ERK Inhibitor LY3214996 Targets ERK Pathway-Driven Cancers: A Therapeutic Approach Toward Precision Medicine
Bhagwat, Shripad V, McMillen, William T, Cai, Shufen, Zhao, Baohui, Whitesell, Matthew, Shen, Weihua, Kindler, Lisa, Flack, Robert S, Wu, Wenjuan, Anderson, Bryan, Zhai, Yan, Yuan, Xiu-Juan, Pogue, Meghann, Van Horn, Robert D, Rao, Xi, McCann, Denis, Dropsey, Andrew J, Manro, Jason, Walgren, Jennie, Yuen, Eunice, Rodriguez, Michael J, Plowman, Gregory D, Tiu, Ramon V, Joseph, Sajan, Peng, Sheng-Bin
Published in Molecular cancer therapeutics (01.02.2020)
Published in Molecular cancer therapeutics (01.02.2020)
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Journal Article
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor
Yingling, Jonathan M, McMillen, William T, Yan, Lei, Huang, Huocong, Sawyer, J Scott, Graff, Jeremy, Clawson, David K, Britt, Karen S, Anderson, Bryan D, Beight, Douglas W, Desaiah, Durisala, Lahn, Michael M, Benhadji, Karim A, Lallena, Maria J, Holmgaard, Rikke B, Xu, Xiaohong, Zhang, Faming, Manro, Jason R, Iversen, Philip W, Iyer, Chandrasekar V, Brekken, Rolf A, Kalos, Michael D, Driscoll, Kyla E
Published in Oncotarget (23.01.2018)
Published in Oncotarget (23.01.2018)
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Journal Article
Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain
Sawyer, J. Scott, Anderson, Bryan D, Beight, Douglas W, Campbell, Robert M, Jones, Michael L, Herron, David K, Lampe, John W, McCowan, Jefferson R, McMillen, William T, Mort, Nicholas, Parsons, Stephen, Smith, Edward C. R, Vieth, Michal, Weir, Leonard C, Yan, Lei, Zhang, Faming, Yingling, Jonathan M
Published in Journal of medicinal chemistry (11.09.2003)
Published in Journal of medicinal chemistry (11.09.2003)
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Journal Article
Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent
Li, Hong-yu, McMillen, William T, Heap, Charles R, McCann, Denis J, Yan, Lei, Campbell, Robert M, Mundla, Sreenivasa R, King, Chi-Hsin R, Dierks, Elizabeth A, Anderson, Bryan D, Britt, Karen S, Huss, Karen L, Voss, Matthew D, Wang, Yan, Clawson, David K, Yingling, Jonathan M, Sawyer, J. Scott
Published in Journal of medicinal chemistry (10.04.2008)
Published in Journal of medicinal chemistry (10.04.2008)
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Journal Article
Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain
SAWYER, J. Scott, BEIGHT, Douglas W, PARSONS, Stephen, SMITH, Edward C. R, WAGNER, Jill R, LEI YAN, FAMING ZHANG, YINGLING, Jonathan M, BRITT, Karen S, ANDERSON, Bryan D, CAMPBELL, Robert M, GOODSON, Theodore JR, HERRON, David K, LI, Hong-Yu, MCMILLEN, William T, MORT, Nicholas
Published in Bioorganic & medicinal chemistry letters (05.07.2004)
Published in Bioorganic & medicinal chemistry letters (05.07.2004)
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Journal Article
Kinetic Characterization of Novel Pyrazole TGF-β Receptor I Kinase Inhibitors and Their Blockade of the Epithelial−Mesenchymal Transition
Peng, Sheng-Bin, Yan, Lei, Xia, Xiaoling, Watkins, Scott A, Brooks, Harold B, Beight, Douglas, Herron, David K, Jones, Michael L, Lampe, John W, McMillen, William T, Mort, Nicholas, Sawyer, J. Scott, Yingling, Jonathan M
Published in Biochemistry (Easton) (22.02.2005)
Published in Biochemistry (Easton) (22.02.2005)
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Journal Article
Dihydropyrrolopyrazole Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: A Novel Benzimidazole Series with Selectivity versus Transforming Growth Factor-β Type II Receptor Kinase and Mixed Lineage Kinase-7
Li, Hong-yu, Wang, Yan, Heap, Charles R, King, Chi-Hsin R, Mundla, Sreenivasa R, Voss, Matthew, Clawson, David K, Yan, Lei, Campbell, Robert M, Anderson, Bryan D, Wagner, Jill R, Britt, Karen, Lu, Ku X, McMillen, William T, Yingling, Jonathan M
Published in Journal of medicinal chemistry (23.03.2006)
Published in Journal of medicinal chemistry (23.03.2006)
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Journal Article
ERK [23-c]-4- THIENO[23-C]PYRROL-4-ONE DERIVATIVES AS ERK INHIBITORS
JOSEPH SAJAN, MCMILLEN WILLIAM T, ZHAO GAIYING, CORTEZ GUILLERMO S, MCLEAN JOHNATHAN ALEXANDER, RODRIGUEZ MICHAEL JOHN
Year of Publication 17.07.2017
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Year of Publication 17.07.2017
Patent
AMINOPYRIDYLOXYPYRAZOLE COMPOUNDS
JOSEPH SAJAN, WOLFANGEL CRAIG D, MCMILLEN WILLIAM T, BEIGHT DOUGLAS W, ZHAO GAIYING, COATES DAVID A, PEI HUAXING, PARTHASARATHY SARAVANAN, SAWYER JASON SCOTT
Year of Publication 26.04.2017
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Year of Publication 26.04.2017
Patent
Abstract 5225: Temporal inhibition of ERK is sufficient for tumor growth inhibition in KRAS -mutant or BRAF -mutant tumors
Bhagwat, Shripad V., Shen, Weihua, Zhao, Baohui, Cai, Shufen, Kindler, Lisa, McMillen, William T., Yuen, Eunice, McCann, Denis, Manro, Jason, Dropsey, Andrew J., Willard, Melinda D., Joseph, Sajan, Peng, Sheng-Bin
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Journal Article
A phase I dose escalation (DE) study of ERK inhibitor, LY3214996, in advanced (adv) cancer (CA) patients (pts)
Pant, Shubham, Bendell, Johanna C., Sullivan, Ryan J., Shapiro, Geoffrey, Millward, Michael, Mi, Gu, Yuen, Eunice, Willard, Melinda D., Wang, Dan, Joseph, Sajan, McMillen, William T., Bhagwat, Shripad V., Tiu, Ramon Velasquez, Patel, Manish R.
Published in Journal of clinical oncology (20.05.2019)
Published in Journal of clinical oncology (20.05.2019)
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Journal Article
Abstract LB-185: Combination of an ERK1/2 inhibitor (LY3214996) with VEGFR-2 inhibitor enhances anti-tumor activity in KRAS mutant non-small cell lung cancer
Wu, Wenjuan, Bhagwat, Shripad V., Jones, Bonita D., Swearingen, Michelle L., Falcon, Beverly L., McMillen, William T., Joseph, Sajan, Buchanan, Sean, Peng, Sheng-Bin, Reinhard, Christoph, Tiu, Ramon V.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Abstract 317: Combination of a novel ERK1/2 inhibitor (LY3214996) with CDK4 and CDK6 inhibitor (abemaciclib) enhances antitumor efficacy in KRAS mutant non-small cell lung cancer (NSCLC)
Wu, Wenjuan, Bhagwat, Shripad V., King, Constance, Pratt, Susan, Gong, Xueqian, Stewart, Julie, Jones, Bonita, Flack, Robert, Beckman, Richard, Falcon, Beverly, Manro, Jason, McMillen, William T., Tiu, Ramon V., Peng, Sheng-Bin, Reinhard, Christoph, Joseph, Sajan, Buchanan, Sean
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract 5245: Identification and characterization of the IDO1 inhibitor LY3381916
Dorsey, Frank C., Benhadji, Karim A., Sams, Lillian L., Young, Debra A., Schindler, John F., Huss, Karen L., Nikolayev, Alexander, Carpenito, Carmine, Clawson, David, Jones, Bonita, Faber, Andrew L., Thomas, James E., Haney, Steven A., Zhao, Gaiying, McMillen, William T., Smeal, Tod, Sall, Daniel J., Kalos, Michael D., Geeganage, Sandaruwan, Henry, James R.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations
Bhagwat, Shripad V., McMillen, William T., Cai, Shufen, Zhao, Baohui, Whitesell, Matthew, Kindler, Lisa, Flack, Robert S., Wu, Wenjuan, Huss, Karen, Anderson, Bryan, Yuan, Xiu-Juan, Jaken, Susan, McCann, Denis, Mathes, Brian, Dropsey, Andrew J., Manro, Jason, Walgren, Jennie, Yuen, Eunice, Gong, Xueqian, Rodriguez, Michael J., Huang, Jianping, Tiu, Ramon V., Joseph, Sajan, Peng, Sheng-Bin
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract 3231: Identifying high quality, potent and selective pyrimidinylthienopyrrolone inhibitors of ERK1/2 kinase: LY3214996
Zhao, Gaiying, McMillen, William T., Cai, Shufen, Zhao, Baohui, Whitesell, Matthew, Wu, Wenjuan, Huss, Karen, Anderson, Bryan, Yuan, Xiu-Juan, Jaken, Susan, Kindler, Lisa, Flack, Robert S., McCann, Denis, Mathes, Brian, Dropsey, Andrew J., Walgren, Jennie, Yuen, Eunice, Manro, Jason, Gong, Xueqian, Cortez, Guillermo, McLean, Johnathan, Rodriguez, Michael J., Tiu, Ramon V., Bhagwat, Shripad V., Joseph, Sajan
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
A concise synthesis of quinazolinone TGF-β RI inhibitor through one-pot three-component Suzuki–Miyaura/etherification and imidate–amide rearrangement reactions
Li, Hong-yu, Wang, Yan, McMillen, William T., Chatterjee, Arindam, Toth, John E., Mundla, Sreenivasa R., Voss, Matthew, Boyer, Robert D., Sawyer, J. Scott
Published in Tetrahedron (19.11.2007)
Published in Tetrahedron (19.11.2007)
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Journal Article
ERK inhibitors
Zhao, Gaiying, Joseph, Sajan, Rodriguez, Michael John, McMillen, William T, Cortez, Guillermo S, McLean, Johnathan Alexander
Year of Publication 13.07.2021
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Year of Publication 13.07.2021
Patent
THIENO[2,3-C]PYRROL-4-ONE DERIVATIVES AS ERK INHIBITORS
SAJAN JOSEPH, WILLIAM T. MCMILLEN, MICHAEL JOHN RODRIGUEZ, GAIYING ZHAO, JOHNATHAN ALEXANDER MCLEAN, GUILLERMO S. CORTEZ
Year of Publication 13.10.2020
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Year of Publication 13.10.2020
Patent
AMINOPYRIDYLOXYPYRAZOLE COMPOUNDS
SAJAN JOSEPH, HUAXING PEI, CRAIG D. WOLFANGEL, DOUGLAS W. BEIGHT, DAVID A. COATES, WILLIAM T. MCMILLEN, GAIYING ZHAO, JASON SCOTT SAWYER, SARAVANAN PARTHASARATHY
Year of Publication 27.04.2022
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Year of Publication 27.04.2022
Patent