Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Dharmaraj Samuel"'
Autor:
Magdeleine Hung, Anita Niedziela-Majka, Weimei Xing, Robert Jordan, Roman Sakowicz, Dharmaraj Samuel, Xiaohong Liu, David Sperandio, Jinny S. Wong, Katherine M. Brendza, Michel Perron, Richard L. Mackman
Publikováno v:
Antimicrobial Agents and Chemotherapy. 59:7109-7112
GS-5806 is a small-molecule inhibitor of human respiratory syncytial virus fusion protein-mediated viral entry. During viral entry, the fusion protein undergoes major conformational changes, resulting in fusion of the viral envelope with the host cel
Autor:
Anne Carey, Kirsten M. Stray, Brian E. Gilbert, Pedro A. Piedra, Dorothy Agnes Theodore, Kerim Babaoglu, Jay P. Parrish, Manoj C. Desai, Lijun Zhang, April Kinkade, Hai Yang, Dharmaraj Samuel, Oliver L. Saunders, Constantine G. Boojamra, Jaclyn Hayes, Robert Jordan, Sangi Michael, Eugene J. Eisenberg, David Sperandio, Dustin Siegel, Richard L. Mackman, Hui Hon Chung, Quynh Iwata, Tomas Cihlar, Michel Perron, Gary Lee, Robert G. Strickley
Publikováno v:
Journal of Medicinal Chemistry. 58:1630-1643
GS-5806 is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a screening hit. The oral absorption properties were optimized by converting to the pyrazolo[1,5-a]-pyrimidine heterocycle, while potenc
Autor:
Dharmaraj Samuel, John R. Somoza, Ruth Wang, Albert Liclican, Armando G. Villaseñor, Nikolai Novikov, Leanna Lagpacan, Giuseppe A. Papalia, Mary E. McGrath, Latesh Lad, David Koditek, Brian E. Schultz, Melanie H. Wong, Weimei Xing
Publikováno v:
The Journal of Biological Chemistry
Background: Idelalisib is a PI3Kδ inhibitor used to treat hematological malignancies. Results: Idelalisib is selective, noncovalent, reversible, and ATP-competitive. Conclusion: The crystal structure helps explain the potency and selectivity of idel
Autor:
Robert Jordan, Stefan Pflanz, Indrani Rebbapragada, Christian R. Frey, Hugo Tharinger, Dharmaraj Samuel, Nikolai Novikov, Mindie H. Nguyen
Publikováno v:
Journal of viral hepatitis. 24(6)
Maintaining detectable levels of antibodies to hepatitis B surface antigen (HBsAg) in serum after HBsAg sero-conversion is the key clinical endpoint indicative of recovery from infection with hepatitis B virus (HBV). As HBV-infected hepatocytes secre
Autor:
Roman Sakowicz, Anita Niedziela-Majka, Stephen R. Yant, Dharmaraj Samuel, Debi Jin, Manuel Tsiang, Xiaohong Liu, Magdeleine Hung, Eric Hu
Publikováno v:
Biochemistry. 51:4416-4428
Human immunodeficiency virus-1 (HIV-1) capsid protein (CA) has become a target of antiviral drug design in recent years. The recognition that binding of small molecules to the CA protein can result in the perturbation of capsid assembly or disassembl
Autor:
Debi Jin, Xiaohong Liu, Susmith Mukund, Dharmaraj Samuel, Anita Niedziela-Majka, Roman Sakowicz, Magdeleine Hung, Manuel Tsiang, Romas Geleziunas, Michael L. Mitchell, Gregg S. Jones, Katherine M. Brendza, Nikolai Novikov
Publikováno v:
Biochemistry. 50:1567-1581
We have developed a homogeneous time-resolved fluorescence resonance energy transfer (FRET)-based assay that detects the formation of HIV-1 integrase (IN) dimers. The assay utilizes IN monomers that express two different epitope tags that are recogni
Autor:
Eric B. Lansdon, Constantine G. Boojamra, Adrian S. Ray, Richard L. Mackman, Katherine M. Brendza, Magdeleine Hung, S. Swaminathan, Dharmaraj Samuel, Xiaohong Liu, Leanna Lagpacan, Tomas Cihlar, Mary E. McGrath, Kirsten L. White
Publikováno v:
Journal of Molecular Biology. 397:967-978
GS-9148 ([5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid) is a dAMP (2'-deoxyadenosine monophosphate) analog that maintains its antiviral activity against drug-resistant HIV. Crystal structures for HIV-1 reverse tran
Autor:
Daniel L. Minor, Paul Bessette, Thomas Mikita, Marco Lolicato, Kate L Lowe, Yun Cheol Kim, Jorge L. Garcia, Shaun R. Coughlin, Tovo David, Lauren Kate Ely, Dharmaraj Samuel
Publikováno v:
Structure (London, England : 1993), vol 26, iss 2
Ely, Lauren K; Lolicato, Marco; David, Tovo; Lowe, Kate; Kim, Yun Cheol; Samuel, Dharmaraj; et al.(2018). Structural Basis for Activity and Specificity of an Anticoagulant Anti-FXIa Monoclonal Antibody and a Reversal Agent. STRUCTURE, 26(2), 187-+. doi: 10.1016/j.str.2017.12.010. Lawrence Berkeley National Laboratory: Retrieved from: http://www.escholarship.org/uc/item/7mk8c84v
Ely, Lauren K; Lolicato, Marco; David, Tovo; Lowe, Kate; Kim, Yun Cheol; Samuel, Dharmaraj; et al.(2018). Structural Basis for Activity and Specificity of an Anticoagulant Anti-FXIa Monoclonal Antibody and a Reversal Agent. STRUCTURE, 26(2), 187-+. doi: 10.1016/j.str.2017.12.010. Lawrence Berkeley National Laboratory: Retrieved from: http://www.escholarship.org/uc/item/7mk8c84v
Coagulation factor XIa is a candidate target for anticoagulants that better separate antithrombotic efficacy from bleeding risk. We report a co-crystal structure of the FXIa protease domain with DEF, a human monoclonal antibody that blocks FXIa funct
Autor:
Dharmaraj Samuel, Chin Yu, Gurunathan Jayaraman, Ding-Kwo Chang, Mei-Ming Chang, Pey-Wen Yang, Gopal Ganesh, Kuo Chu Hwang, Vishwa Deo Trivedi, Sue-Lein Wang, Thallampuranam Krishnaswamy S. Kumar
Publikováno v:
Protein Science. 9:344-352
The in vitro refolding of hen egg-white lysozyme is studied in the presence of various osmolytes. Proline is found to prevent aggregation during protein refolding. However, other osmolytes used in this study fail to exhibit a similar property. Experi
Autor:
Dharmaraj Samuel, Ping-Chiang Lyu, Hsiao Nai-Wan, Gurunathan Jayaraman, Tzu-Ying Yang, Li-Chuan Chen, Yu-Nan Liu
Publikováno v:
Biochemistry. 42:11183-11193
A unique class of proteins, containing high-mobility group (HMG) domain(s), recognizes unusual DNA structures and/or bends specific to AT-rich linear double-stranded DNA. The DNA binding feature of these proteins is exhibited in the HMG domain(s). Al