Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Leanna Staben"'
Autor:
Peter S. Dragovich, Mingtao He, Leanna Staben, Hongyan Zhang, Melinda M. Mulvihill, Catherine Wilson, Hao Zhou, Tracy Kleinheinz, Binqing Wei, Jianfeng Xin, Nicole Blaquiere, Fanwei Meng, John S. Wai, Susan Kaufman, Liang Liu, Rebecca K. Rowntree, Steven T. Staben, Jing Wang, Katherine R. Kozak, Josefa dela Cruz-Chuh, Zijin Xu, Steven J. Hartman, Robert A. Blake, Xiaoyu Zhu, Sunil Bhakta, Donglu Zhang, Hui Yao, Aimee O'Donohue, Jack Sadowsky, Qi Liu, Pragya Adhikari, Liling Liu, Ying Lu, Thomas H. Pillow, Jinhua Chen, Emel Adaligil, Karen E. Gascoigne
Publikováno v:
Journal of Medicinal Chemistry. 64:2534-2575
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin ligase-mediated ubiquitination continue to grow. However, these chi
Autor:
Donglu Zhang, Binqing Wei, Jun Guo, Thomas H. Pillow, Buyun Chen, Chenghong Zhang, Leanna Staben, Dewakar Sangaraju, Gail Lewis Phillips, Dian Su, Yong Ma, Cyrus Khojasteh, Sudheer Bobba, Jianshuang Wang, Peter S. Dragovich, Shuai Wang
Publikováno v:
Drug Metabolism and Disposition. 47:547-555
Duocarmycins [including cyclopropyl pyrroloindole (CPI) or cyclopropyl benzoindole (CBI)] are a class of DNA minor-groove alkylators and seco-CPI/CBIs are synthetic pro-forms that can spirocyclize to CPI/CBI. Bis-CPI/CBIs are potential drug candidate
Autor:
Steven J. Hartman, Ying Lu, Wentao Wei, Hao Zhou, Geoffrey Del Rosario, Robert A. Blake, Xiaoyu Zhu, Nicholas Corr, Aaron Fullerton, Shang-Fan Yu, Peter S. Dragovich, Jing Wang, Rebecca K. Rowntree, Donglu Zhang, Hui Yao, Emel Adaligil, Fan Jiang, Hongyan Zhang, Jack Sadowsky, John S. Wai, Jinhua Chen, Thomas H. Pillow, Susan Kaufman, Zijin Xu, Katherine R. Kozak, Jeremy Murray, Shenhua Zhang, Leanna Staben, Josefa dela Cruz-Chuh, Pragya Adhikari, Aimee O'Donohue, Tracy Kleinheinz, Liling Liu, Melinda M. Mulvihill, William S. Sawyer, Yongxin Zhao, Binqing Wei
Publikováno v:
Journal of medicinal chemistry. 64(5)
Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a targeted manner via co-opted ubiquitin ligases have enormous potential to transform the field of medicinal chemistry. These chimeric molecules, often termed pr
Autor:
Peter S. Dragovich, Jun Guo, Josefa dela Cruz-Chuh, Guangmin Li, Binqing Wei, Zijin Xu, Leanna Staben, Geoff Del Rosario, Shang-Fan Yu, Thomas H. Pillow, Katherine R. Kozak, Mary Ann Go, Jinhua Chen, Rebecca K. Rowntree, John S. Wai, Carl Ng, Keyang Xu, Donglu Zhang, S. Cyrus Khojasteh, Gail Lewis Phillips
Publikováno v:
Journal of medicinal chemistry. 63(17)
Cytotoxic pyrrolobenzodiazepine (PBD)-dimer molecules are frequently utilized as payloads for antibody-drug conjugates (ADCs), and many examples are currently in clinical development. In order to further explore this ADC payload class, the physicoche
Autor:
Leanna Staben, Josefa dela Cruz-Chuh, Hoa Le, Thomas H. Pillow, Binqing Wei, Dian Su, Peter S. Dragovich, Breanna S. Vollmar, Peter W. Fan, S. Cyrus Khojasteh, Gail Lewis Phillips, Yong Ma, Richard Vandlen, Cornelis E. C. A. Hop, Sudheer Bobba, Chenghong Zhang, Jun Guo, Donglu Zhang, Jack Sadowsky, Katherine R. Kozak
Publikováno v:
Bioconjugate Chemistry. 29:267-274
The valine-citrulline (Val-Cit) dipeptide and p-aminobenzyl (PAB) spacer have been commonly used as a cleavable self-immolating linker in ADC design including in the clinically approved ADC, brentuximab vedotin (Adcetris). When the same linker was us
Autor:
Katherine R. Kozak, Siao Ping Tsai, Doug Leipold, Luke Masterson, Hui Yao, Stefan Steinbacher, Jim Nonomiya, Keyang Xu, Helga Raab, Vishal Verma, Binqing Wei, Jeff Lau, Tao Wang, Janet Gunzner-Toste, Shang-Fan Yu, John A. Flygare, Thomas H. Pillow, Leanna Staben, John S. Wai, Zijin Xu, Brian Safina, Gail Dianne Phillips, Philip Howard, Jing Wang, Dian Su, Josefa Chuh, Jinhua Chen, Guiling Zhao, Guangmin Li, Rachana Ohri, Yichin Liu, Amrita V. Kamath, Charles Eigenbrot
Publikováno v:
Journal of Medicinal Chemistry. 61:989-1000
Antibody-drug conjugates (ADCs) have become an important therapeutic modality for oncology, with three approved by the FDA and over 60 others in clinical trials. Despite the progress, improvements in ADC therapeutic index are desired. Peptide-based A
Autor:
Mingtao He, Chun Sing Li, Yongxin Zhao, Deepak Sampath, Leanna Staben, Ingrid E. Wertz, Hao Zhou, Rebecca K. Rowntree, Ellen Ingalla, Xinxin Wang, Richard Zang, Ying Lu, Qi Liu, Jiawei Lu, Gail Lewis Phillips, Binqing Wei, Fanwei Meng, Nicole Blaquiere, Yun-Xing Cheng, Steven T. Staben, Keyang Xu, Jinping Han, Tommy Lai, Kaishan Peng, Kunpeng Wan, Peter S. Dragovich, Lingyao Meng, Tracy Kleinheinz, Jinhua Chen, Amrita V. Kamath, John S. Wai, Carl Ng, Pragya Adhikari, Steven J. Hartman, Jianfeng Xin, Jintang He, Douglas D. Leipold, Thomas H. Pillow, Donglu Zhang, Hui Yao, Jack Sadowsky, Robert A. Blake, Willem den Besten
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are currently of high interest in medicinal chemistry. However, these entities are relatively large compounds that ofte
Autor:
Michael Berlin, Roy Haskell, Emma Rousseau, Connor Quinn, An Nguyen, Alicia Morgan, Tharu M. Fernando, Christopher M. Rose, Alexey Ishchenko, Fabio Broccatelli, Peter S. Dragovich, Emily Chan, Vijay Sethuraman, Xiaofen Ye, Gregory Cadelina, Mark Bookbinder, Brian D. Hamman, Kim Davenport, Jennifer Cantley, Jing Wang, Jonathan Maher, Debbie Gordon, Mark Merchant, Robert L. Yauch, Huifen Chen, Donald S. Kirkpatrick, Jennifer Pizzano, Catherine Wilson, John Moffat, Leanna Staben, Xin Chen
Publikováno v:
Cancer Research. 80:5687-5687
The mammalian SWI/SNF complex catalyzes the remodeling of chromatin through the helicase activity of two mutually-exclusive, paralogous subunits, BRG1 and BRM. BRG1 is frequently mutated in cancer and its inactivation results in a cellular dependence
Autor:
Leanna Staben, Klaus Koefoed, Helga Raab, Cecile Chalouni, Yana Khalfin, Laura DePalatis, Kelly M. Loyet, Thomas H. Pillow, Min Xu, Byoung-Chul Lee, Peter S. Andersen, Emile Plise, Janice Kim, Elizabeth Luis, Martine Darwish, Rina Fong, Man-Wah Tan, Eric J. Brown, Patrick J. Lupardus, J. Hiroshi Morisaki, Summer Park, Sophie M. Lehar, Donghong Yan, Richard Vandlen, Joseph P. Lyssikatos, Magnus Strandh, Wouter L. W. Hazenbos, John A. Flygare, Sanjeev Mariathasan, Kimberly Kajihara, Hilda Hernandez, Jonathan Cheong
Publikováno v:
Nature. 527:323-328
Staphylococcus aureus is considered to be an extracellular pathogen. However, survival of S. aureus within host cells may provide a reservoir relatively protected from antibiotics, thus enabling long-term colonization of the host and explaining clini
Autor:
Geoffrey Del Rosario, Jun Guo, Jinhua Chen, Zijin Xu, Shang-Fan Yu, Gang Yan, Andrew Polson, Luna Liu, Rachana Ohri, Jeffrey Lau, Bing Zheng, Byoung-Chul Lee, H. Zhou, Keyang Xu, Jiawei Lu, John S. Wai, Leanna Staben, Josefa dela Cruz-Chuh, Thomas H. Pillow, Gail Lewis Phillips, Katherine R. Kozak, Wenwen Cai
Publikováno v:
ACS medicinal chemistry letters. 8(10)
The tubulysins are promising anticancer cytotoxic agents due to the clinical validation of their mechanism of action (microtubule inhibition) and their particular activity against multidrug-resistant tumor cells. Yet their high potency and subsequent