Quantitative, titratable and high-throughput reporter assays to measure DNA double strand break repair activity in cells
Rajendra, Eeson, Grande, Diego, Mason, Bethany, Di Marcantonio, Daniela, Armstrong, Lucy, Hewitt, Graeme, Elinati, Elias, Galbiati, Alessandro, Boulton, Simon J, Heald, Robert A, Smith, Graeme C M, Robinson, Helen M R
Published in Nucleic acids research (28.02.2024)
Published in Nucleic acids research (28.02.2024)
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Antitumor Polycyclic Acridines. 20. Search for DNA Quadruplex Binding Selectivity in a Series of 8,13-Dimethylquino[4,3,2-kl]acridinium Salts: Telomere- Targeted Agents
Cheng, Mai-Kim, Modi, Chetna, Cookson, Jennifer C, Hutchinson, Ian, Heald, Robert A, McCarroll, Andrew J, Missailidis, Sotiris, Tanious, Farial, Wilson, W. David, Mergny, Jean-Louis, Laughton, Charles A, Stevens, Malcolm F. G
Published in Journal of medicinal chemistry (28.02.2008)
Published in Journal of medicinal chemistry (28.02.2008)
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Pharmacodynamics of the G-Quadruplex-Stabilizing Telomerase Inhibitor 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in Vitro: Activity in Human Tumor Cells Correlates with Telomere Length and Can Be Enhanced, or Antagonized, with Cytotoxic Agents
Cookson, Jennifer C, Dai, Fangping, Smith, Victoria, Heald, Robert A, Laughton, Charles A, Stevens, Malcolm F G, Burger, Angelika M
Published in Molecular pharmacology (01.12.2005)
Published in Molecular pharmacology (01.12.2005)
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Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance
Zatreanu, Diana, Robinson, Helen M. R., Alkhatib, Omar, Boursier, Marie, Finch, Harry, Geo, Lerin, Grande, Diego, Grinkevich, Vera, Heald, Robert A., Langdon, Sophie, Majithiya, Jayesh, McWhirter, Claire, Martin, Niall M. B., Moore, Shaun, Neves, Joana, Rajendra, Eeson, Ranzani, Marco, Schaedler, Theresia, Stockley, Martin, Wiggins, Kimberley, Brough, Rachel, Sridhar, Sandhya, Gulati, Aditi, Shao, Nan, Badder, Luned M., Novo, Daniela, Knight, Eleanor G., Marlow, Rebecca, Haider, Syed, Callen, Elsa, Hewitt, Graeme, Schimmel, Joost, Prevo, Remko, Alli, Christina, Ferdinand, Amanda, Bell, Cameron, Blencowe, Peter, Bot, Chris, Calder, Mathew, Charles, Mark, Curry, Jayne, Ekwuru, Tennyson, Ewings, Katherine, Krajewski, Wojciech, MacDonald, Ellen, McCarron, Hollie, Pang, Leon, Pedder, Chris, Rigoreau, Laurent, Swarbrick, Martin, Wheatley, Ed, Willis, Simon, Wong, Ai Ching, Nussenzweig, Andre, Tijsterman, Marcel, Tutt, Andrew, Boulton, Simon J., Higgins, Geoff S., Pettitt, Stephen J., Smith, Graeme C. M., Lord, Christopher J.
Published in Nature communications (17.06.2021)
Published in Nature communications (17.06.2021)
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Hanan, Emily J., Braun, Marie-Gabrielle, Heald, Robert A., MacLeod, Calum, Chan, Connie, Clausen, Saundra, Edgar, Kyle A., Eigenbrot, Charles, Elliott, Richard, Endres, Nicholas, Friedman, Lori S., Gogol, Emily, Gu, Xiao-Hui, Thibodeau, Rebecca Hong, Jackson, Philip S., Kiefer, James R., Knight, Jamie D., Nannini, Michelle, Narukulla, Raman, Pace, Amanda, Pang, Jodie, Purkey, Hans E., Salphati, Laurent, Sampath, Deepak, Schmidt, Stephen, Sideris, Steve, Song, Kyung, Sujatha-Bhaskar, Swathi, Ultsch, Mark, Wallweber, Heidi, Xin, Jianfeng, Yeap, SiewKuen, Young, Amy, Zhong, Yu, Staben, Steven T.
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Antitumor Polycyclic Acridines. 8. Synthesis and Telomerase-Inhibitory Activity of Methylated Pentacyclic Acridinium Salts
Heald, Robert A, Modi, Chetna, Cookson, Jenny C, Hutchinson, Ian, Laughton, Charles A, Gowan, Sharon M, Kelland, Lloyd R, Stevens, Malcolm F. G
Published in Journal of medicinal chemistry (31.01.2002)
Published in Journal of medicinal chemistry (31.01.2002)
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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity
Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta
Stockley, Martin L., Ferdinand, Amanda, Benedetti, Giovanni, Blencowe, Peter, Boyd, Susan M., Calder, Mat, Charles, Mark D., Edwardes, Lucy V., Ekwuru, Tennyson, Finch, Harry, Galbiati, Alessandro, Geo, Lerin, Grande, Diego, Grinkevich, Vera, Holliday, Nicholas D., Krajewski, Wojciech W., MacDonald, Ellen, Majithiya, Jayesh B., McCarron, Hollie, McWhirter, Claire L., Patel, Viral, Pedder, Chris, Rajendra, Eeson, Ranzani, Marco, Rigoreau, Laurent J. M., Robinson, Helen M. R., Schaedler, Theresia, Sirina, Julija, Smith, Graeme C. M., Swarbrick, Martin E., Turnbull, Andrew P., Willis, Simon, Heald, Robert A.
Published in Journal of medicinal chemistry (27.10.2022)
Published in Journal of medicinal chemistry (27.10.2022)
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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)
Heffron, Timothy P, Heald, Robert A, Ndubaku, Chudi, Wei, BinQing, Augistin, Martin, Do, Steven, Edgar, Kyle, Eigenbrot, Charles, Friedman, Lori, Gancia, Emanuela, Jackson, Philip S, Jones, Graham, Kolesnikov, Aleksander, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, McLean, Neville, Mörtl, Mario, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Staben, Steven T, Steinbacher, Stefan, Tsui, Vickie, Wallin, Jeffrey, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Small-Molecule Polθ Inhibitors Provide Safe and Effective Tumor Radiosensitization in Preclinical Models
Rodriguez-Berriguete, Gonzalo, Ranzani, Marco, Prevo, Remko, Puliyadi, Rathi, Machado, Nicole, Bolland, Hannah R, Millar, Val, Ebner, Daniel, Boursier, Marie, Cerutti, Aurora, Cicconi, Alessandro, Galbiati, Alessandro, Grande, Diego, Grinkevich, Vera, Majithiya, Jayesh B, Piscitello, Desiree, Rajendra, Eeson, Stockley, Martin L, Boulton, Simon J, Hammond, Ester M, Heald, Robert A, Smith, Graeme C M, Robinson, Helen M R, Higgins, Geoff S
Published in Clinical cancer research (14.04.2023)
Published in Clinical cancer research (14.04.2023)
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Correction to “Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta”
Stockley, Martin L., Benedetti, Giovanni, Blencowe, Peter, Boulton, Simon J., Boyd, Susan M., Calder, Mat, Charles, Mark D., Edwardes, Lucy V., Ekwuru, Tennyson, Ferdinand, Amanda, Finch, Harry, Galbiati, Alessandro, Geo, Lerin, Grande, Diego, Grinkevich, Vera, Higgins, Geoff S., Holliday, Nicholas D., Krajewski, Wojciech W., MacDonald, Ellen, Majithiya, Jayesh B., McCarron, Hollie, McWhirter, Claire L., Patel, Viral, Pedder, Chris, Rajendra, Eeson, Ranzani, Marco, Rigoreau, Laurent J. M., Robinson, Helen M. R., Schaedler, Theresia, Sirina, Julija, Smith, Graeme C. M., Swarbrick, Martin E., Turnbull, Andrew P., Willis, Simon, Zemla, Aleksandra, Heald, Robert A.
Published in Journal of medicinal chemistry (09.03.2023)
Published in Journal of medicinal chemistry (09.03.2023)
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Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Hanan, Emily J, Eigenbrot, Charles, Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Dotson, Jennafer, Heald, Robert A, Jackson, Philip S, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Tam, Christine, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yin, Jianping, Yu, Christine, Zilberleyb, Inna, Heffron, Timothy P
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor
Chan, Bryan K, Hanan, Emily J, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dela Vega, Trisha, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard L, Heald, Robert A, Jackson, Philip S, Knight, Jamie D, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions
Heald, Robert A, Jackson, Philip, Savy, Pascal, Jones, Mark, Gancia, Emanuela, Burton, Brenda, Newman, Richard, Boggs, Jason, Chan, Emily, Chan, Jocelyn, Choo, Edna, Merchant, Mark, Rudewicz, Patrick, Ultsch, Mark, Wiesmann, Christian, Yue, Qin, Belvin, Marcia, Price, Steve
Published in Journal of medicinal chemistry (24.05.2012)
Published in Journal of medicinal chemistry (24.05.2012)
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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles
Safina, Brian S, Elliott, Richard L, Forrest, Andrew K, Heald, Robert A, Murray, Jeremy M, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Seward, Eileen M, Staben, Steven T, Ultsch, Mark, Wei, Binqing, Yang, Wenqian, Sutherlin, Daniel P
Published in ACS medicinal chemistry letters (14.09.2017)
Published in ACS medicinal chemistry letters (14.09.2017)
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5-Aminopyrimidin-2-ylnitriles as Cathepsin K inhibitors
MORLEY, Andrew D, KENNY, Peter W, WARD, Stuart, WILKINSON, Tina J, BURTON, Brenda, HEALD, Robert A, MACFAUL, Philip A, MULLETT, Julia, PAGE, Ken, PORRES, Soraya S, ROSENBRIER RIBEIRO, Lyn, SMITH, Phil
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
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Conformationally Restricted Analogues of Psorospermin: Design, Synthesis, and Bioactivity of Natural-Product-Related Bisfuranoxanthones
Heald, Robert A, Dexheimer, Thomas S, Vankayalapati, Hariprasad, Siddiqui-Jain, Adam, Szabo, Lajos Z, Gleason-Guzman, Mary C, Hurley, Laurence H
Published in Journal of medicinal chemistry (21.04.2005)
Published in Journal of medicinal chemistry (21.04.2005)
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