Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
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.
Published in Nature communications (09.05.2022)
Published in Nature communications (09.05.2022)
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Journal Article
Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations
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.
Published in Angewandte Chemie International Edition (17.08.2020)
Published in Angewandte Chemie International Edition (17.08.2020)
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Journal Article
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
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.
Published in Journal of thoracic oncology (01.11.2019)
Published in Journal of thoracic oncology (01.11.2019)
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Journal Article
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
To, Ciric, Ringelberg, Carol S, Royce, Darlene B, Williams, Charlotte R, Risingsong, Renee, Sporn, Michael B, Liby, Karen T
Published in Carcinogenesis (New York) (01.07.2015)
Published in Carcinogenesis (New York) (01.07.2015)
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Journal Article
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer
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
Published in Nature cancer (01.04.2022)
Published in Nature cancer (01.04.2022)
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The PARP Inhibitors, Veliparib and Olaparib, Are Effective Chemopreventive Agents for Delaying Mammary Tumor Development in BRCA1-deficient Mice
CIRIC TO, KIM, Eun-Hee, ROYCE, Darlene B, WILLIAMS, Charlotte R, COLLINS, Ryan M, RISINGSONG, Renee, SPORN, Michael B, LIBY, Karen T
Published in Cancer prevention research (Philadelphia, Pa.) (01.07.2014)
Published in Cancer prevention research (Philadelphia, Pa.) (01.07.2014)
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Journal Article
Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality
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.
Published in ACS central science (26.06.2024)
Published in ACS central science (26.06.2024)
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Journal Article
Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations
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.
Published in Angewandte Chemie (17.08.2020)
Published in Angewandte Chemie (17.08.2020)
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Journal Article
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor
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
Published in Cancer discovery (01.07.2019)
Published in Cancer discovery (01.07.2019)
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Journal Article
A Constitutive EGFR Kinase Dimer to Study Inhibitor Pharmacology
Kim, Justin J, Schaeffner, Ilse K, Heppner, David E, To, Ciric, Jänne, Pasi A, Beyett, Tyler S, Eck, Michael J
Published in Molecular pharmacology (01.02.2024)
Published in Molecular pharmacology (01.02.2024)
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Journal Article
Discovery of a potent dual ALK and EGFR T790M inhibitor
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.
Published in European journal of medicinal chemistry (18.08.2017)
Published in European journal of medicinal chemistry (18.08.2017)
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Journal Article
Design of a “Two-in-One” Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites
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
Published in Journal of medicinal chemistry (27.01.2022)
Published in Journal of medicinal chemistry (27.01.2022)
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Journal Article
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC
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.
Published in Bioorganic & medicinal chemistry letters (15.07.2022)
Published in Bioorganic & medicinal chemistry letters (15.07.2022)
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Journal Article
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors
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
Published in ACS medicinal chemistry letters (14.11.2019)
Published in ACS medicinal chemistry letters (14.11.2019)
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Journal Article
Design of a “two-in-one” mutant-selective EGFR inhibitor that spans the orthosteric and allosteric sites
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.
Published in Journal of medicinal chemistry (20.10.2021)
Published in Journal of medicinal chemistry (20.10.2021)
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Journal Article
Synthetic triterpenoids inhibit GSK3β activity and localization and affect focal adhesions and cell migration
To, Ciric, Roy, Ashbeel, Chan, Eddie, Prado, Marco A.M., Di Guglielmo, Gianni M.
Published in Biochimica et biophysica acta. Molecular cell research (01.07.2017)
Published in Biochimica et biophysica acta. Molecular cell research (01.07.2017)
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Journal Article
Synthetic Triterpenoids Target the Arp2/3 Complex and Inhibit Branched Actin Polymerization
To, Ciric, Shilton, Brian H., Di Guglielmo, Gianni M.
Published in The Journal of biological chemistry (03.09.2010)
Published in The Journal of biological chemistry (03.09.2010)
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Journal Article
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR -mutant lung cancer
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
Published in Science translational medicine (01.09.2021)
Published in Science translational medicine (01.09.2021)
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