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1.

Degrader-antibody conjugates.

Dragovich, Peter S.

Chem Soc Rev ; 51(10): 3886-3897, 2022 May 23.

Article in English | MEDLINE | ID: mdl-35506708

2.

Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.

Wei, BinQing; Robarge, Kirk; Labadie, Sharada S; Chen, Jinhua; Corson, Laura B; DiPasquale, Antonio; Dragovich, Peter S; Eigenbrot, Charles; Evangelista, Marie; Fauber, Benjamin P; Hitz, Anna; Hong, Rebecca; Lai, Kwong Wah; Liu, Wenfeng; Ma, Shuguang; Malek, Shiva; O'Brien, Thomas; Pang, Jodie; Peterson, David; Salphati, Laurent; Sampath, Deepak; Sideris, Steven; Ultsch, Mark; Xu, Zijin; Yen, Ivana; Yu, Dong; Yue, Qin; Zhou, Aihe; Purkey, Hans E.

Bioorg Med Chem Lett ; 59: 128576, 2022 03 01.

Article in English | MEDLINE | ID: mdl-35065235

3.

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

Dragovich, Peter S; Adhikari, Pragya; Blake, Robert A; Blaquiere, Nicole; Chen, Jinhua; Cheng, Yun-Xing; den Besten, Willem; Han, Jinping; Hartman, Steven J; He, Jintang; He, Mingtao; Rei Ingalla, Ellen; Kamath, Amrita V; Kleinheinz, Tracy; Lai, Tommy; Leipold, Douglas D; Li, Chun Sing; Liu, Qi; Lu, Jiawei; Lu, Ying; Meng, Fanwei; Meng, Lingyao; Ng, Carl; Peng, Kaishan; Lewis Phillips, Gail; Pillow, Thomas H; Rowntree, Rebecca K; Sadowsky, Jack D; Sampath, Deepak; Staben, Leanna; Staben, Steven T; Wai, John; Wan, Kunpeng; Wang, Xinxin; Wei, BinQing; Wertz, Ingrid E; Xin, Jianfeng; Xu, Keyang; Yao, Hui; Zang, Richard; Zhang, Donglu; Zhou, Hao; Zhao, Yongxin.

Bioorg Med Chem Lett ; 30(4): 126907, 2020 02 15.

Article in English | MEDLINE | ID: mdl-31902710

4.

Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.

Su, Dian; Chen, Jinhua; Cosino, Ely; Dela Cruz-Chuh, Josefa; Davis, Helen; Del Rosario, Geoffrey; Figueroa, Isabel; Goon, Leanne; He, Jintang; Kamath, Amrita V; Kaur, Surinder; Kozak, Katherine R; Lau, Jeffrey; Lee, Donna; Lee, M Violet; Leipold, Douglas; Liu, Luna; Liu, Peter; Lu, Guo-Liang; Nelson, Chris; Ng, Carl; Pillow, Thomas H; Polakis, Paul; Polson, Andrew G; Rowntree, Rebecca K; Saad, Ola; Safina, Brian; Stagg, Nicola J; Tercel, Moana; Vandlen, Richard; Vollmar, Breanna S; Wai, John; Wang, Tao; Wei, BinQing; Xu, Keyang; Xue, Juanjuan; Xu, Zijin; Yan, Gang; Yao, Hui; Yu, Shang-Fan; Zhang, Donglu; Zhong, Fiona; Dragovich, Peter S.

Bioconjug Chem ; 30(5): 1356-1370, 2019 05 15.

Article in English | MEDLINE | ID: mdl-30966735

5.

Carfilzomib Is Not an Appropriate Payload of Antibody-Drug Conjugates Due to Rapid Inactivation by Lysosomal Enzymes.

Ma, Yong; Dela Cruz-Chuh, Josefa; Khojasteh, S Cyrus; Dragovich, Peter S; Pillow, Thomas H; Zhang, Donglu.

Drug Metab Dispos ; 47(8): 884-889, 2019 08.

Article in English | MEDLINE | ID: mdl-31072822

6.

Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues.

Zhang, Donglu; Dragovich, Peter S; Yu, Shang-Fan; Ma, Yong; Pillow, Thomas H; Sadowsky, Jack D; Su, Dian; Wang, Wei; Polson, Andrew; Khojasteh, S Cyrus; Hop, Cornelis E C A.

Drug Metab Dispos ; 47(10): 1146-1155, 2019 10.

Article in English | MEDLINE | ID: mdl-31358513

7.

Catalytic Cleavage of Disulfide Bonds in Small Molecules and Linkers of Antibody-Drug Conjugates.

Zhang, Donglu; Fourie-O'Donohue, Aimee; Dragovich, Peter S; Pillow, Thomas H; Sadowsky, Jack D; Kozak, Katherine R; Cass, Robert T; Liu, Liling; Deng, Yuzhong; Liu, Yichin; Hop, Cornelis E C A; Khojasteh, S Cyrus.

Drug Metab Dispos ; 47(10): 1156-1163, 2019 10.

Article in English | MEDLINE | ID: mdl-31085544

8.

Preclinical assessment of the ADME, efficacy and drug-drug interaction potential of a novel NAMPT inhibitor.

Liederer, Bianca M; Cheong, Jonathan; Chou, Kang-Jye; Dragovich, Peter S; Le, Hoa; Liang, Xiaorong; Ly, Justin; Mukadam, Sophie; Oeh, Jason; Sampath, Deepak; Wang, Leslie; Wong, Susan.

Xenobiotica ; 49(9): 1063-1077, 2019 Sep.

Article in English | MEDLINE | ID: mdl-30257601

9.

Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody-Drug Conjugates with Phenol-Containing Payloads.

Zhang, Donglu; Le, Hoa; Cruz-Chuh, Josefa Dela; Bobba, Sudheer; Guo, Jun; Staben, Leanna; Zhang, Chenghong; Ma, Yong; Kozak, Katherine R; Lewis Phillips, Gail D; Vollmar, Breanna S; Sadowsky, Jack D; Vandlen, Richard; Wei, BinQing; Su, Dian; Fan, Peter; Dragovich, Peter S; Khojasteh, S Cyrus; Hop, Cornelis E C A; Pillow, Thomas H.

Bioconjug Chem ; 29(2): 267-274, 2018 02 21.

Article in English | MEDLINE | ID: mdl-29369629

10.

Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.

Dragovich, Peter S; Blake, Robert A; Chen, Chunjiao; Chen, Jinhua; Chuh, Josefa; den Besten, Willem; Fan, Fang; Fourie, Aimee; Hartman, Steven J; He, Changrong; He, Jintang; Ingalla, Ellen Rei; Kozak, Katherine R; Leong, Steven R; Lu, Jiawei; Ma, Yong; Meng, Lingyao; Nannini, Michelle; Oeh, Jason; Ohri, Rachana; Lewis Phillips, Gail; Pillow, Thomas H; Rowntree, Rebecca K; Sampath, Deepak; Vandlen, Richard; Vollmar, Breanna; Wai, John; Wertz, Ingrid E; Xu, Keyang; Xu, Zijin; Zhang, Donglu.

Chemistry ; 24(19): 4830-4834, 2018 Apr 03.

Article in English | MEDLINE | ID: mdl-29493023

11.

Exploration of Pyrrolobenzodiazepine (PBD)-Dimers Containing Disulfide-Based Prodrugs as Payloads for Antibody-Drug Conjugates.

Pei, Zhonghua; Chen, Chunjiao; Chen, Jinhua; Cruz-Chuh, Josefa Dela; Delarosa, Reginald; Deng, Yuzhong; Fourie-O'Donohue, Aimee; Figueroa, Isabel; Guo, Jun; Jin, Weiwei; Khojasteh, S Cyrus; Kozak, Katherine R; Latifi, Brandon; Lee, James; Li, Guangmin; Lin, Eva; Liu, Liling; Lu, Jiawei; Martin, Scott; Ng, Carl; Nguyen, Trung; Ohri, Rachana; Lewis Phillips, Gail; Pillow, Thomas H; Rowntree, Rebecca K; Stagg, Nicola J; Stokoe, David; Ulufatu, Sheila; Verma, Vishal A; Wai, John; Wang, Jing; Xu, Keyang; Xu, Zijin; Yao, Hui; Yu, Shang-Fan; Zhang, Donglu; Dragovich, Peter S.

Mol Pharm ; 15(9): 3979-3996, 2018 09 04.

Article in English | MEDLINE | ID: mdl-30040421

12.

Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.

Dragovich, Peter S; Broccatelli, Fabio; Chen, Jinhua; Fan, Peter; Le, Hoa; Mao, Weiguang; Pillow, Thomas H; Polson, Andrew G; Wai, John; Xu, Zijin; Yao, Hui; Zhang, Donglu.

Bioorg Med Chem Lett ; 27(23): 5300-5304, 2017 12 01.

Article in English | MEDLINE | ID: mdl-29079474

13.

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

Liang, Jun; Labadie, Sharada; Zhang, Birong; Ortwine, Daniel F; Patel, Snahel; Vinogradova, Maia; Kiefer, James R; Mauer, Till; 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; An, Le; Ran, Yingqing; Classon, Marie; Trojer, Patrick; Dragovich, Peter S; Murray, Lesley.

Bioorg Med Chem Lett ; 27(13): 2974-2981, 2017 07 01.

Article in English | MEDLINE | ID: mdl-28512031

14.

Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates.

Zhang, Donglu; Yu, Shang-Fan; Ma, Yong; Xu, Keyang; Dragovich, Peter S; Pillow, Thomas H; Liu, Luna; Del Rosario, Geoffrey; He, Jintang; Pei, Zhonghua; Sadowsky, Jack D; Erickson, Hans K; Hop, Cornelis E C A; Khojasteh, S Cyrus.

Drug Metab Dispos ; 44(9): 1517-23, 2016 09.

Article in English | MEDLINE | ID: mdl-27417182

15.

Antibody Drug Conjugates Differentiate Uptake and DNA Alkylation of Pyrrolobenzodiazepines in Tumors from Organs of Xenograft Mice.

Ma, Yong; Khojasteh, S Cyrus; Hop, Cornelis E C A; Erickson, Hans K; Polson, Andrew; Pillow, Thomas H; Yu, Shang-Fan; Wang, Hong; Dragovich, Peter S; Zhang, Donglu.

Drug Metab Dispos ; 44(12): 1958-1962, 2016 12.

Article in English | MEDLINE | ID: mdl-27683653

16.

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.

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.

Bioorg Med Chem Lett ; 26(16): 4036-41, 2016 08 15.

Article in English | MEDLINE | ID: mdl-27406798

17.

Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.

Labadie, Sharada S; Dragovich, Peter S; Cummings, Richard T; Deshmukh, Gauri; Gustafson, Amy; Han, Ning; Harmange, Jean-Christophe; Kiefer, James R; Li, Yue; Liang, Jun; Liederer, Bianca M; Liu, Yichin; Manieri, Wanda; Mao, Wiefeng; Murray, Lesley; Ortwine, Daniel F; Trojer, Patrick; VanderPorten, Erica; Vinogradova, Maia; Wen, Li.

Bioorg Med Chem Lett ; 26(18): 4492-4496, 2016 09 15.

Article in English | MEDLINE | ID: mdl-27499454

18.

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Labadie, Sharada; Dragovich, Peter S; Chen, Jinhua; Fauber, Benjamin P; Boggs, Jason; Corson, Laura B; Ding, Charles Z; Eigenbrot, Charles; Ge, HongXiu; Ho, Qunh; Lai, Kwong Wah; Ma, Shuguang; Malek, Shiva; Peterson, David; Purkey, Hans E; Robarge, Kirk; Salphati, Laurent; Sideris, Steven; Ultsch, Mark; VanderPorten, Erica; Wei, BinQing; Xu, Qing; Yen, Ivana; Yue, Qin; Zhang, Huihui; Zhang, Xuying; Zhou, Aihe.

Bioorg Med Chem Lett ; 25(1): 75-82, 2015 Jan 01.

Article in English | MEDLINE | ID: mdl-25466195

19.

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Zak, Mark; Liederer, Bianca M; Sampath, Deepak; Yuen, Po-Wai; Bair, Kenneth W; Baumeister, Timm; Buckmelter, Alexandre J; Clodfelter, Karl H; Cheng, Eric; Crocker, Lisa; Fu, Bang; Han, Bingsong; Li, Guangkun; Ho, Yen-Ching; Lin, Jian; Liu, Xiongcai; Ly, Justin; O'Brien, Thomas; Reynolds, Dominic J; Skelton, Nicholas; Smith, Chase C; Tay, Suzanne; Wang, Weiru; Wang, Zhongguo; Xiao, Yang; Zhang, Lei; Zhao, Guiling; Zheng, Xiaozhang; Dragovich, Peter S.

Bioorg Med Chem Lett ; 25(3): 529-41, 2015 Feb 01.

Article in English | MEDLINE | ID: mdl-25556090

20.

Preclinical models of nicotinamide phosphoribosyltransferase inhibitor-mediated hematotoxicity and mitigation by co-treatment with nicotinic acid.

Tarrant, Jacqueline M; Dhawan, Preeti; Singh, Jatinder; Zabka, Tanja S; Clarke, Emer; DosSantos, Garry; Dragovich, Peter S; Sampath, Deepak; Lin, Tori; McCray, Bobbi; La, Nghi; Nguyen, Trung; Kauss, Ariel; Dambach, Donna; Misner, Dinah L; Diaz, Dolores; Uppal, Hirdesh.

Toxicol Mech Methods ; 25(3): 201-11, 2015 Mar.

Article in English | MEDLINE | ID: mdl-25894564

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