ian D., Waszkowycz, Bohdan, Ogilvie, Donald J.

“…RET (REarranged during Transfection) is a receptor tyrosine kinase, which plays pivotal roles in regulating cell survival, differentiation, proliferation,…”
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Small-Molecule Inhibition of UBE2T/FANCL-Mediated Ubiquitylation in the Fanconi Anemia Pathway by Cornwell, Matthew J, Thomson, Graeme J, Coates, Julia, Belotserkovskaya, Rimma, Waddell, Ian D, Jackson, Stephen P, Galanty, Yaron

“…The Fanconi anemia pathway orchestrates the repair of DNA interstrand cross-links and stalled replication forks. A key step in this pathway is UBE2T and…”
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Regulation of ALT-associated homology-directed repair by polyADP-ribosylation by Hoang, Song My, Kaminski, Nicole, Bhargava, Ragini, Barroso-González, Jonathan, Lynskey, Michelle L., García-Expósito, Laura, Roncaioli, Justin L., Wondisford, Anne R., Wallace, Callen T., Watkins, Simon C., James, Dominic I., Waddell, Ian D., Ogilvie, Donald, Smith, Kate M., da Veiga Leprevost, Felipe, Mellacharevu, Dattatreya, Nesvizhskii, Alexey I., Li, Jianfeng, Ray-Gallet, Dominique, Sobol, Robert W., Almouzni, Genevieve, O’Sullivan, Roderick J.

“…The synthesis of poly(ADP-ribose) (PAR) reconfigures the local chromatin environment and recruits DNA-repair complexes to damaged chromatin. PAR degradation by…”
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Poly (ADP) Ribose Glycohydrolase Can Be Effectively Targeted in Pancreatic Cancer by Jain, Aditi, Agostini, Lebaron C, McCarthy, Grace A, Chand, Saswati N, Ramirez, AnnJosette, Nevler, Avinoam, Cozzitorto, Joseph, Schultz, Christopher W, Lowder, Cinthya Yabar, Smith, Kate M, Waddell, Ian D, Raitses-Gurevich, Maria, Stossel, Chani, Gorman, Yulia Glick, Atias, Dikla, Yeo, Charles J, Winter, Jordan M, Olive, Kenneth P, Golan, Talia, Pishvaian, Michael J, Ogilvie, Donald, James, Dominic I, Jordan, Allan M, Brody, Jonathan R

“…Patients with metastatic pancreatic ductal adenocarcinoma (PDAC) have an average survival of less than 1 year, underscoring the importance of evaluating novel…”
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First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib by James, Dominic I, Smith, Kate M, Jordan, Allan M, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, Jones, Stuart, Kelly, Paul, McGonagle, Alison E, Small, Helen, Stowell, Alexandra I. J, Tucker, Julie, Waddell, Ian D, Waszkowycz, Bohdan, Ogilvie, Donald J

“…The enzyme poly­(ADP-ribose) glycohydrolase (PARG) performs a critical role in the repair of DNA single strand breaks (SSBs). However, a detailed understanding…”
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Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade [version 1; peer review: 4 approved] by Watson, Amanda J, Hopkins, Gemma V, Hitchin, Samantha, Begum, Habiba, Jones, Stuart, Jordan, Allan, Holt, Sarah, March, H. Nikki, Newton, Rebecca, Small, Helen, Stowell, Alex, Waddell, Ian D, Waszkowycz, Bohdan, Ogilvie, Donald J

“…RET (REarranged during Transfection) is a receptor tyrosine kinase, which plays pivotal roles in regulating cell survival, differentiation, proliferation,…”
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Studying Catabolism of Protein ADP-Ribosylation by Palazzo, Luca, James, Dominic I, Waddell, Ian D, Ahel, Ivan

“…Protein ADP-ribosylation is a conserved posttranslational modification that regulates many major cellular functions, such as DNA repair, transcription,…”
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Rethinking ‘academic’ drug discovery: the Manchester Institute perspective by Jordan, Allan M., Waddell, Ian D., Ogilvie, Donald J.

“…•We identify challenges common to academic and charitable drug discovery units.•We propose alternate, creative and accessible solutions to these challenges.•We…”
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Androgen Receptor and Poly(ADP-ribose) Glycohydrolase Inhibition Increases Efficiency of Androgen Ablation in Prostate Cancer Cells by Zhang, Manqi, Lai, Yanhao, Vasquez, Judy L., James, Dominic I., Smith, Kate M., Waddell, Ian D., Ogilvie, Donald J., Liu, Yuan, Agoulnik, Irina U.

“…There is mounting evidence of androgen receptor signaling inducing genome instability and changing DNA repair capacity in prostate cancer cells. Expression of…”
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A high-throughput screening-compatible homogeneous time-resolved fluorescence assay measuring the glycohydrolase activity of human poly(ADP-ribose) glycohydrolase by Stowell, Alexandra I.J., James, Dominic I., Waddell, Ian D., Bennett, Neil, Truman, Caroline, Hardern, Ian M., Ogilvie, Donald J.

“…Poly(ADP-ribose) (PAR) polymers are transient post-translational modifications, and their formation is catalyzed by poly(ADP-ribose) polymerase (PARP) enzymes…”
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The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity by Newton, Rebecca, Bowler, Katherine A., Burns, Emily M., Chapman, Philip J., Fairweather, Emma E., Fritzl, Samantha J.R., Goldberg, Kristin M., Hamilton, Niall M., Holt, Sarah V., Hopkins, Gemma V., Jones, Stuart D., Jordan, Allan M., Lyons, Amanda J., Nikki March, H., McDonald, Neil Q., Maguire, Laura A., Mould, Daniel P., Purkiss, Andrew G., Small, Helen F., Stowell, Alexandra I.J., Thomson, Graeme J., Waddell, Ian D., Waszkowycz, Bohdan, Watson, Amanda J., Ogilvie, Donald J.

“…Deregulation of the receptor tyrosine kinase RET has been implicated in medullary thyroid cancer, a small percentage of lung adenocarcinomas,…”
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Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase by Hamilton, Niall M, Dawson, Martin, Fairweather, Emma E, Hamilton, Nicola S, Hitchin, James R, James, Dominic I, Jones, Stuart D, Jordan, Allan M, Lyons, Amanda J, Small, Helen F, Thomson, Graeme J, Waddell, Ian D, Ogilvie, Donald J

“…Novel derivatives of the steroid DHEA 1, a known uncompetitive inhibitor of G6PD, were designed, synthesized, and tested for their ability to inhibit this…”
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Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – A cautionary disclosure by Acton, Ben, Small, Helen F., Smith, Kate M., McGonagle, Alison, Stowell, Alexandra I.J., James, Dominic I., Hamilton, Niall M., Hamilton, Nicola, Hitchin, James R., Hutton, Colin P., Waddell, Ian D., Ogilvie, Donald J., Jordan, Allan M.

“…[Display omitted] Fluorination of metabolic hotspots in a molecule is a common medicinal chemistry strategy to improve in vivo half-life and exposure and,…”
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TNF-alpha increases ubiquitin-conjugating activity in skeletal muscle by up-regulating UbcH2/E220k by Li, Yi-Ping, Lecker, Stewart H., Chen, Yuling, Waddell, Ian D., Goldberg, Alfred L., Reid, Michael B.

“…In some inflammatory diseases, TNF-alpha is thought to stimulate muscle catabolism via an NF-kappaB-dependent process that increases ubiquitin conjugation to…”
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