Search Results - "Prajapati, Sudeep"

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma by Joshi, Jaya Julie, Coffey, Heather, Corcoran, Erik, Tsai, Jennifer, Huang, Chia-Ling, Ichikawa, Kana, Prajapati, Sudeep, Hao, Ming-Hong, Bailey, Suzanna, Wu, Jeremy, Rimkunas, Victoria, Karr, Craig, Subramanian, Vanitha, Kumar, Pavan, MacKenzie, Crystal, Hurley, Raelene, Satoh, Takashi, Yu, Kun, Park, Eunice, Rioux, Nathalie, Kim, Amy, Lai, Weidong G, Yu, Lihua, Zhu, Ping, Buonamici, Silvia, Larsen, Nicholas, Fekkes, Peter, Wang, John, Warmuth, Markus, Reynolds, Dominic J, Smith, Peter G, Selvaraj, Anand

“…Activation of the fibroblast growth factor receptor FGFR4 by FGF19 drives hepatocellular carcinoma (HCC), a disease with few, if any, effective treatment…”
Get full text

H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers by Seiler, Michael, Yoshimi, Akihide, Darman, Rachel, Chan, Betty, Keaney, Gregg, Thomas, Michael, Agrawal, Anant A, Caleb, Benjamin, Csibi, Alfredo, Sean, Eckley, Fekkes, Peter, Karr, Craig, Klimek, Virginia, Lai, George, Lee, Linda, Kumar, Pavan, Lee, Stanley Chun-Wei, Liu, Xiang, Mackenzie, Crystal, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Peng, Shouyong, Prajapati, Sudeep, Taylor, Justin, Teng, Teng, Wang, John, Warmuth, Markus, Yao, Huilan, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter G, Buonamici, Silvia

“…The small molecule H3B-8800 selectively modulates RNA splicing to preferentially kill tumor cells bearing mutations in genes encoding spliceosome components…”
Get full text

Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A–SF3b complex by Teng, Teng, Tsai, Jennifer HC, Puyang, Xiaoling, Seiler, Michael, Peng, Shouyong, Prajapati, Sudeep, Aird, Daniel, Buonamici, Silvia, Caleb, Benjamin, Chan, Betty, Corson, Laura, Feala, Jacob, Fekkes, Peter, Gerard, Baudouin, Karr, Craig, Korpal, Manav, Liu, Xiang, T. Lowe, Jason, Mizui, Yoshiharu, Palacino, James, Park, Eunice, Smith, Peter G., Subramanian, Vanitha, Wu, Zhenhua Jeremy, Zou, Jian, Yu, Lihua, Chicas, Agustin, Warmuth, Markus, Larsen, Nicholas, Zhu, Ping

“…Pladienolide, herboxidiene and spliceostatin have been identified as splicing modulators that target SF3B1 in the SF3b subcomplex. Here we report that PHF5A,…”
Get full text

Annulation of Thioimidates and Vinyl Carbodiimides to Prepare 2-Aminopyrimidines, Competent Nucleophiles for Intramolecular Alkyne Hydroamination. Synthesis of (−)-Crambidine by Perl, Nicholas R, Ide, Nathan D, Prajapati, Sudeep, Perfect, Hahdi H, Durón, Sergio G, Gin, David Y

“…A convergent synthesis of (−)-crambidine is reported. The sequence capitalizes on two novel key transformations, including a [4+2] annulation of thioimidates…”
Get full text

Estrogen Receptor Covalent Antagonists: The Best Is Yet to Come by Furman, Craig, Hao, Ming-Hong, Prajapati, Sudeep, Reynolds, Dominic, Rimkunas, Victoria, Zheng, Guo Z, Zhu, Ping, Korpal, Manav

“…The development of tamoxifen and subsequent estrogen receptor alpha (ERα) antagonists represents a tremendous therapeutic breakthrough in the treatment of…”
Get full text

REM-422, a Potent, Selective, Oral Small Molecule mRNA Degrader of the MYB Oncogene, Demonstrates Anti-Tumor Activity in Mouse Xenograft Models of AML by Prajapati, Sudeep, Cameron, Michael, Dunyak, Bryan M., Shan, Mengge, Siu, Y. Amy, Levin-Furtney, Samantha, Powe, Joshua, Burchfiel, Eileen T.M., Cabral, Sarah E., Harney, Alycen M., Keenan, Regina K., Larpenteur, Kevin M., Maag, Jesper L.V., Snyder, Andrew R., Nguyen, Dan T., Blaustein, Cecile, Buonamici, Silvia, Reynolds, Dominic, Schnaderbeck, Matthew J., Seiler, Michael, Vaillancourt, Frédéric H., Smith, Peter, Kaprielian, Zaven, Kung, Charles

“…The c-MYB (MYB) oncogenic transcription factor is a key regulator of hematopoietic cell differentiation and proliferation. Recurrent genetic lesions or…”
Get full text

Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA) by Rioux, Nathalie, Smith, Sherri, Korpal, Manav, O’Shea, Morgan, Prajapati, Sudeep, Zheng, Guo Zhu, Warmuth, Markus, Smith, Peter G.

“…Purpose H3B-6545, a novel selective estrogen receptor (ER)α covalent antagonist (SERCA) which inactivates both wild-type and mutant ERα, is in clinical…”
Get full text

Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer by Furman, Craig, Puyang, Xiaoling, Zhang, Zhaojie, Wu, Zhenhua J, Banka, Deepti, Aithal, Kiran B, Albacker, Lee A, Hao, Ming-Hong, Irwin, Sean, Kim, Amy, Montesion, Meagan, Moriarty, Alyssa D, Murugesan, Karthikeyan, Nguyen, Tuong-Vi, Rimkunas, Victoria, Sahmoud, Tarek, Wick, Michael J, Yao, Shihua, Zhang, Xun, Zeng, Hao, Vaillancourt, Frédéric H, Bolduc, David M, Larsen, Nicholas, Zheng, Guo Zhu, Prajapati, Sudeep, Zhu, Ping, Korpal, Manav

“…Nearly 30% of patients with relapsed breast cancer present activating mutations in estrogen receptor alpha (ERα) that confer partial resistance to existing…”
Get full text

Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWT and ERaMUT breast cancer by Korpal, Manav, Furman, Craig, Puyang, Xiaoling, Zhang, Zhaojie, Wu, Zhenhua, Banka, Deepti, Das, Subhasree, Destenaves, Benoit, Gao, Lei, Hamilton, Erika, Hao, Ming-Hong, Irwin, Sean, Johnston, Stephen, Joshi, Jaya J, Juric, Dejan, Kim, Amy, Nguyen, Tuong-Vi, Pipas, Marc, Pluard, Timothy, Rimkunas, Victoria, Rioux, Nathalie, Schindler, Joanne, Smith, Peter, Thomas, Michael, Wang, John, Wang, Judy S, Warmuth, Markus, Yao, Huilan, Yao, Shihua, Yu, Lihua, Vaillancourt, Frédéric H, Bolduc, David M, Larsen, Nicholas A, Zheng, GuoZhu, Prajapati, Sudeep, Sahmoud, Tarek, Gualberto, Antonio, Zhu, Ping

“…Abstract Mutations in the ligand-binding domain of estrogen receptor alpha (ERα) are detected in up to 30% of patients (pts) who have relapsed or progressed…”
Get full text

Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3 by Brawn, Ryan A, Cook, Andrew, Omoto, Kiyoyuki, Ke, Jiyuan, Karr, Craig, Colombo, Federico, Virrankoski, Milena, Prajapati, Sudeep, Reynolds, Dominic, Bolduc, David M, Nguyen, Tuong-Vi, Gee, Patricia, Borrelli, Deanna, Caleb, Benjamin, Yao, Shihua, Irwin, Sean, Larsen, Nicholas A, Selvaraj, Anand, Zhao, Xuesong, Ioannidis, Stephanos

“…Fibroblast growth factor receptors (FGFR) 2 and 3 have been established as drivers of numerous types of cancer with multiple drugs approved or entering late…”
Get full text

Combined inhibition of FGFR4 and VEGFR signaling enhances efficacy in FGF19 driven hepatocellular carcinoma by Zhao, Xuesong, Joshi, Jaya Julie, Aird, Daniel, Karr, Craig, Yu, Kun, Huang, Chialing, Colombo, Federico, Virrankoski, Milena, Prajapati, Sudeep, Selvaraj, Anand

“…Hepatocellular carcinoma (HCC) is an aggressive liver malignancy that is difficult to treat with no approved biomarker based targeted therapies. FGF19-FGFR4…”
Get full text

In vitro-in vivo correlation of clearance for H3B-5942, a novel selective erα covalent antagonist (SERCA) by Colombo, Federico, Smith, Sherri, Korpal, Manav, Hao, Ming-Hung, Nix, Darrel, O’Shea, Morgan, Prajapati, Sudeep, Wang, John, Warmuth, Markus, Smith, Peter, Rioux, Nathalie

Get full text

Abstract 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma by Selvaraj, Anand, Corcoran, Erik, Coffey, Heather, Prajapati, Sudeep, Hao, Ming-Hong, Larsen, Nicholas, Tsai, Jennifer, Satoh, Takashi, Ichikawa, Kana, Joshi, Julie Jaya, Hurley, Raelene, Wu, Jeremy, Huang, Chia-Ling, Bailey, Suzanna, Karr, Craig, Kumar, Pavan, Rimkunas, Victoria, Mackenzie, Crystal, Rioux, Nathalie, Kim, Amy, Akare, Sandeep, Lai, George, Yu, Lihua, Fekkes, Peter, Wang, John, Warmuth, Markus, Smith, Peter, Reynolds, Dominic

“…Abstract Hepatocellular carcinoma (HCC) has limited treatment options and generally poor prognosis. Recent genomic studies have identified FGF19 as a driver…”
Get full text

H3B-8800, an Orally Bioavailable Modulator of the SF3b Complex, Shows Efficacy in Spliceosome-Mutant Myeloid Malignancies by Buonamici, Silvia, Yoshimi, Akihide, Thomas, Michael, Seiler, Michael, Chan, Betty, Caleb, Benjamin, Darman, Rachel, Fekkes, Peter, Karr, Craig, Keaney, Gregg F., Klimek, Virginia M., Kunii, Kaiko, Lee, Linda, Lee, Stanley Chun-Wei, Liu, Xiang, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Prajapati, Sudeep, Taylor, Justin, Wang, John, Warmuth, Markus, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter G

“…Mutations in RNA splicing factors confer an alteration of function and are common in patients with myelodysplastic syndrome (MDS, ~45%), chronic myelomonocytic…”
Get full text

Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers by Buonamici, Silvia, Yoshimi, Akihide, Thomas, Michael, Seiler, Michael, Chan, Betty, Caleb, Benjamin, Csibi, Fred, Darman, Rachel, Fekkes, Peter, Karr, Craig, Keaney, Gregg, Kim, Amy, Klimek, Virginia, Kumar, Pavan, Kunii, Kaiko, Lee, Stanley Chun-Wei, Liu, Xiang, MacKenzie, Crystal, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Prajapati, Sudeep, Rioux, Nathalie, Taylor, Justin, Wang, John, Warmuth, Markus, Yao, Huilan, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter

“…Abstract Genomic characterization of hematologic and solid cancers has revealed recurrent somatic mutations affecting genes encoding the RNA splicing factors…”
Get full text

Total Synthesis of 6‑Deoxypladienolide D and Assessment of Splicing Inhibitory Activity in a Mutant SF3B1 Cancer Cell Line by Arai, Kenzo, Buonamici, Silvia, Chan, Betty, Corson, Laura, Endo, Atsushi, Gerard, Baudouin, Hao, Ming-Hong, Karr, Craig, Kira, Kazunobu, Lee, Linda, Liu, Xiang, Lowe, Jason T, Luo, Tuoping, Marcaurelle, Lisa A, Mizui, Yoshiharu, Nevalainen, Marta, O’Shea, Morgan Welzel, Park, Eun Sun, Perino, Samantha A, Prajapati, Sudeep, Shan, Mingde, Smith, Peter G, Tivitmahaisoon, Parcharee, Wang, John Yuan, Warmuth, Markus, Wu, Kuo-Ming, Yu, Lihua, Zhang, Huiming, Zheng, Guo-Zhu, Keaney, Gregg F

“…A total synthesis of the natural product 6-deoxypladienolide D (1) has been achieved. Two noteworthy attributes of the synthesis are (1) a late-stage allylic…”
Get full text

Abstract 2941: Targeting MCL1-dependent cancers through RNA splicing modulation by Park, Eun Sun, Aicher, Michelle, Aird, Daniel, Buonamici, Silvia, Chan, Betty, Eifert, Cheryl, Fekkes, Peter, Furman, Craig, Gerard, Baudouin, Karr, Craig, Keaney, Gregg, Kunii, Kaiko, Lee, Linda, Pazolli, Ermira, Prajapati, Sudeep, Satoh, Takashi, Smith, Peter, Wang, John Yuan, Wang, Karen, Warmuth, Markus, Yu, Lihua, Zhu, Ping, Mizui, Yoshiharu, Corson, Laura B.

“…Abstract Myeloid cell leukemia 1 (MCL1) is a member of the BCL2-family of proteins governing the apoptosis pathway and is one of the most frequently amplified…”
Get full text

Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERα WT and ERα MUT Breast Cancer by Puyang, Xiaoling, Furman, Craig, Zheng, Guo Zhu, Wu, Zhenhua J, Banka, Deepti, Aithal, Kiran, Agoulnik, Sergei, Bolduc, David M, Buonamici, Silvia, Caleb, Benjamin, Das, Subhasree, Eckley, Sean, Fekkes, Peter, Hao, Ming-Hong, Hart, Andrew, Houtman, René, Irwin, Sean, Joshi, Jaya J, Karr, Craig, Kim, Amy, Kumar, Namita, Kumar, Pavan, Kuznetsov, Galina, Lai, Weidong G, Larsen, Nicholas, Mackenzie, Crystal, Martin, Lesley-Ann, Melchers, Diana, Moriarty, Alyssa, Nguyen, Tuong-Vi, Norris, John, O'Shea, Morgan, Pancholi, Sunil, Prajapati, Sudeep, Rajagopalan, Sujatha, Reynolds, Dominic J, Rimkunas, Victoria, Rioux, Nathalie, Ribas, Ricardo, Siu, Amy, Sivakumar, Sasirekha, Subramanian, Vanitha, Thomas, Michael, Vaillancourt, Frédéric H, Wang, John, Wardell, Suzanne, Wick, Michael J, Yao, Shihua, Yu, Lihua, Warmuth, Markus, Smith, Peter G, Zhu, Ping, Korpal, Manav

“…Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to 30% of patients who have…”
Get more information

Abstract 5564: Total synthesis of 6-deoxypladienolide D and assessment of splicing inhibitory activity in a mutant SF3B1 cancer cell line by Arai, Kenzo, Buonamici, Silvia, Chan, Betty, Corson, Laura, Endo, Atsushi, Gerard, Baudouin, Hao, Ming-Hong, Karr, Craig, Kira, Kazunobu, Lee, Linda, Liu, Xiang, Lowe, Jason T., Luo, Tuoping, Marcaurelle, Lisa A., Mizui, Yoshiharu, Nevalainen, Marta, Welzel O'Shea, Morgan, Park, Eun Sun, Perino, Samantha A., Prajapati, Sudeep, Shan, Mingde, Smith, Peter G., Tivitmahaisoon, Parcharee, Wang, John Yuan, Warmuth, Markus, Wu, Kuo-Ming, Yu, Lihua, Zhang, Huiming, Zheng, Guo Zhu, Keaney, Gregg F.

“…Abstract Hotspot mutations in several components of the spliceosome have been reported in various hematological (CLL, MDS, etc.) and solid tumor (melanoma,…”
Get full text

Efforts toward the synthesis of polycyclic guanidine natural products using a versatile [4 + 2]-heteroannulation strategy by Prajapati, Sudeep

“…The crambescidin and saxitoxin families of alkaloids comprise a class of natural products with significant biological and chemical interest. While the…”
Get full text