Next‐generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells
Bame, Eris, Tang, Hao, Burns, Jeremy C, Arefayene, Million, Michelsen, Klaus, Ma, Bin, Marx, Isaac, Prince, Robin, Roach, Allie M, Poreci, Urjana, Donaldson, Douglas, Cullen, Patrick, Casey, Fergal, Zhu, Jing, Carlile, Thomas M, Sangurdekar, Dipen, Zhang, Baohong, Trapa, Patrick, Santoro, Joseph, Muragan, Param, Pellerin, Alex, Rubino, Stephen, Gianni, Davide, Bajrami, Bekim, Peng, Xiaomei, Coppell, Alex, Riester, Katherine, Belachew, Shibeshih, Mehta, Devangi, Palte, Mike, Hopkins, Brian T, Scaramozza, Matthew, Franchimont, Nathalie, Mingueneau, Michael
Published in Clinical & translational immunology (2021)
Published in Clinical & translational immunology (2021)
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BTK inhibition limits B-cell–T-cell interaction through modulation of B-cell metabolism: implications for multiple sclerosis therapy
Li, Rui, Tang, Hao, Burns, Jeremy C., Hopkins, Brian T., Le Coz, Carole, Zhang, Bo, de Barcelos, Isabella Peixoto, Romberg, Neil, Goldstein, Amy C., Banwell, Brenda L., Luning Prak, Eline T., Mingueneau, Michael, Bar-Or, Amit
Published in Acta neuropathologica (01.04.2022)
Published in Acta neuropathologica (01.04.2022)
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The Discovery of 7‑Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)‑N‑(6-methylpyrazolo[1,5‑a]pyrimidin-3-yl)imidazo[1,2‑a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke
Evans, Ryan, Bolduc, Philippe N., Pfaffenbach, Magnus, Gao, Fang, May-Dracka, Tricia, Fang, Terry, Hopkins, Brian T., Chodaparambil, Jayanth V, Henry, Kate L., Li, Pei, Metrick, Claire, Nelson, Ashley, Trapa, Patrick, Thomas, Ankur, Burkly, Linda, Peterson, Emily A.
Published in Journal of medicinal chemistry (28.03.2024)
Published in Journal of medicinal chemistry (28.03.2024)
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Journal Article
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors
Ma, Bin, Metrick, Claire M., Gu, Chungang, Hoemberger, Marc, Bajrami, Bekim, Bame, Eris, Huang, Jiansheng, Mingueneau, Michael, Murugan, Paramasivam, Santoro, Joseph C., Tang, Hao, Wang, Ti, Hopkins, Brian T.
Published in Bioorganic & medicinal chemistry letters (15.03.2022)
Published in Bioorganic & medicinal chemistry letters (15.03.2022)
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Journal Article
Discovery of BIIB068: A Selective, Potent, Reversible Bruton’s Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases
Ma, Bin, Bohnert, Tonika, Otipoby, Kevin L, Tien, Eric, Arefayene, Million, Bai, Judy, Bajrami, Bekim, Bame, Eris, Chan, Timothy R, Humora, Michael, MacPhee, J. Michael, Marcotte, Douglas, Mehta, Devangi, Metrick, Claire M, Moniz, George, Polack, Evelyne, Poreci, Urjana, Prefontaine, Annick, Sheikh, Sarah, Schroeder, Patricia, Smirnakis, Karen, Zhang, Lei, Zheng, Fengmei, Hopkins, Brian T
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Journal Article
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis
Hopkins, Brian T, Bame, Eris, Bajrami, Bekim, Black, Cheryl, Bohnert, Tonika, Boiselle, Carrie, Burdette, Doug, Burns, Jeremy C, Delva, Luisette, Donaldson, Douglas, Grater, Richard, Gu, Chungang, Hoemberger, Marc, Johnson, Josh, Kapadnis, Sudarshan, King, Kris, Lulla, Mukesh, Ma, Bin, Marx, Isaac, Magee, Tom, Meissner, Robert, Metrick, Claire M, Mingueneau, Michael, Murugan, Paramasivam, Otipoby, Kevin L, Polack, Evelyne, Poreci, Urjana, Prince, Robin, Roach, Allie M, Rowbottom, Chris, Santoro, Joseph C, Schroeder, Patricia, Tang, Hao, Tien, Eric, Zhang, Fengmei, Lyssikatos, Joseph
Published in Journal of medicinal chemistry (27.01.2022)
Published in Journal of medicinal chemistry (27.01.2022)
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Journal Article
Corrigendum to “Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors” [Bioorg. Med. Chem. Lett. 60 (2022) 128549]
Ma, Bin, Metrick, Claire M., Gu, Chungang, Hoemberger, Marc, Bajrami, Bekim, Bame, Eris, Huang, Jiansheng, Mingueneau, Michael, Murugan, Paramasivam, Nevalainen, Marta, Santoro, Joseph C., Tang, Hao, Wang, Ti, Hopkins, Brian T.
Published in Bioorganic & medicinal chemistry letters (15.09.2022)
Published in Bioorganic & medicinal chemistry letters (15.09.2022)
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Journal Article
Parallel Synthesis of Terminal Alkynes Using a ROMPgel-Supported Ethyl 1-Diazo-2-oxopropylphosphonate
Barrett, Anthony G. M, Hopkins, Brian T, Love, Andrew C, Tedeschi, Livio
Published in Organic letters (04.03.2004)
Published in Organic letters (04.03.2004)
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Journal Article
Sulfone Displacement Approach for Large-Scale Synthesis of 4‑Chloro‑N‑(1-methyl‑1H‑pyrazol-4-yl)pyrimidin-2-amine
Li, Chaomin, Haeffner, Fredrik, Wang, Shujun, Yuan, Cuicui, Shang, Deju, Shi, Xianglin, Ma, Bin, Hopkins, Brian T, O’Brien, Erin M
Published in Organic process research & development (21.01.2022)
Published in Organic process research & development (21.01.2022)
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Journal Article
Identification of individual protein-ligand NOEs in the limit of intermediate exchange
Reibarkh, Mikhail, Malia, Thomas J, Hopkins, Brian T, Wagner, Gerhard
Published in Journal of biomolecular NMR (01.09.2006)
Published in Journal of biomolecular NMR (01.09.2006)
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Journal Article
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis
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.
Published in Journal of medicinal chemistry (23.05.2024)
Published in Journal of medicinal chemistry (23.05.2024)
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Journal Article
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model
Vandeveer, George H., Arduini, Robert M., Baker, Darren P., Barry, Kevin, Bohnert, Tonika, Bowden-Verhoek, Jon K., Conlon, Patrick, Cullen, Patrick F., Guan, Bing, Jenkins, Tracy J., Liao, Shu-Yu, Lin, Lin, Liu, Yu-Ting, Marcotte, Douglas, Mertsching, Elisabeth, Metrick, Claire M., Negrou, Ella, Powell, Noel, Scott, Daniel, Silvian, Laura F., Hopkins, Brian T.
Published in Bioorganic & medicinal chemistry letters (15.01.2023)
Published in Bioorganic & medicinal chemistry letters (15.01.2023)
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Journal Article
Optimization of novel reversible Bruton’s tyrosine kinase inhibitors identified using Tethering-fragment-based screens
Hopkins, Brian T., Bame, Eris, Bell, Noah, Bohnert, Tonika, Bowden-Verhoek, Jon K., Bui, Minna, Cancilla, Mark T., Conlon, Patrick, Cullen, Patrick, Erlanson, Daniel A., Fan, Junfa, Fuchs-Knotts, Tarra, Hansen, Stig, Heumann, Stacey, Jenkins, Tracy J., Marcotte, Douglas, McDowell, Bob, Mertsching, Elisabeth, Negrou, Ella, Otipoby, Kevin L., Poreci, Urjana, Romanowski, Michael J., Scott, Daniel, Silvian, Laura, Yang, Wenjin, Zhong, Min
Published in Bioorganic & medicinal chemistry (01.07.2019)
Published in Bioorganic & medicinal chemistry (01.07.2019)
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Journal Article
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton’s tyrosine kinase inhibitors
Hopkins, Brian T., Bame, Eris, Bell, Noah, Bohnert, Tonika, Bowden-Verhoek, Jon K., Bui, Minna, Cancilla, Mark T., Conlon, Patrick, Cullen, Patrick, Erlanson, Daniel A., Fan, Junfa, Fuchs-Knotts, Tarra, Hansen, Stig, Heumann, Stacey, Jenkins, Tracy J., Gua, Chuck, Liu, Ying, Liu, YuTing, Lulla, Mukush, Marcotte, Douglas, Marx, Isaac, McDowell, Bob, Mertsching, Elisabeth, Negrou, Ella, Romanowski, Michael J., Scott, Daniel, Silvian, Laura, Yang, Wenjin, Zhong, Min
Published in Bioorganic & medicinal chemistry (15.08.2021)
Published in Bioorganic & medicinal chemistry (15.08.2021)
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Journal Article
Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases
Marcotte, Douglas J., Liu, Yu‐Ting, Arduini, Robert M., Hession, Catherine A., Miatkowski, Konrad, Wildes, Craig P., Cullen, Patrick F., Hong, Victor, Hopkins, Brian T., Mertsching, Elisabeth, Jenkins, Tracy J., Romanowski, Michael J., Baker, Darren P., Silvian, Laura F.
Published in Protein science (01.03.2010)
Published in Protein science (01.03.2010)
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Journal Article
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance
May-Dracka, Tricia L, Gao, Fang, Hopkins, Brian T, Hronowski, Xiaoping, Chen, TeYu, Chodaparambil, Jayanth V, Metrick, Claire M, Cullivan, Mike, Enyedy, Istvan, Kaliszczak, Maciej, Kankel, Mark W, Marx, Isaac, Michell-Robinson, Mackenzie A, Murugan, Param, Kumar, P. Rajesh, Rooney, Michael, Schuman, Eli, Sen, Anindya, Wang, Ti, Ye, Tao, Peterson, Emily A
Published in ACS medicinal chemistry letters (14.04.2022)
Published in ACS medicinal chemistry letters (14.04.2022)
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Journal Article
브루톤 티로신 키나제의 분해를 표적으로 하는 화합물
YAP JEREMY L, HOPKINS BRIAN T, GUCKIAN KEVIN M, STEFAN ERIC, ANDERSON COREY DON, O'SHEA MORGAN WELZEL, CHENG XINPENG, NEVALAINEN MARTA, AHN JAE YOUNG, MARX ISAAC
Year of Publication 08.02.2024
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Year of Publication 08.02.2024
Patent
BENZOAZEPINE ANALOGS AS INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE
PRINCE ROBIN, HOPKINS BRIAN T, PATIENCE DANIEL B, PETERSON MATTHEW, MA BIN, LYSSIKATOS JOSEPH P, ZHENG FENGMEI, MARX ISAAC
Year of Publication 01.12.2023
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Year of Publication 01.12.2023
Patent
ROMPgel-Supported Triphenylphosphine with Potential Application in Parallel Synthesis
Årstad, Erik, Barrett, Anthony G. M, Hopkins, Brian T, Köbberling, Johannes
Published in Organic letters (30.05.2002)
Published in Organic letters (30.05.2002)
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