Search Results - "Dragovich, Peter"

Degrader-antibody conjugates by Dragovich, Peter S

“…Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody some type of…”
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Antibody–Drug Conjugates for Immunology by Dragovich, Peter S

“…The application of antibody–drug conjugates (ADCs) to fields outside of oncology is increasing but is still relatively uncommon. A recent publication describes…”
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Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer by Sampath, Deepak, Zabka, Tanja S, Misner, Dinah L, O'Brien, Thomas, Dragovich, Peter S

“…NAD is a metabolite that is an important cofactor and second messenger for a number of cellular processes such as genomic stability and metabolism that are…”
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Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers by 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.

“…The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently mutated in cancer and inactivation results in a cellular dependence on…”
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Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity by Pillow, Thomas H., Adhikari, Pragya, Blake, Robert A., Chen, Jinhua, Del Rosario, Geoffrey, Deshmukh, Gauri, Figueroa, Isabel, Gascoigne, Karen E., Kamath, Amrita V., Kaufman, Susan, Kleinheinz, Tracy, Kozak, Katherine R., Latifi, Brandon, Leipold, Douglas D., Sing Li, Chun, Li, Ruina, Mulvihill, Melinda M., O'Donohue, Aimee, Rowntree, Rebecca K., Sadowsky, Jack D., Wai, John, Wang, Xinxin, Wu, Cong, Xu, Zijin, Yao, Hui, Yu, Shang‐Fan, Zhang, Donglu, Zang, Richard, Zhang, Hongyan, Zhou, Hao, Zhu, Xiaoyu, Dragovich, Peter S.

“…The ability to selectively degrade proteins with bifunctional small molecules has the potential to fundamentally alter therapy in a variety of diseases…”
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Small-Molecule Lead-Finding Trends across the Roche and Genentech Research Organizations by Dragovich, Peter S, Haap, Wolfgang, Mulvihill, Melinda M, Plancher, Jean-Marc, Stepan, Antonia F

“…The origin of small-molecule leads that were pursued across the independent research organizations Roche and Genentech from 2009 to 2020 is described. The…”
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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα) by 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

“…[Display omitted] Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are…”
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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 by 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

“…Approved antibody-drug conjugates (ADCs) for HER2-positive breast cancer include trastuzumab emtansine and trastuzumab deruxtecan. To develop a differentiated…”
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Structural basis for resistance to diverse classes of NAMPT inhibitors by 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

“…Inhibiting NAD biosynthesis by blocking the function of nicotinamide phosphoribosyl transferase (NAMPT) is an attractive therapeutic strategy for targeting…”
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Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase by 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

“…A 2-amino-5-aryl-pyrazine was identified as an inhibitor of human lactate dehydrogenase A (LDHA) via a biochemical screening campaign. Biochemical and…”
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Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors by 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

“…The voltage-gated sodium (Na V ) channel Na V 1.7 has been identified as a potential novel analgesic target due to its involvement in human pain syndromes…”
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Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues by 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

“…Antibody-drug conjugates (ADCs) contain a disease-receptor antibody and a payload drug connected via a linker. The payload delivery depends on both tumor…”
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Catalytic Cleavage of Disulfide Bonds in Small Molecules and Linkers of Antibody-Drug Conjugates by 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

“…In cells, catalytic disulfide cleavage is an essential mechanism in protein folding and synthesis. However, detailed enzymatic catalytic mechanism relating…”
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Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody–Drug Conjugates by 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

“…Cytotoxic pyrrolobenzodiazepine (PBD)-dimer molecules are frequently utilized as payloads for antibody–drug conjugates (ADCs), and many examples are currently…”
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Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase by Zabka, Tanja S, Singh, Jatinder, Dhawan, Preeti, Liederer, Bianca M, Oeh, Jason, Kauss, Mara A, Xiao, Yang, Zak, Mark, Lin, Tori, McCray, Bobbi, La, Nghi, Nguyen, Trung, Beyer, Joseph, Farman, Cynthia, Uppal, Hirdesh, Dragovich, Peter S, O'Brien, Thomas, Sampath, Deepak, Misner, Dinah L

“…Nicotinamide phosphoribosyltransferase (NAMPT) is a pleiotropic protein with intra- and extra-cellular functions as an enzyme, cytokine, growth factor, and…”
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Calicheamicin Antibody-Drug Conjugates with Improved Properties by Vollmar, Breanna S, Frantz, Chris, Schutten, Melissa M, Zhong, Fiona, Del Rosario, Geoffrey, Go, Mary Ann T, Yu, Shang-Fan, Leipold, Douglas D, Kamath, Amrita V, Ng, Carl, Xu, Keyang, Dela Cruz-Chuh, Josefa, Kozak, Katherine R, Chen, Jinhua, Xu, Zijin, Wai, John, Adhikari, Pragya, Erickson, Hans K, Dragovich, Peter S, Polson, Andrew G, Pillow, Thomas H

“…Calicheamicin antibody-drug conjugates (ADCs) are effective therapeutics for leukemias with two recently approved in the United States: Mylotarg (gemtuzumab…”
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PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models by Berlin, Michael, Cantley, Jennifer, Bookbinder, Mark, Bortolon, Elizabeth, Broccatelli, Fabio, Cadelina, Greg, Chan, Emily W., Chen, Huifen, Chen, Xin, Cheng, Yunxing, Cheung, Tommy K., Davenport, Kim, DiNicola, Dean, Gordon, Debbie, Hamman, Brian D., Harbin, Alicia, Haskell, Roy, He, Mingtao, Hole, Alison J., Januario, Thomas, Kerry, Philip S., Koenig, Stefan G., Li, Limei, Merchant, Mark, Pérez-Dorado, Inmaculada, Pizzano, Jennifer, Quinn, Connor, Rose, Christopher M., Rousseau, Emma, Soto, Leofal, Staben, Leanna R., Sun, Hongming, Tian, Qingping, Wang, Jing, Wang, Weifeng, Ye, Crystal S., Ye, Xiaofen, Zhang, Penghong, Zhou, Yuhui, Yauch, Robert, Dragovich, Peter S.

“…The identification of VHL-binding proteolysis targeting chimeras (PROTACs) that potently degrade the BRM protein (also known as SMARCA2) in SW1573 cell-based…”
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An Anti-CD22- seco -CBI-Dimer Antibody-Drug Conjugate (ADC) for the Treatment of Non-Hodgkin Lymphoma That Provides a Longer Duration of Response than Auristatin-Based ADCs in Preclinical Models by Yu, Shang-Fan, Lee, Donna W, Zheng, Bing, Del Rosario, Geoffrey, Leipold, Douglas, Booler, Helen, Zhong, Fiona, Carrasco-Triguero, Montserrat, Hong, Kyu, Yan, Peter, Rowntree, Rebecca K, Schutten, Melissa M, Pillow, Thomas, Sadowsky, Jack D, Dragovich, Peter S, Polson, Andrew G

“…We are interested in developing a second generation of antibody-drug conjugates (ADCs) for the treatment of non-Hodgkin lymphoma (NHL) that could provide a…”
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From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors by 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

“…[Display omitted] A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight…”
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Carfilzomib Is Not an Appropriate Payload of Antibody-Drug Conjugates Due to Rapid Inactivation by Lysosomal Enzymes by Ma, Yong, Dela Cruz-Chuh, Josefa, Khojasteh, S Cyrus, Dragovich, Peter S, Pillow, Thomas H, Zhang, Donglu

“…Carfilzomib (CFZ) is a proteasome inhibitor used for oncology indications including treating multiple myeloma. CFZ is a potent cytotoxic agent with an IC value…”
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