Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Karin Reif"'
Autor:
Joseph W. Lubach, Jennifer Vogt, Wendy B. Young, Charles Eigenbrot, Arna Katewa, James J. Crawford, Dinah Misner, Harvey Wong, Hans E. Purkey, Wendy Lee, Adam R. Johnson, Karin Reif, Jacob Z. Chen, Satoko Kakiuchi-Kiyota, Lichuan Liu, Julia Heidmann, Christine Yu, James R. Kiefer, Kelly J. Delatorre
Publikováno v:
ACS Med Chem Lett
[Image: see text] Bruton’s tyrosine kinase (Btk) is thought to play a pathogenic role in chronic immune diseases such as rheumatoid arthritis and lupus. While covalent, irreversible Btk inhibitors are approved for treatment of hematologic malignanc
Autor:
Steve Gallion, Jacob Z. Chen, Kropf Jeffrey E, Joseph W. Lubach, Pat Maciejewski, Heleen Scheerens, Seung H. Lee, Aaron C. Schmitt, Daniel F. Ortwine, Arna Katewa, Jin-Ming Xiong, Huiyong Hu, James J. Crawford, Wei Deng, Karin Reif, Zhongdong Zhao, Julie DiPaolo, Liming Dong, Kevin S. Currie, Fusheng Zhou, Peter Blomgren, Jonathon Hau, Charles Eigenbrot, Meire Bremer, Jen Macaluso, Adam R. Johnson, Scott A. Mitchell, Jianjun Xu, Lichuan Liu, James Barbosa, Wendy B. Young, Harvey Wong, Xiaojing Wang
Publikováno v:
ACS Medicinal Chemistry Letters
In our continued effort to discover and develop best-in-class Bruton’s tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds
Autor:
Tao Huang, Yichin Liu, Karin Reif, Amy Hilderbrand, Eric Stefanich, John C. Tran, Nisana Andersen, Isidro Hötzel, Jianyong Wang, Daniel Tran
Publikováno v:
Analytical Chemistry. 88:11521-11526
Deamidation of therapeutic antibodies may result in decreased drug activity and undesirable changes in pharmacokinetics and immunogenicity. Therefore, it is necessary to monitor the deamidation levels [during storage] and after in vivo administration
Autor:
James J. Crawford, Joseph W. Lubach, Peter Blomgren, Pat Maciejewski, Steve Gallion, Jen Macaluso, Julie Di Paolo, Donna Dambach, Adam R. Johnson, Christine Yu, Xiaojing Wang, James Barbosa, Jin-Ming Xiong, Karin Reif, Zhongdong Zhao, Harvey Wong, Aaron C. Schmitt, Kevin S. Currie, Wendy B. Young, Kropf Jeffrey E, Scott A. Mitchell, Heleen Scheerens, Seung H. Lee, Charles Eigenbrot, Meire Bremer, Daniel F. Ortwine, Jianjun Xu, Lichuan Liu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:575-579
BTK inhibitor GDC-0834 (1) was found to be rapidly metabolized in human studies, resulting in a suspension of clinical trials. The primary route of metabolism was through cleavage of the acyclic amide bond connecting the terminal tetrahydrobenzothiop
Autor:
Daniel F. Ortwine, Rebecca Erickson, Jonathan Hau, Binqing Wei, Charles Eigenbrot, Arna Katewa, James J. Crawford, Regina Choy, Dinah Misner, Georgette Castanedo, Pawan Bir Kohli, Suzanne Tay, Liming Dong, Lisa D. Belmont, Joseph W. Lubach, Wendy B. Young, Adam R. Johnson, Lichuan Liu, Harvey Wong, Leah Schutt, Karin Reif, Brent S. McKenzie, Melis Coraggio, Nico Ghilardi, Wendy Lee
Publikováno v:
Journal of medicinal chemistry. 61(6)
Bruton's tyrosine kinase (Btk) is a nonreceptor cytoplasmic tyrosine kinase involved in B-cell and myeloid cell activation, downstream of B-cell and Fcγ receptors, respectively. Preclinical studies have indicated that inhibition of Btk activity migh
Autor:
Aaron C. Schmitt, Donna Dambach, Jen Macaluso, Kevin S. Currie, Xiaojing Wang, James Barbosa, Sarah G. Hymowitz, Kropf Jeffrey E, Steve Gallion, Peter Blomgren, Lichuan Liu, Scott A. Mitchell, Julie Di Paolo, Jin-Ming Xiong, Joseph W. Lubach, Pat Maciejewski, C. Gregory Sowell, Heleen Scheerens, Seung H. Lee, Karin Reif, Zhongdong Zhao, Wendy B. Young, Jianjun Xu, Harvey Wong, Brigitte Maurer, Daniel F. Ortwine, James J. Crawford, Meire Bremer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25(6):1333-1337
SAR studies focused on improving the pharmacokinetic (PK) properties of the previously reported potent and selective Btk inhibitor CGI-1746 (1) resulted in the clinical candidate GDC-0834 (2), which retained the potency and selectivity of CGI-1746, b
Autor:
Laura DeForge, Eric Suto, Justin Lesch, Joseph W. Lubach, Arna Katewa, Zora Modrusan, Tao Huang, Allen Nguyen, Harvey Wong, Lichuan Liu, Jianyong Wang, Jason A. Hackney, James J. Crawford, Adam R. Johnson, Chungkee Poon, Sami McVay, Jacob Z. Chen, Zhonghua Lin, Yugang Wang, Marya Liimatta, Jason DeVoss, Peter Blomgren, Kevin S. Currie, Karin Reif, Wendy B. Young, Cary D. Austin, Michael J. Townsend, Nandhini Ramamoorthi, Jonathan Hau, Julie DiPaolo, Meire Bremer, Wyne P. Lee
Publikováno v:
JCI Insight. 2
Systemic lupus erythematosus (SLE) is often associated with exaggerated B cell activation promoting plasma cell generation, immune-complex deposition in the kidney, renal infiltration of myeloid cells, and glomerular nephritis. Type-I IFNs amplify th
Autor:
Bryan K. Chan, Cristina Lewis, Steve Price, Brian Safina, Robert Heald, Zachary Kevin Sweeney, Jodie Pang, Karin Reif, Georgette Castanedo, Jun Li, Daniel P. Sutherlin, Michael Flagella, Eileen Mary Seward, Jeremy Murray, Jim Nonomiya, Laurent Salphati, Angelina Bisconte, Binqing Wei, Diane E. Carrera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23(17):4953-4959
In an effort to identify potent and isoform selective inhibitors of PI3Kδ, GNE-293 (34) was identified. Inhibitor 2 was found to induce micronuclei formation in both the MNT and HCA in vitro assays. Compounds testing negative for genotoxicity were s
Autor:
Wendy B. Young, Karin Reif, Jed Ross, Jacqueline M. Tarrant, Donna M. Dambach, Karin Staflin, Adam R. Johnson, Arna Katewa, Rebecca Erickson, Maj Hedehus, Shelly Zhong, Sock-Cheng Lewin-Koh, Fiona Zhong, Lichuan Liu, Michelle McDowell, James J. Crawford, Dinah L. Misner, Richard A. D. Carano, Harvey Wong, Leah Schutt
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 360(1)
Bruton's tyrosine kinase (BTK) is a member of the Tec family of cytoplasmic tyrosine kinases involved in B-cell and myeloid cell signaling. Small molecule inhibitors of BTK are being investigated for treatment of several hematologic cancers and autoi
Autor:
Xiumin Wu, Hai Ngu, Min Xu, David F. Choy, Karin Reif, Arna Katewa, Elizabeth Luis, Jianyong Wang, Cary D. Austin, Meijuan Zhou, Wyne P. Lee, Tao Huang, Nandhini Ramamoorthi, Yongchang Shi, Meredith Hazen, Mercedesz Balazs, Erick R. Castellanos, Donghong Yan, Zhonghua Lin, Marissa L. Matsumoto, Yonglei Shang, Jo-Anne Hongo, Jian Payandeh, Joseph R. Arron, Isidro Hötzel, Margaret Solon
Publikováno v:
JCI Insight. 1
Eosinophilic inflammation and Th2 cytokine production are central to the pathogenesis of asthma. Agents that target either eosinophils or single Th2 cytokines have shown benefits in subsets of biomarker-positive patients. More broadly effective treat