Search Results - "To, Ciric"

Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors by Beyett, Tyler S., To, Ciric, Heppner, David E., Rana, Jaimin K., Schmoker, Anna M., Jang, Jaebong, De Clercq, Dries J. H., Gomez, Gabriel, Scott, David A., Gray, Nathanael S., Jänne, Pasi A., Eck, Michael J.

“…Lung cancer is frequently caused by activating mutations in the epidermal growth factor receptor (EGFR). Allosteric EGFR inhibitors offer promise as the next…”
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Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations by Jang, Jaebong, To, Ciric, De Clercq, Dries J. H., Park, Eunyoung, Ponthier, Charles M., Shin, Bo Hee, Mushajiang, Mierzhati, Nowak, Radosław P., Fischer, Eric S., Eck, Michael J., Jänne, Pasi A., Gray, Nathanael S.

“…Targeting epidermal growth factor receptor (EGFR) through an allosteric mechanism provides a potential therapeutic strategy to overcome drug‐resistant EGFR…”
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EGFR-Mutated Lung Cancers Resistant to Osimertinib through EGFR C797S Respond to First-Generation Reversible EGFR Inhibitors but Eventually Acquire EGFR T790M/C797S in Preclinical Models and Clinical Samples by Rangachari, Deepa, To, Ciric, Shpilsky, Jason E, VanderLaan, Paul A, Kobayashi, Susumu S, Mushajiang, Mierzhati, Lau, Christie J, Paweletz, Cloud P, Oxnard, Geoffrey R, Jänne, Pasi A, Costa, Daniel B

“…Osimertinib is approved for advanced EGFR-mutated NSCLC, and identification of on-target mechanisms of resistance (i.e., EGFR C797S) to this third-generation…”
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Dimethyl fumarate and the oleanane triterpenoids, CDDO-imidazolide and CDDO-methyl ester, both activate the Nrf2 pathway but have opposite effects in the A/J model of lung carcinogenesis by To, Ciric, Ringelberg, Carol S, Royce, Darlene B, Williams, Charlotte R, Risingsong, Renee, Sporn, Michael B, Liby, Karen T

“…Lung cancer accounts for the highest number of cancer-related deaths in the USA, highlighting the need for better prevention and therapy. Activation of the…”
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An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer by To, Ciric, Beyett, Tyler S, Jang, Jaebong, Feng, William W, Bahcall, Magda, Haikala, Heidi M, Shin, Bo H, Heppner, David E, Rana, Jaimin K, Leeper, Brittaney A, Soroko, Kara M, Poitras, Michael J, Gokhale, Prafulla C, Kobayashi, Yoshihisa, Wahid, Kamal, Kurppa, Kari J, Gero, Thomas W, Cameron, Michael D, Ogino, Atsuko, Mushajiang, Mierzhati, Xu, Chunxiao, Zhang, Yanxi, Scott, David A, Eck, Michael J, Gray, Nathanael S, Jänne, Pasi A

“…Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant…”
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The PARP Inhibitors, Veliparib and Olaparib, Are Effective Chemopreventive Agents for Delaying Mammary Tumor Development in BRCA1-deficient Mice by CIRIC TO, KIM, Eun-Hee, ROYCE, Darlene B, WILLIAMS, Charlotte R, COLLINS, Ryan M, RISINGSONG, Renee, SPORN, Michael B, LIBY, Karen T

“…Poly-ADP ribose polymerase (PARP) inhibitors are effective for the treatment of BRCA-deficient tumors. Women with these mutations have an increased risk of…”
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Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality by Li, Zhengnian, Jiang, Jie, Ficarro, Scott B., Beyett, Tyler S., To, Ciric, Tavares, Isidoro, Zhu, Yingde, Li, Jiaqi, Eck, Michael J., Jänne, Pasi A., Marto, Jarrod A., Zhang, Tinghu, Che, Jianwei, Gray, Nathanael S.

“…A systematic strategy to develop dual-warhead inhibitors is introduced to circumvent the limitations of conventional covalent inhibitors such as vulnerability…”
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Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations by Jang, Jaebong, To, Ciric, De Clercq, Dries J. H., Park, Eunyoung, Ponthier, Charles M., Shin, Bo Hee, Mushajiang, Mierzhati, Nowak, Radosław P., Fischer, Eric S., Eck, Michael J., Jänne, Pasi A., Gray, Nathanael S.

“…Targeting epidermal growth factor receptor (EGFR) through an allosteric mechanism provides a potential therapeutic strategy to overcome drug‐resistant EGFR…”
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Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor by To, Ciric, Jang, Jaebong, Chen, Ting, Park, Eunyoung, Mushajiang, Mierzhati, De Clercq, Dries J H, Xu, Man, Wang, Stephen, Cameron, Michael D, Heppner, David E, Shin, Bo Hee, Gero, Thomas W, Yang, Annan, Dahlberg, Suzanne E, Wong, Kwok-Kin, Eck, Michael J, Gray, Nathanael S, Jänne, Pasi A

“…Allosteric kinase inhibitors offer a potentially complementary therapeutic strategy to ATP-competitive kinase inhibitors due to their distinct sites of target…”
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Abstract 30: Intermittent treatment with the PARP inhibitor olaparib delays tumor development in BRCA1-deficient mice by Liby, Karen T., To, Ciric

“…Abstract Women with inherited BRCA gene mutations are at extremely high risk for developing breast cancer. Although these high risk patients are ideal…”
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Discovery of a potent dual ALK and EGFR T790M inhibitor by Jang, Jaebong, Son, Jung Beom, To, Ciric, Bahcall, Magda, Kim, So Young, Kang, Seock Yong, Mushajiang, Mierzhati, Lee, Younho, Jänne, Pasi A., Choi, Hwan Geun, Gray, Nathanael S.

“…The mutational activations of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) are validated oncogenic events and the targets of…”
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Design of a “Two-in-One” Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites by Wittlinger, Florian, Heppner, David E, To, Ciric, Günther, Marcel, Shin, Bo Hee, Rana, Jaimin K, Schmoker, Anna M, Beyett, Tyler S, Berger, Lena M, Berger, Benedict-Tilman, Bauer, Nicolas, Vasta, James D, Corona, Cesear R, Robers, Matthew B, Knapp, Stefan, Jänne, Pasi A, Eck, Michael J, Laufer, Stefan A

“…Inhibitors targeting the epidermal growth factor receptor (EGFR) are an effective therapy for patients with non-small cell lung cancer harboring drug-sensitive…”
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Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC by Gero, Thomas W., Heppner, David E., Beyett, Tyler S., To, Ciric, Azevedo, Seth C., Jang, Jaebong, Bunnell, Thomas, Feru, Frederic, Li, Zhengnian, Shin, Bo Hee, Soroko, Kara M., Gokhale, Prafulla C., Gray, Nathanael S., Jänne, Pasi A., Eck, Michael J., Scott, David A.

“…[Display omitted] The C797S mutation confers resistance to covalent EGFR inhibitors used in the treatment of lung tumors with the activating L858R mutation…”
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Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors by De Clercq, Dries J. H, Heppner, David E, To, Ciric, Jang, Jaebong, Park, Eunyoung, Yun, Cai-Hong, Mushajiang, Mierzhati, Shin, Bo Hee, Gero, Thomas W, Scott, David A, Jänne, Pasi A, Eck, Michael J, Gray, Nathanael S

“…Allosteric kinase inhibitors represent a promising new therapeutic strategy for targeting kinases harboring oncogenic driver mutations in cancers. Here, we…”
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Design of a “two-in-one” mutant-selective EGFR inhibitor that spans the orthosteric and allosteric sites by Wittlinger, Florian, Heppner, David E., To, Ciric, Günther, Marcel, Shin, Bo Hee, Rana, Jaimin K., Schmoker, Anna M., Beyett, Tyler S., Berger, Lena M., Berger, Benedict-Tilman, Bauer, Nicolas, Vasta, James D., Corona, Cesear R., Robers, Matthew B., Knapp, Stefan, Jänne, Pasi A., Eck, Michael J., Laufer, Stefan A.

“…Inhibitors targeting the epidermal growth factor receptor (EGFR) are an effective therapy for patients with non-small cell lung cancer harboring drug-sensitive…”
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Synthetic triterpenoids inhibit GSK3β activity and localization and affect focal adhesions and cell migration by To, Ciric, Roy, Ashbeel, Chan, Eddie, Prado, Marco A.M., Di Guglielmo, Gianni M.

“…Synthetic triterpenoids are a class of anti-cancer compounds that target many cellular functions, including apoptosis and cell growth in both cell culture and…”
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Synthetic Triterpenoids Target the Arp2/3 Complex and Inhibit Branched Actin Polymerization by To, Ciric, Shilton, Brian H., Di Guglielmo, Gianni M.

“…Synthetic triterpenoids are anti-tumor agents that affect numerous cellular functions including apoptosis and growth inhibition. Here, we used mass…”
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Abstract 466: Synthetic triterpenoids target cell migration and cell adhesion via GSK3β by To, Ciric, Di Guglielmo, Gianni M.

“…Abstract Synthetic triterpenoids are a class of anti-tumor compounds that target various cellular functions including apoptosis, growth inhibition,…”
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Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR -mutant lung cancer by Eser, Pınar Özden, Paranal, Raymond M, Son, Jieun, Ivanova, Elena, Kuang, Yanan, Haikala, Heidi M, To, Ciric, Okoro, Jeffrey J, Dholakia, Kshiti H, Choi, Jihyun, Eum, Yoonji, Ogino, Atsuko, Missios, Pavlos, Ercan, Dalia, Xu, Man, Poitras, Michael J, Wang, Stephen, Ngo, Kenneth, Dills, Michael, Yanagita, Masahiko, Lopez, Timothy, Lin, Mika, Tsai, Jeanelle, Floch, Nicolas, Chambers, Emily S, Heng, Jennifer, Anjum, Rana, Santucci, Alison D, Michael, Kesi, Schuller, Alwin G, Cross, Darren, Smith, Paul D, Oxnard, Geoffrey R, Barbie, David A, Sholl, Lynette M, Bahcall, Magda, Palakurthi, Sangeetha, Gokhale, Prafulla C, Paweletz, Cloud P, Daley, George Q, Jänne, Pasi A

“…The clinical efficacy of epidermal growth factor receptor (EGFR)–targeted therapy in -mutant non–small cell lung cancer is limited by the development of drug…”
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Abstract LB-265: Comparison of oleanane triterpenoids and dimethyl fumarate in lung cancer by To, Ciric, Royce, Darlene B., Williams, Charlotte R., Risingsong, Renee, Sporn, Michael B., Liby, Karen T.

“…Abstract Lung cancer accounts for the highest number of cancer-related deaths in the United States, highlighting the need for better therapies. Nrf2 is an…”
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