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Your search keyword '"Dragovich, Peter S."' showing total 18 results
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18 results on '"Dragovich, Peter S."'

2. The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results

Author

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., and Cho, Eunpi

Published
2024
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3. Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers

Author

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, and Yauch, Robert L.

Published
2022
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4. PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Author

Berlin, Michael, primary, Cantley, Jennifer, additional, Bookbinder, Mark, additional, Bortolon, Elizabeth, additional, Broccatelli, Fabio, additional, Cadelina, Greg, additional, Chan, Emily W., additional, Chen, Huifen, additional, Chen, Xin, additional, Cheng, Yunxing, additional, Cheung, Tommy K., additional, Davenport, Kim, additional, DiNicola, Dean, additional, Gordon, Debbie, additional, Hamman, Brian D., additional, Harbin, Alicia, additional, Haskell, Roy, additional, He, Mingtao, additional, Hole, Alison J., additional, Januario, Thomas, additional, Kerry, Philip S., additional, Koenig, Stefan G., additional, Li, Limei, additional, Merchant, Mark, additional, Pérez-Dorado, Inmaculada, additional, Pizzano, Jennifer, additional, Quinn, Connor, additional, Rose, Christopher M., additional, Rousseau, Emma, additional, Soto, Leofal, additional, Staben, Leanna R., additional, Sun, Hongming, additional, Tian, Qingping, additional, Wang, Jing, additional, Wang, Weifeng, additional, Ye, Crystal S., additional, Ye, Xiaofen, additional, Zhang, Penghong, additional, Zhou, Yuhui, additional, Yauch, Robert, additional, and Dragovich, Peter S., additional

Published
2024
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6. Supplementary Data from Calicheamicin Antibody–Drug Conjugates with Improved Properties

Author

Vollmar, Breanna S., primary, Frantz, Chris, primary, Schutten, Melissa M., primary, Zhong, Fiona, primary, del Rosario, Geoffrey, primary, Go, Mary Ann T., primary, Yu, Shang-Fan, primary, Leipold, Douglas D., primary, Kamath, Amrita V., primary, Ng, Carl, primary, Xu, Keyang, primary, dela Cruz-Chuh, Josefa, primary, Kozak, Katherine R., primary, Chen, Jinhua, primary, Xu, Zijin, primary, Wai, John, primary, Adhikari, Pragya, primary, Erickson, Hans K., primary, Dragovich, Peter S., primary, Polson, Andrew G., primary, and Pillow, Thomas H., primary

Published
2023
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7. Supplementary Data from 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

Author

Yu, Shang-Fan, primary, Lee, Donna W., primary, Zheng, Bing, primary, del Rosario, Geoffrey, primary, Leipold, Douglas, primary, Booler, Helen, primary, Zhong, Fiona, primary, Carrasco-Triguero, Montserrat, primary, Hong, Kyu, primary, Yan, Peter, primary, Rowntree, Rebecca K., primary, Schutten, Melissa M., primary, Pillow, Thomas, primary, Sadowsky, Jack D., primary, Dragovich, Peter S., primary, and Polson, Andrew G., primary

Published
2023
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8. Supplementary Table 1. Supplementary Figures 1 and 2. from Intratumoral Payload Concentration Correlates with the Activity of Antibody–Drug Conjugates

Author

Zhang, Donglu, primary, Yu, Shang-Fan, primary, Khojasteh, S. Cyrus, primary, Ma, Yong, primary, Pillow, Thomas H., primary, Sadowsky, Jack D., primary, Su, Dian, primary, Kozak, Katherine R., primary, Xu, Keyang, primary, Polson, Andrew G., primary, Dragovich, Peter S., primary, and Hop, Cornelis E.C.A., primary

Published
2023
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9. Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

Author

Kschonsak, Marc, primary, Jao, Christine C, additional, Arthur, Christopher P, additional, Rohou, Alexis L, additional, Bergeron, Philippe, additional, Ortwine, Daniel F, additional, McKerrall, Steven J, additional, Hackos, David H, additional, Deng, Lunbin, additional, Chen, Jun, additional, Li, Tianbo, additional, Dragovich, Peter S, additional, Volgraf, Matthew, additional, Wright, Matthew R, additional, Payandeh, Jian, additional, Ciferri, Claudio, additional, and Tellis, John C, additional

Published
2023
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10. Author response: Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

Author

Kschonsak, Marc, primary, Jao, Christine C, primary, Arthur, Christopher P, additional, Rohou, Alexis L, additional, Bergeron, Philippe, additional, Ortwine, Daniel F, additional, McKerrall, Steven J, additional, Hackos, David H, additional, Deng, Lunbin, additional, Chen, Jun, additional, Li, Tianbo, additional, Dragovich, Peter S, additional, Volgraf, Matthew, additional, Wright, Matthew R, additional, Payandeh, Jian, additional, Ciferri, Claudio, additional, and Tellis, John C, additional

Published
2023
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11. PROTACs Targeting BRM (SMARCA2) Afford Selective In VivoDegradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Author

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, and Dragovich, Peter S.

Abstract

The identification of VHL-binding proteolysis targeting chimeras (PROTACs) that potently degrade the BRM protein (also known as SMARCA2) in SW1573 cell-based experiments is described. These molecules exhibit between 10- and 100-fold degradation selectivity for BRM over the closely related paralog protein BRG1 (SMARCA4). They also selectively impair the proliferation of the H1944 “BRG1-mutant” NSCLC cell line, which lacks functional BRG1 protein and is thus highly dependent on BRM for growth, relative to the wild-type Calu6 line. In vivoexperiments performed with a subset of compounds identified PROTACs that potently and selectively degraded BRM in the Calu6 and/or the HCC2302 BRG1 mutant NSCLC xenograft models and also afforded antitumor efficacy in the latter system. Subsequent PK/PD analysis established a need to achieve strong BRM degradation (>95%) in order to trigger meaningful antitumor activity in vivo. Intratumor quantitation of mRNA associated with two genes whose transcription was controlled by BRM (PLAUand KRT80) also supported this conclusion.

Published
2024
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12. CryoEM reveals unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

Author

Kschonsak, Marc, primary, Jao, Christine C., additional, Arthur, Christopher P., additional, Rohou, Alexis L., additional, Bergeron, Philippe, additional, Ortwine, Daniel, additional, McKerrall, Steven J., additional, Hackos, David H., additional, Deng, Lunbin, additional, Chen, Jun, additional, Dragovich, Peter S., additional, Volgraf, Matthew, additional, Wright, Matthew R., additional, Payandeh, Jian, additional, Ciferri, Claudio, additional, and Tellis, John C., additional

Published
2022
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13. Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase

Author

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, and Purkey, Hans E.

Published
2022
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17. Degrader-antibody conjugates.

Author

Dragovich, Peter S.

Subjects
*SCIENTIFIC literature, *ANTIBODY-drug conjugates, *LIGASES, *MONOCLONAL antibodies, *PROTEINS, *UBIQUITINATION
Abstract

Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical linker. This review provides a current summary of the DAC field. Many general aspects associated with the creation and biological performance of traditional cytotoxic antibody-drug conjugates (ADCs) are initially presented. These characteristics are subsequently compared and contrasted with related parameters that impact DAC generation and biological activity. Several examples of DACs assembled from both the scientific and the patent literature are utilized to highlight differing strategies for DAC creation, and specific challenges associated with DAC construction are documented. Collectively, the assembled examples demonstrate that biologically-active DACs can be successfully prepared using a variety of PROTAC payloads which employ diverse E3 ligases to degrade multiple protein targets. [ABSTRACT FROM AUTHOR]

Published
2022
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18. Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody–Drug Conjugates with Phenol-Containing Payloads

Author

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., and Pillow, Thomas H.

Abstract

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 used to connect to the phenol of the cyclopropabenzindolone (CBI) (P1), the resulting ADC1showed loss of potency in CD22 target-expressing cancer cell lines (e.g., BJAB, WSU-DLCL2). In comparison, the conjugate (ADC2) of a cyclopropapyrroloindolone (CPI) (P2) was potent despite the two corresponding free drugs having similar picomolar cell-killing activity. Although the corresponding spirocyclization products of P1and P2, responsible for DNA alkylation, are a prominent component in buffer, the linker immolation was slow when the PAB was connected as an ether (PABE) to the phenol in P1compared to that in P2. Additional immolation studies with two other PABE-linked substituted phenol compounds showed that electron-withdrawing groups accelerated the immolation to release an acidic phenol-containing payload (to delocalize the negative charge on the anticipated anionic phenol oxygen during immolation). In contrast, efficient immolation of LD4did not result in an active ADC4because the payload (P4) had a low potency to kill cells. In addition, nonimmolation of LD5did not affect the cell-killing potency of its ADC5since immolation is not required for DNA alkylation by the center-linked pyrrolobenzodiazepine. Therefore, careful evaluation needs to be conducted when the Val-Cit-PAB linker is used to connect antibodies to a phenol-containing drug as the linker immolation, as well as payload potency and stability, affects the cell-killing activity of an ADC.

Published
2024
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