Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.

Authors: Himmelbauer, Martin K., Bajrami, Bekim, Basile, Rebecca, Capacci, Andrew, Chen, TeYu, Choi, Colin K., Gilfillan, Rab, Gonzalez-Lopez de Turiso, Felix, Gu, Chungang, Hoemberger, Marc, Johnson, Douglas S., Jones, J. Howard, Kadakia, Ekta, Kirkland, Melissa, Lin, Edward Y., Liu, Ying, Ma, Bin, Magee, Tom, Mantena, Srinivasa, Marx, Isaac E.

Source: Journal of Medicinal Chemistry; 5/23/2024, Vol. 67 Issue 10, p8122-8140, 19p

Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis

Authors: Himmelbauer, Martin K., Bajrami, Bekim, Basile, Rebecca, Capacci, Andrew, Chen, TeYu, Choi, Colin K., Gilfillan, Rab, Gonzalez-Lopez de Turiso, Felix, Gu, Chungang, Hoemberger, Marc, Johnson, Douglas S., Jones, J. Howard, Kadakia, Ekta, Kirkland, Melissa, Lin, Edward Y., Liu, Ying, Ma, Bin, Magee, Tom, Mantena, Srinivasa, Marx, Isaac E., Metrick, Claire M., Mingueneau, Michael, Murugan, Paramasivam, Muste, Cathy A., Nadella, Prasad, Nevalainen, Marta, Parker Harp, Chelsea R., Pattaropong, Vatee, Pietrasiewicz, Alicia, Prince, Robin J., Purgett, Thomas J., Santoro, Joseph C., Schulz, Jurgen, Sciabola, Simone, Tang, Hao, Vandeveer, H. George, Wang, Ti, Yousaf, Zain, Helal, Christopher J., Hopkins, Brian T.

Source: Journal of Medicinal Chemistry; May 2024, Vol. 67 Issue: 10 p8122-8140, 19p

Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo.

Authors: Jones, J. Howard, Zhili Xin, Himmelbauer, Martin, Dechantsreiter, Michael, Enyedy, Istvan, Hedde, Joseph, Fang, Terry, Coomaraswamy, Janaky, King, Kristopher W., Murugan, Paramasivam, Santoro, Joseph C., Hesson, Thomas, Walther, Dirk M., Ru Wei, Fengmei Zheng, Marcotte, Douglas J., Spilker, Kerri, Kumar, P. Rajesh, Ying Liu, Gilfillan, Rab

Source: Journal of Medicinal Chemistry; 10/28/2021, Vol. 64 Issue 20, p15402-15419, 18p

Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo

Authors: Jones, J. Howard, Xin, Zhili, Himmelbauer, Martin, Dechantsreiter, Michael, Enyedy, Istvan, Hedde, Joseph, Fang, Terry, Coomaraswamy, Janaky, King, Kristopher W., Murugan, Paramasivam, Santoro, Joseph C., Hesson, Thomas, Walther, Dirk M., Wei, Ru, Zheng, Fengmei, Marcotte, Douglas J., Spilker, Kerri, Kumar, P. Rajesh, Liu, Ying, Gilfillan, Rab, Gonzalez-Lopez de Turiso, Felix

Source: Journal of Medicinal Chemistry; October 2021, Vol. 64 Issue: 20 p15402-15419, 18p

Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors.

Authors: Himmelbauer, Martin K., Xin, Zhili, Jones, J. Howard, Enyedy, Istvan, King, Kristopher, Marcotte, Douglas J., Murugan, Paramasivam, Santoro, Joseph C., Hesson, Thomas, Spilker, Kerri, Johnson, Joshua L., Luzzio, Michael J., Gilfillan, Rab, de Turiso, Felix Gonzalez-Lopez

Source: Journal of Medicinal Chemistry; 12/12/2019, Vol. 62 Issue 23, p10740-10756, 17p

Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors

Authors: Himmelbauer, Martin K., Xin, Zhili, Jones, J. Howard, Enyedy, Istvan, King, Kristopher, Marcotte, Douglas J., Murugan, Paramasivam, Santoro, Joseph C., Hesson, Thomas, Spilker, Kerri, Johnson, Joshua L., Luzzio, Michael J., Gilfillan, Rab, de Turiso, Felix Gonzalez-Lopez

Source: Journal of Medicinal Chemistry; December 2019, Vol. 62 Issue: 23 p10740-10756, 17p

Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo

Authors: Halkina, Tamara, Henderson, Jaclyn L., Lin, Edward Y., Himmelbauer, Martin K., Jones, J. Howard, Nevalainen, Marta, Feng, Jun, King, Kristopher, Rooney, Michael, Johnson, Joshua L., Marcotte, Douglas J., Chodaparambil, Jayanth V., Kumar, P. Rajesh, Patterson, Thomas A., Murugan, Paramasivam, Schuman, Eli, Wong, LaiYee, Hesson, Thomas, Lamore, Sarah, Bao, Channa, Calhoun, Michael, Certo, Hannah, Amaral, Brenda, Dillon, Gregory M., Gilfillan, Rab, de Turiso, Felix Gonzalez-Lopez

Source: Journal of Medicinal Chemistry; 20210101, Issue: Preprints