Degrader-antibody conjugates von Dragovich, Peter S

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Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer von Sampath, Deepak, Zabka, Tanja S, Misner, Dinah L, O'Brien, Thomas, Dragovich, Peter S

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Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers von Cantley, Jennifer, Ye, Xiaofen, Rousseau, Emma, Januario, Tom, Hamman, Brian D., Rose, Christopher M., Cheung, Tommy K., Hinkle, Trent, Soto, Leofal, Quinn, Connor, Harbin, Alicia, Bortolon, Elizabeth, Chen, Xin, Haskell, Roy, Lin, Eva, Yu, Shang-Fan, Del Rosario, Geoff, Chan, Emily, Dunlap, Debra, Koeppen, Hartmut, Martin, Scott, Merchant, Mark, Grimmer, Matt, Broccatelli, Fabio, Wang, Jing, Pizzano, Jennifer, Dragovich, Peter S., Berlin, Michael, Yauch, Robert L.

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The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results von Lewis, Gail D., Li, Guangmin, Guo, Jun, Yu, Shang-Fan, Fields, Carter T., Lee, Genee, Zhang, Donglu, Dragovich, Peter S., Pillow, Thomas, Wei, BinQing, Sadowsky, Jack, Leipold, Douglas, Wilson, Tim, Kamath, Amrita, Mamounas, Michael, Lee, M. Violet, Saad, Ola, Choeurng, Voleak, Ungewickell, Alexander, Monemi, Sharareh, Crocker, Lisa, Kalinsky, Kevin, Modi, Shanu, Jung, Kyung Hae, Hamilton, Erika, LoRusso, Patricia, Krop, Ian, Schutten, Melissa M., Commerford, Renee, Sliwkowski, Mark X., Cho, Eunpi

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Antibody–Drug Conjugates for Immunology von Dragovich, Peter S

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Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors von Kschonsak, Marc, Jao, Christine C, Arthur, Christopher P, Rohou, Alexis L, Bergeron, Philippe, Ortwine, Daniel F, McKerrall, Steven J, Hackos, David H, Deng, Lunbin, Chen, Jun, Li, Tianbo, Dragovich, Peter S, Volgraf, Matthew, Wright, Matthew R, Payandeh, Jian, Ciferri, Claudio, Tellis, John C

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Structural basis for resistance to diverse classes of NAMPT inhibitors von Wang, Weiru, Elkins, Kristi, Oh, Angela, Ho, Yen-Ching, Wu, Jiansheng, Li, Hong, Xiao, Yang, Kwong, Mandy, Coons, Mary, Brillantes, Bobby, Cheng, Eric, Crocker, Lisa, Dragovich, Peter S, Sampath, Deepak, Zheng, Xiaozhang, Bair, Kenneth W, O'Brien, Thomas, Belmont, Lisa D

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Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody–Drug Conjugates von Staben, Leanna R, Chen, Jinhua, Cruz-Chuh, Josefa dela, del Rosario, Geoff, Go, Mary Ann, Guo, Jun, Khojasteh, S. Cyrus, Kozak, Katherine R, Li, Guangmin, Ng, Carl, Lewis Phillips, Gail D, Pillow, Thomas H, Rowntree, Rebecca K, Wai, John, Wei, BinQing, Xu, Keyang, Xu, Zijin, Yu, Shang-Fan, Zhang, Donglu, Dragovich, Peter S

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Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase von Fauber, Benjamin P., Dragovich, Peter S., Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Liu, Yingchun, Malek, Shiva, Peterson, David, Pitts, Keith, Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wang, Jing, Wei, BinQing, Yen, Ivana, Yue, Qin

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Structure-Based Discovery of Novel Amide-Containing Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors von Zheng, Xiaozhang, Bauer, Paul, Baumeister, Timm, Buckmelter, Alexandre J, Caligiuri, Maureen, Clodfelter, Karl H, Han, Bingsong, Ho, Yen-Ching, Kley, Nikolai, Lin, Jian, Reynolds, Dominic J, Sharma, Geeta, Smith, Chase C, Wang, Zhongguo, Dragovich, Peter S, Gunzner-Toste, Janet, Liederer, Bianca M, Ly, Justin, O’Brien, Thomas, Oh, Angela, Wang, Leslie, Wang, Weiru, Xiao, Yang, Zak, Mark, Zhao, Guiling, Yuen, Po-wai, Bair, Kenneth W

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Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase von Dragovich, Peter S., Fauber, Benjamin P., Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Malek, Shiva, Pan, Borlan, Peterson, David, Pitts, Keith, Purkey, Hans E., Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying

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Structure-Based Identification of Ureas as Novel Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors von Zheng, Xiaozhang, Bauer, Paul, Baumeister, Timm, Buckmelter, Alexandre J, Caligiuri, Maureen, Clodfelter, Karl H, Han, Bingsong, Ho, Yen-Ching, Kley, Nikolai, Lin, Jian, Reynolds, Dominic J, Sharma, Geeta, Smith, Chase C, Wang, Zhongguo, Dragovich, Peter S, Oh, Angela, Wang, Weiru, Zak, Mark, Gunzner-Toste, Janet, Zhao, Guiling, Yuen, Po-wai, Bair, Kenneth W

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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies von Liang, Jun, Zhang, Birong, Labadie, Sharada, Ortwine, Daniel F., Vinogradova, Maia, Kiefer, James R., Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley

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Supplementation of Nicotinic Acid with NAMPT Inhibitors Results in Loss of In Vivo Efficacy in NAPRT1 -Deficient Tumor Models von O'Brien, Thomas, Oeh, Jason, Xiao, Yang, Liang, Xiaorong, Vanderbilt, Alexander, Qin, Ann, Yang, Lulu, Lee, Leslie B, Ly, Justin, Cosino, Ely, LaCap, Jennifer A, Ogasawara, Annie, Williams, Simon, Nannini, Michelle, Liederer, Bianca M, Jackson, Peter, Dragovich, Peter S, Sampath, Deepak

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Improved translation of stability for conjugated antibodies using an in vitro whole blood assay von Fourie-O'Donohue, Aimee, Chu, Phillip Y., Chuh, Josefa dela Cruz, Tchelepi, Robert, Tsai, Siao Ping, Tran, John C., Sawyer, William S., Su, Dian, Ng, Carl, Xu, Keyang, Yu, Shang-Fan, Pillow, Thomas H., Sadowsky, Jack, Dragovich, Peter S., Liu, Yichin, Kozak, Katherine R.

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Preclinical optimization of Ly6E-targeted ADCs for increased durability and efficacy of anti-tumor response von Dela Cruz Chuh, Josefa, Go, MaryAnn, Chen, Yvonne, Guo, Jun, Rafidi, Hanine, Mandikian, Danielle, Sun, Yonglian, Lin, Zhonghua, Schneider, Kellen, Zhang, Pamela, Vij, Rajesh, Sharpnack, Danielle, Chan, Pamela, de la Cruz, Cecile, Sadowsky, Jack, Seshasayee, Dhaya, Koerber, James T., Pillow, Thomas H., Phillips, Gail D., Rowntree, Rebecca K., Boswell, C. Andrew, Kozak, Katherine R., Polson, Andrew G., Polakis, Paul, Yu, Shang-Fan, Dragovich, Peter S., Agard, Nicholas J.

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Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs von Zhang, Donglu, Ma, Bin, Dragovich, Peter S., Ma, Li, Chen, Shu, Chen, Eugene C., Ye, Xiaofen, Liu, Joyce, Pizzano, Jennifer, Bortolon, Elizabeth, Chan, Emily, Zhang, Xing, Chen, Yi-Chen, Levy, Elizabeth S., Yauch, Robert L., Khojasteh, S. Cyrus, Hop, Cornelis E. C. A.

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Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT) von Dragovich, Peter S., Bair, Kenneth W., Baumeister, Timm, Ho, Yen-Ching, Liederer, Bianca M., Liu, Xiongcai, Liu, Yongbo, O’Brien, Thomas, Oeh, Jason, Sampath, Deepak, Skelton, Nicholas, Wang, Leslie, Wang, Weiru, Wu, Hongxing, Xiao, Yang, Yuen, Po-wai, Zak, Mark, Zhang, Lei, Zheng, Xiaozhang

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Crystallographic Identification of a Noncompetitive Inhibitor Binding Site on the Hepatitis C Virus NS5B RNA Polymerase Enzyme von Love, Robert A, Parge, Hans E, Yu, Xiu, Hickey, Michael J, Diehl, Wade, Gao, Jingjin, Wriggers, Hilary, Ekker, Anne, Wang, Liann, Thomson, James A, Dragovich, Peter S, Fuhrman, Shella A

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Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors von Zheng, Xiaozhang, Baumeister, Timm, Buckmelter, Alexandre J, Caligiuri, Maureen, Clodfelter, Karl H, Han, Bingsong, Ho, Yen-Ching, Kley, Nikolai, Lin, Jian, Reynolds, Dominic J, Sharma, Geeta, Smith, Chase C, Wang, Zhongguo, Dragovich, Peter S, Oh, Angela, Wang, Weiru, Zak, Mark, Wang, Yunli, Yuen, Po-Wai, Bair, Kenneth W

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