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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, Georgia, Haling, Jacob R, Chen, Huifen, Song, Kyung, Price, Steve, Heald, Robert, Hewitt, Joanne F M, Zak, Mark, Peck, Ariana, Orr, Christine, Merchant, Mark, Hoeflich, Klaus P, Chan, Jocelyn, Luoh, Shiuh-Ming, Anderson, Daniel J, Ludlam, Mary J C, Wiesmann, Christian, Ultsch, Mark, Friedman, Lori S, Malek, Shiva, Belvin, Marcia
Published in Nature (London) (12.09.2013)
Published in Nature (London) (12.09.2013)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
Edge effects in mixed conifer group selection openings: tree height response to resource gradients
York, Robert A, Battles, John J, Heald, Robert C
Published in Forest ecology and management (03.07.2003)
Published in Forest ecology and management (03.07.2003)
Get full text
Journal Article