Search Results - "Pizzano, Jennifer"

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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Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs by Kou, Ponien, Levy, Elizabeth S, Nguyen, An D, Zhang, Donglu, Chen, Shu, Cui, Yusi, Zhang, Xing, Broccatelli, Fabio, Pizzano, Jennifer, Cantley, Jennifer, Bortolon, Elizabeth, Rousseau, Emma, Berlin, Michael, Dragovich, Peter, Sethuraman, Vijay

“…Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development. They have rapidly evolved in recent years, with several of them in…”
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Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs by 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.

“…Background Proteolysis-targeting chimeras (PROTACs) are being developed for therapeutic use. However, they have poor pharmacokinetic profiles and their tissue…”
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Evaluation of Cynomolgus Monkey Pregnane X Receptor, Primary Hepatocyte, and in Vivo Pharmacokinetic Changes in Predicting Human CYP3A4 Induction by Kim, Sean, Dinchuk, Joseph E, Anthony, Monique N, Orcutt, Tami, Zoeckler, Mary E, Sauer, Mary B, Mosure, Kathleen W, Vuppugalla, Ragini, Grace, Jr, James E, Simmermacher, Jean, Dulac, Heidi A, Pizzano, Jennifer, Sinz, Michael

“…Monkeys have been proposed as an animal model to predict the magnitude of human clinical drug-drug interactions caused by CYP3A4 enzyme induction. To evaluate…”
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Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models by Gough, Sheryl M, Flanagan, John J, Teh, Jessica, Andreoli, Monica, Rousseau, Emma, Pannone, Melissa, Bookbinder, Mark, Willard, Ryan, Davenport, Kim, Bortolon, Elizabeth, Cadelina, Gregory, Gordon, Debbie, Pizzano, Jennifer, Macaluso, Jennifer, Soto, Leofal, Corradi, John, Digianantonio, Katherine, Drulyte, Ieva, Morgan, Alicia, Quinn, Connor, Békés, Miklós, Ferraro, Caterina, Chen, Xin, Wang, Gan, Dong, Hanqing, Wang, Jing, Langley, David R, Houston, John, Gedrich, Richard, Taylor, Ian C

“…Estrogen receptor (ER) alpha signaling is a known driver of ER-positive (ER+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer…”
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Abstract 43: Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer by Snyder, Lawrence B., Neklesa, Taavi K., Chen, Xin, Dong, Hanqing, Ferraro, Caterina, Gordon, Deborah A., Macaluso, Jennifer, Pizzano, Jennifer, Wang, Jing, Willard, Ryan R., Vitale, Nicholas, Peck, Ron, Moore, Marcia Dougan, Crews, Craig M., Houston, John, Crew, Andrew P., Taylor, Ian

“…Abstract Prostate cancer is the second leading cause of cancer death in men in the United States. The androgen receptor (AR) plays critical roles in both early…”
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Abstract 3075: Enhanced efficacy of ARV-471, a novel PROTAC® estrogen receptor degrader, in combination with targeted agents in estrogen receptor-positive (ER+) breast cancer models by Teh, Jessica, Bortolon, Elizabeth, Pizzano, Jennifer, Pannone, Melissa, Landrette, Sean, Gedrich, Richard, Taylor, Ian

“…Abstract ARV-471 is a selective, orally bioavailable PROteolysis-TArgeting Chimera (PROTAC®) small molecule that induces wild-type and mutant estrogen receptor…”
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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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Potent and Orally Bioavailable BCL6 PROTAC TM Degraders Demonstrate Efficacy in Pre-Clinical Models of Diffuse Large B-Cell Lymphoma (DLBCL) by Gough, Sheryl M, Sherman, Dan, DeCarr, Lynn, Eaton, Sarah, Milanovic, Maja, Bookbinder, Mark, Pizzano, Jennifer, Altieri, Martha, Corradi, John, Xiao, Hong, Gallego, Felipe, Soto, Leofal, Lingamaneni, Ram, Chen, Xin, Zhang, Wei, Wang, Gan, Dong, Hanqing, Chirnomas, Deborah, Berlin, Michael, Hornberger, Keith, Snyder, Lawrence, Taylor, Ian

“…The BCL6 transcription repressor (B-cell lymphoma 6, BCL6) protein has been shown to be a key molecular driver of diffuse large B-cell lymphoma (DLBCL)…”
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Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer by Snyder, Lawrence B., Flanagan, John J., Qian, Yimin, Gough, Sheryl M., Andreoli, Monica, Bookbinder, Mark, Cadelina, Gregory, Bradley, John, Rousseau, Emma, Chandler, Julian, Willard, Ryan, Pizzano, Jennifer, Crews, Craig M., Crew, Andrew P., Houston, John, Moore, Marcia Dougan, Peck, Ron, Taylor, Ian

“…Abstract ARV-471, an estrogen receptor (ER) alpha PROTAC® protein degrader, is a hetero-bifunctional molecule that facilitates the interactions between…”
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Abstract 5687: Selective, chemically-induced degradation of BRM ( SMARCA2 ) enables in vivo efficacy in BRG1 ( SMARCA4 )-deficient xenograft tumor models by Berlin, Michael, Cantley, Jennifer, Wang, Jing, Bookbinder, Mark, Cadelina, Gregory, Chan, Emily, Chen, Huifen, Chen, Xin, Davenport, Kim, Fernando, Tharu, Gordon, Debbie, Hamman, Brian, Haskell, Roy, Ishchenko, Alexey, Kirkpatrick, Donald S., Maher, Jonathan, Merchant, Mark, Moffat, John, Morgan, Alicia, Nguyen, An, Pizzano, Jennifer, Quinn, Connor, Rose, Christopher M., Rousseau, Emma, Sethuraman, Vijay, Staben, Leanna, Wilson, Catherine, Ye, Xiaofen, Broccatelli, Fabio, Yauch, Robert, Dragovich, Peter S.

“…Abstract The mammalian SWI/SNF complex catalyzes the remodeling of chromatin through the helicase activity of two mutually-exclusive, paralogous subunits, BRG1…”
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ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer by Neklesa, Taavi, Snyder, Lawrence B, Willard, Ryan R, Vitale, Nicholas, Pizzano, Jennifer, Gordon, Deborah A, Bookbinder, Mark, Macaluso, Jennifer, Dong, Hanqing, Ferraro, Caterina, Wang, Gan, Wang, Jing, Crews, Craig M, Houston, John, Crew, Andrew P, Taylor, Ian

“…Abstract only 259 Background: The Androgen Receptor (AR) remains the principal driver of castration-resistant prostate cancer during the transition from a…”
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Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer by Neklesa, Taavi, Snyder, Lawrence B., Willard, Ryan R., Vitale, Nicholas, Raina, Kanak, Pizzano, Jennifer, Gordon, Deborah, Bookbinder, Mark, Macaluso, Jennifer, Dong, Hanqing, Liu, Zheng, Ferraro, Caterina, Wang, Gan, Wang, Jing, Crews, Craig M., Houston, John, Crew, Andrew P., Taylor, Ian

“…Abstract The Androgen Receptor (AR) remains the principal driver of castration-resistant prostate cancer during the transition from a localized to metastatic…”
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Abstract 432: Mechanisms of acquired resistance to ARV-471, a novel PROTAC® estrogen receptor degrader by Teh, Jessica, Bessonett, Shannon, Wu, Wendy, Kuhlberg, Christopher, Wynne, Alissa, Landrette, Sean, Andreoli, Monica, Bortolon, Elizabeth, Pizzano, Jennifer, Gedrich, Richard, Taylor, Ian

“…Abstract ARV-471 is an orally bioavailable cereblon (CRBN)-based PROteolysis-TArgeting Chimera (PROTAC®) small molecule that demonstrates superior ER…”
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An oral androgen receptor PROTAC degrader for prostate cancer by Neklesa, Taavi, Snyder, Lawrence B, Willard, Ryan R, Vitale, Nicholas, Raina, Kanak, Pizzano, Jennifer, Gordon, Deborah A, Bookbinder, Mark, Macaluso, Jennifer, Dong, Hanqing, Liu, Zheng, Ferraro, Caterina, Wang, Gan, Wang, Jing, Crews, Craig M, Houston, John, Crew, Andrew P, Taylor, Ian

“…Abstract only 381 Background: The Androgen Receptor (AR) remains the principal driver of castration-resistant prostate cancer during the transition from a…”
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Abstract PR09: KRAS-targeted PROTAC degraders are broadly efficacious against KRAS-dependent tumor models by Smith, Kathryn, Lopez-Arroyo, Andrea, Berk, Jason, Hegan, Peter, Nower, Peter, Tice, Samantha, Moutran, Aurelie, Pizzano, Jennifer, Dowtin, Amanda, Bookbinder, Mark, Bortolon, Elizabeth, Cadelina, Greg, Karim, Fazlul, Digianantonio, Katie, Bekes, Miklos, Medina, Jesus

“…Abstract KRAS is genomically altered in about one third of all human tumors. Due to its central role in oncogenesis, many attempts have been made in the last…”
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Role of regional absorption and gastrointestinal motility on variability in oral absorption of a model drug by Narang, Ajit S., Balakrishnan, Anand, Morrison, John, Li, Jinjiang, Wang, Jennifer, Gu, Huidong, Taylor, Katrina, Santone, Kenneth, Ehrmann, Jon, Beyer, Sophie, Lu, Xujin, Ketner, Rod, Pizzano, Jennifer, Orcutt, Tami, Shields, Eric, Dulac, Heidi, Aborn, Sharon, Batchelder, Margaret, Lentz, Kimberley

“…[Display omitted] Variability in oral absorption in pre-clinical species makes human dose projection challenging. In this study, we investigated the…”
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Evaluation of Cynomolgus Monkey Pregnane X Receptor, Primary Hepatocyte, and in Vivo Pharmacokinetic Changes in Predicting Human CYP3A4 Inductions by KIM, Sean, DINCHUK, Joseph E, DULAC, Heidi A, PIZZANO, Jennifer, SINZ, Michael, ANTHONY, Monique N, ORCUTT, Tami, ZOECKLER, Mary E, SAUER, Mary B, MOSURE, Kathleen W, VUPPUGALLA, Ragini, GRACE, James E, SIMMERMACHER, Jean

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Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential by Kim, Sean, Pray, Devin, Zheng, Ming, Morgan, Daniel G, Pizzano, Jennifer G, Zoeckler, Mary E, Chimalakonda, Anjaneya, Sinz, Michael W

“…The SXR humanized mouse model was used to quantitatively assess an in vivo induction response of the human PXR agonist, rifampicin. Three days of rifampicin…”
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