Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform
Staben, Steven T., Ndubaku, Chudi, Blaquiere, Nicole, Belvin, Marcia, Bull, Richard J., Dudley, Danette, Edgar, Kyle, Gray, Daniel, Heald, Robert, Heffron, Timothy P., Jones, Graham E., Jones, Mark, Kolesnikov, Aleks, Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy, McLean, Neville J., Nonomiya, Jim, Olivero, Alan G., Ord, Rachel, Pang, Jodie, Price, Stephen, Prior, Wei Wei, Rouge, Lionel, Salphati, Laurent, Sampath, Deepak, Wallin, Jeff, Wang, Lan, Wei, BinQing, Weismann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
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Journal Article
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase
Staben, Steven T, Siu, Michael, Goldsmith, Richard, Olivero, Alan G, Do, Steven, Burdick, Daniel J, Heffron, Timothy P, Dotson, Jenna, Sutherlin, Daniel P, Zhu, Bing-Yan, Tsui, Vickie, Le, Hoa, Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy M, Nonomiya, Jim, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Rouge, Lionel, Sampath, Deepak, Sideris, Steve, Wiesmann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
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Journal Article
Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase
Staben, Steven T., Blaquiere, Nicole, Tsui, Vickie, Kolesnikov, Aleksandr, Do, Steven, Bradley, Erin K., Dotson, Jenna, Goldsmith, Richard, Heffron, Timothy P., Lesnick, John, Lewis, Cristina, Murray, Jeremy, Nonomiya, Jim, Olivero, Alan G., Pang, Jodie, Rouge, Lionel, Salphati, Laurent, Wei, BinQing, Wiesmann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
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Journal Article
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
Staben, Steven T., Heffron, Timothy P., Sutherlin, Daniel P., Bhat, Seema R., Castanedo, Georgette M., Chuckowree, Irina S., Dotson, Jenna, Folkes, Adrian J., Friedman, Lori S., Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy M., Nonomiya, Jim, Olivero, Alan G., Plise, Emile, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Rouge, Lionel, Sampath, Deepak, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Weismann, Christian, Wu, Ping, Zhu, Bing-Yan
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
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Journal Article
Synthesis of Aromatic Bisabolene Natural Products via Palladium-Catalyzed Cross-Couplings of Organozinc Reagents
Vyvyan, James R, Loitz, Celeste, Looper, Ryan E, Mattingly, Cheryl S, Peterson, Emily A, Staben, Steven T
Published in Journal of organic chemistry (02.04.2004)
Published in Journal of organic chemistry (02.04.2004)
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Overcoming Preclinical Safety Obstacles to Discover ( S )- N -((1,2,3,5,6,7-Hexahydro- s -indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5 H -pyrazolo[5,1- b ][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor
McBride, Christopher, Trzoss, Lynnie, Povero, Davide, Lazic, Milos, Ambrus-Aikelin, Geza, Santini, Angelina, Pranadinata, Rama, Bain, Gretchen, Stansfield, Ryan, Stafford, Jeffrey A., Veal, James, Takahashi, Ryan, Ly, Justin, Chen, Shu, Liu, Liling, Nespi, Marika, Blake, Robert, Katewa, Arna, Kleinheinz, Tracy, Sujatha-Bhaskar, Swathi, Ramamoorthi, Nandhini, Sims, Jessica, McKenzie, Brent, Chen, Mark, Ultsch, Mark, Johnson, Matthew, Murray, Jeremy, Ciferri, Claudio, Staben, Steven T., Townsend, Michael J., Stivala, Craig E.
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family Ligands
Steffek, Micah, Helgason, Elizabeth, Popovych, Nataliya, Rougé, Lionel, Bruning, John M., Li, Ke Sherry, Burdick, Daniel J., Cai, Jianping, Crawford, Terry, Xue, Jing, Decurtins, Willy, Fang, Chunlin, Grubers, Felix, Holliday, Michael J., Langley, Allyson, Petersen, Ann, Satz, Alexander Lee, Song, Aimin, Stoffler, Daniel, Strebel, Quentin, Tom, Jeffrey Y. K., Skelton, Nicholas, Staben, Steven T., Wichert, Moreno, Mulvihill, Melinda M., Dueber, Erin C.
Published in Biochemistry (Easton) (05.01.2022)
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Published in Biochemistry (Easton) (05.01.2022)
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Abstract PR03: Selective degradation of mutant PIK3CA promotes increased mutant specificity in a subset of PI3K ATP-competitive inhibitors
Nguyen, Lan, Edgar, Kyle, Song, Kyung, Schmidt, Stephen, Schutz, Victorai, Ishisoko, Noriko, Torres, Eric, Das, Akash, Murali, Divya, Sideris, Steve, Wendorff, Timothy, Saabye, Matt, Purkey, Hans, Sudhamsu, Jawahar, Staben, Steven, Hanan, Emily, Hatzivassiliou, Georgia, Friedman, Lori, Endres, Nicholas F.
Published in Molecular cancer research (01.10.2020)
Published in Molecular cancer research (01.10.2020)
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Journal Article
Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development
Edgar, Kyle, Hanan, Emily, Staben, Steven, Schmidt, Stephen, Hong, Rebecca, Song, Kyung, Young, Amy, Hamilton, Patricia, Arrazate, Alfonso, Cruz, Cecile de la, Belvin, Marcia, Nannini, Michelle, Friedman, Lori S., Sampath, Deepak
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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ChemInform Abstract: Heteroarylation of Azine N-Oxides
Gosselin, Francis, Savage, Scott J., Blaquiere, Nicole, Staben, Steven T.
Published in ChemInform (12.06.2012)
Published in ChemInform (12.06.2012)
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Journal Article
Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
Sutherlin, Daniel P., Baker, Stewart, Bisconte, Angelina, Blaney, Paul M., Brown, Anthony, Chan, Bryan K., Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M., Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C., Lewis, Cristina, Murray, Jeremy, Nadin, Alan J., Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S., Salphati, Laurent, Staben, Steven, Seward, Eileen M., Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K., Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
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Journal Article
Selective inhibition of NF-kB inducing kinase (NIK) is therapeutically efficacious in IFNα-accelerated lupus nephritis prone mice
Brightbill, Hans D, Suto, Eric, Blaquiere, Nicole, Ramamoorthi, Nandhini, Sujatha-Bhaskar, Swathi, Gogol, Emily, Castanedo, Georgette, Jackson, Benjamin, Haller, Susan, Lesch, Justin, Bents, Karin, Everett, Christine, Kohli, Pawan Bir, Linge, Sandra, Christian, Laura, Barrett, Kathy, Jaochico, Allan, Berezhkovskiy, Leonid M, Fan, Peter W, Veliz, Kelli, Townsend, Michael, DeVoss, Jason, Johnson, Adam, Godemann, Robert, Lee, Wyne P, Austin, Cary D, McKenzie, Brent, Hackney, Jason A, Crawford, James J, Staben, Steven, Ismaili, Moulay Hicham Alaoui, Wu, Lawren C, Ghilardi, Nico
Published in The Journal of immunology (1950) (01.05.2017)
Published in The Journal of immunology (1950) (01.05.2017)
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Journal Article
Abstract A067: Targeting p21-activated kinases in breast cancer
Hoeflich, Klaus, Ong, Christy, Lyle, Karen, Jubb, Adrian, Zhou, Wei, Harris, Adrian, Belvin, Marcia, Friedman, Lori, Koeppen, Hartmut, Rudolph, Joachim, Staben, Steven
Published in Molecular cancer research (01.10.2013)
Published in Molecular cancer research (01.10.2013)
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Journal Article
Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors
Olivero, Alan G., Heffron, Timothy P., Baumgardner, Matthew, Belvin, Marcia, Ross, Leanne Berry, Blaquiere, Nicole, Bradley, Erin, Castanedo, Georgette, Derynck, Mika, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle, Folkes, Adrian, Francis, Ross, Gianetti, Tony, Goldsmith, Richard, Goldsmith, Paul, Guan, Jane, Harrison, Trevor, Heald, Robert, Hsu, Jerry, Jackson, Phillip, Jones, Graham, Kim, Amy, Kolesnikov, Aleks, Lackner, Mark, Lee, Leslie, Lesnick, John, Lewis, Cristina, Mamounas, Michael, McLean, Neville, Murray, Jeremy, Ndubaku, Chudi, Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Prior, Wei Wei, Salphati, Laurent, Sampath, Deepack, Sideris, Stephen, Siu, Michael, Staben, Steven, Sutherlin, Daniel, Ultsch, Mark, Wallin, Jeff, Wang, Lan, Wiesmann, Christian, Zhang, Xiaolin, Friedman, Lori S.
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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Journal Article
Potent and selective inhibitors of PI3KI': Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
Sutherlin, Daniel P, Baker, Stewart, Bisconte, Angelina, Blaney, Paul M, Brown, Anthony, Chan, Bryan K, Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M, Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C, Lewis, Cristina, Murray, Jeremy, Nadin, Alan J, Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S, Salphati, Laurent, Staben, Steven, Seward, Eileen M, Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K, Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
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Journal Article
Compuestos derivados de heterociclil-pirano-heterociclilo, heterociclil-oxepina-heterociclilo, benzopirano-heterociclilo y benzoxepina-heterociclilo sustituidos; composicion farmaceutica; procedimiento de preparacion de la composicion; kit farmaceutico; y su uso en el tratamiento del cancer, mediado por la inhibicion de pi3k
GOLDSMITH, RICHARD; HEFFRON, TIM; SUTHERLIN, DANIEL P.; PEGG, NEIL; ZHU, BING-YAN; DO, STEVEN; STABEN, STEVEN; OLIVERO, ALAN G.; SIU, MICHAEL; BAYLISS, TRACY; FOLKES, ADRIAN; GOLDSMITH, PAUL; KOLESNIKOV, ALEKSANDR
Year of Publication 15.01.2010
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Year of Publication 15.01.2010
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