Monomeric Targeted Protein Degraders
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Published in Journal of medicinal chemistry (22.10.2020)
Published in Journal of medicinal chemistry (22.10.2020)
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Structure of the essential inner membrane lipopolysaccharide–PbgA complex
Clairfeuille, Thomas, Buchholz, Kerry R., Li, Qingling, Verschueren, Erik, Liu, Peter, Sangaraju, Dewakar, Park, Summer, Noland, Cameron L., Storek, Kelly M., Nickerson, Nicholas N., Martin, Lynn, Dela Vega, Trisha, Miu, Anh, Reeder, Janina, Ruiz-Gonzalez, Maria, Swem, Danielle, Han, Guanghui, DePonte, Daniel P., Hunter, Mark S., Gati, Cornelius, Shahidi-Latham, Sheerin, Xu, Min, Skelton, Nicholas, Sellers, Benjamin D., Skippington, Elizabeth, Sandoval, Wendy, Hanan, Emily J., Payandeh, Jian, Rutherford, Steven T.
Published in Nature (London) (20.08.2020)
Published in Nature (London) (20.08.2020)
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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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Journal Article
RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy
Song, Kyung W, Edgar, Kyle A, Hanan, Emily J, Hafner, Marc, Oeh, Jason, Merchant, Mark, Sampath, Deepak, Nannini, Michelle A, Hong, Rebecca, Phu, Lilian, Forrest, William F, Stawiski, Eric, Schmidt, Stephen, Endres, Nicholas, Guan, Jane, Wallin, Jeffrey J, Cheong, Jonathan, Plise, Emile G, Lewis Phillips, Gail D, Salphati, Laurent, Heffron, Timothy P, Olivero, Alan G, Malek, Shiva, Staben, Steven T, Kirkpatrick, Donald S, Dey, Anwesha, Friedman, Lori S
Published in Cancer discovery (01.01.2022)
Published in Cancer discovery (01.01.2022)
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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Hanan, Emily J, van Abbema, Anne, Barrett, Kathy, Blair, Wade S, Blaney, Jeff, Chang, Christine, Eigenbrot, Charles, Flynn, Sean, Gibbons, Paul, Hurley, Christopher A, Kenny, Jane R, Kulagowski, Janusz, Lee, Leslie, Magnuson, Steven R, Morris, Claire, Murray, Jeremy, Pastor, Richard M, Rawson, Tom, Siu, Michael, Ultsch, Mark, Zhou, Aihe, Sampath, Deepak, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling
Zak, Mark, Hanan, Emily J., Lupardus, Patrick, Brown, David G., Robinson, Colin, Siu, Michael, Lyssikatos, Joseph P., Romero, F. Anthony, Zhao, Guiling, Kellar, Terry, Mendonca, Rohan, Ray, Nicholas C., Goodacre, Simon C., Crackett, Peter H., McLean, Neville, Hurley, Christopher A., Yuen, Po-wai, Cheng, Yun-Xing, Liu, Xiongcai, Liimatta, Marya, Kohli, Pawan Bir, Nonomiya, Jim, Salmon, Gary, Buckley, Gerry, Lloyd, Julia, Gibbons, Paul, Ghilardi, Nico, Kenny, Jane R., Johnson, Adam
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
Published in Bioorganic & medicinal chemistry letters (15.06.2019)
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Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study
Heald, Robert, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Bryan, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dominguez-Fernandez, Belen, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Jackson, Philip, Knight, Jamie, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam, Merchant, Mark, Mortara, Kyle, Purkey, Hans, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (25.11.2015)
Published in Journal of medicinal chemistry (25.11.2015)
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Optimization of globomycin analogs as novel gram-negative antibiotics
Garland, Keira, Pantua, Homer, Braun, Marie-Gabrielle, Burdick, Daniel J., Castanedo, Georgette M., Chen, Yi-Chen, Cheng, Yun-Xing, Cheong, Jonathan, Daniels, Blake, Deshmukh, Gauri, Fu, Yuhong, Gibbons, Paul, Gloor, Susan L., Hua, Rongbao, Labadie, Sharada, Liu, Xiongcai, Pastor, Richard, Stivala, Craig, Xu, Min, Xu, Yiming, Zheng, Hao, Kapadia, Sharookh B., Hanan, Emily J.
Published in Bioorganic & medicinal chemistry letters (15.10.2020)
Published in Bioorganic & medicinal chemistry letters (15.10.2020)
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Unstable Mechanisms of Resistance to Inhibitors of Escherichia coli Lipoprotein Signal Peptidase
Pantua, Homer, Skippington, Elizabeth, Braun, Marie-Gabrielle, Noland, Cameron L., Diao, Jingyu, Peng, Yutian, Gloor, Susan L., Yan, Donghong, Kang, Jing, Katakam, Anand Kumar, Reeder, Janina, Castanedo, Georgette M., Garland, Keira, Komuves, Laszlo, Sagolla, Meredith, Austin, Cary D., Murray, Jeremy, Xu, Yiming, Modrusan, Zora, Xu, Min, Hanan, Emily J., Kapadia, Sharookh B.
Published in mBio (08.09.2020)
Published in mBio (08.09.2020)
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4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase
Hanan, Emily J., Baumgardner, Matt, Bryan, Marian C., Chen, Yuan, Eigenbrot, Charles, Fan, Peter, Gu, Xiao-Hui, La, Hank, Malek, Shiva, Purkey, Hans E., Schaefer, Gabriele, Schmidt, Stephen, Sideris, Steve, Yen, Ivana, Yu, Christine, Heffron, Timothy P.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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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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Lipid Tales: Optimizing Arylomycin Membrane Anchors
Koehler, Michael F. T., Chen, Yi-Chen, Chen, Yongsheng, Chen, Yuan, Crawford, James J., Durk, Matthew R., Garland, Keira, Hanan, Emily J., Higuchi, Robert I., Hu, Huiyong, Ly, Cuong Q., Paraselli, Prasuna G., Roberts, Tucker C., Schwarz, Jacob B., Smith, Peter A., Yu, Zhiyong, Heise, Christopher E.
Published in ACS medicinal chemistry letters (09.11.2023)
Published in ACS medicinal chemistry letters (09.11.2023)
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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 and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
Zak, Mark, Mendonca, Rohan, Balazs, Mercedesz, Barrett, Kathy, Bergeron, Philippe, Blair, Wade S, Chang, Christine, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Hamman, Chris, Hanan, Emily J, Harstad, Eric, Hewitt, Peter R, Hurley, Christopher A, Jin, Tian, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Kulagowski, Janusz J, Labadie, Sharada, Liao, Jiangpeng, Liimatta, Marya, Lin, Zhonghua, Lupardus, Patrick J, Maxey, Robert J, Murray, Jeremy M, Pulk, Rebecca, Rodriguez, Madeleine, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, Ultsch, Mark, van Abbema, Anne, Ward, Stuart I, Xiao, Ling, Xiao, Yisong
Published in Journal of medicinal chemistry (12.07.2012)
Published in Journal of medicinal chemistry (12.07.2012)
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Discovery of a potent and selective Aurora kinase inhibitor
Oslob, Johan D., Romanowski, Michael J., Allen, Darin A., Baskaran, Subramanian, Bui, Minna, Elling, Robert A., Flanagan, William M., Fung, Amy D., Hanan, Emily J., Harris, Shannon, Heumann, Stacey A., Hoch, Ute, Jacobs, Jeffrey W., Lam, Joni, Lawrence, Chris E., McDowell, Robert S., Nannini, Michelle A., Shen, Wang, Silverman, Jeffrey A., Sopko, Michelle M., Tangonan, Bradley T., Teague, Juli, Yoburn, Josh C., Yu, Chul H., Zhong, Min, Zimmerman, Kristin M., O’Brien, Tom, Lew, Willard
Published in Bioorganic & medicinal chemistry (01.09.2008)
Published in Bioorganic & medicinal chemistry (01.09.2008)
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Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR
Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Clausen, Saundra, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Heald, Robert, Jackson, Philip, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam E, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Wang, Shumei, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in ACS medicinal chemistry letters (14.01.2016)
Published in ACS medicinal chemistry letters (14.01.2016)
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Preclinical development of the PI3K Alpha selective and PIK3CA Mutant selective inhibitor GDC-0077 and prediction of its human pharmacokinetics
Pang, Jodie, Baumgardner, Matthew, Braun, Marie-Gabrielle, Cheong, Jonathan, Edgar, Kyle, Friedman, Lori, Hanan, Emily, Jaochico, Allan, Ma, Shuguang, Plise, Emile, Schmidt, Stephen, Liu, Ning, Song, Kyung, Staben, Steve, Salphati, Laurent
Published in Drug metabolism and pharmacokinetics (01.01.2019)
Published in Drug metabolism and pharmacokinetics (01.01.2019)
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Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye
Zhong, Min, Gadek, Thomas R, Bui, Minna, Shen, Wang, Burnier, John, Barr, Kenneth J, Hanan, Emily J, Oslob, Johan D, Yu, Chul H, Zhu, Jiang, Arkin, Michelle R, Evanchik, Marc J, Flanagan, W. Mike, Hoch, Ute, Hyde, Jennifer, Prabhu, Saileta, Silverman, Jeffrey A, Wright, Jasmin
Published in ACS medicinal chemistry letters (08.03.2012)
Published in ACS medicinal chemistry letters (08.03.2012)
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Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study
Heald, Robert, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Bryan, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dominguez-Fernandez, Belen, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Jackson, Philip, Knight, Jamie, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam, Merchant, Mark, Mortara, Kyle, Purkey, Hans, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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