Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Tatyana Zvyaga"'
Autor:
Jeremy H. Toyn, Lorin A. Thompson, Kimberley A. Lentz, Jere E. Meredith, Catherine R. Burton, Sethu Sankaranararyanan, Valerie Guss, Tracey Hall, Lawrence G. Iben, Carol M. Krause, Rudy Krause, Xu-Alan Lin, Maria Pierdomenico, Craig Polson, Alan S. Robertson, R. Rex Denton, James E. Grace, John Morrison, Joseph Raybon, Xiaoliang Zhuo, Kimberly Snow, Ramesh Padmanabha, Michele Agler, Kim Esposito, David Harden, Margaret Prack, Sam Varma, Victoria Wong, Yingjie Zhu, Tatyana Zvyaga, Samuel Gerritz, Lawrence R. Marcin, Mendi A. Higgins, Jianliang Shi, Cong Wei, Joseph L. Cantone, Dieter M. Drexler, John E. Macor, Richard E. Olson, Michael K. Ahlijanian, Charles F. Albright
Publikováno v:
International Journal of Alzheimer's Disease, Vol 2014 (2014)
Alzheimer’s disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid Aβ1-42, in the brain. Aβ1-42 levels can be decreased by γ-secretase modulators (GSM), whi
Externí odkaz:
https://doaj.org/article/1dce320132d4411583a19dcbfe2b54ae
Autor:
Matthew D. Hill, Haiquan Fang, Derek Norris, George V. Delucca, Hong Huang, Mikkel DeBenedetto, Claude Quesnelle, William D. Schmitz, John S. Tokarski, Steven Sheriff, Chunhong Yan, Caroline Fanslau, Zuzana Haarhoff, Christine Huang, Melissa Kramer, Shilpa Madari, Krista Menard, Laura Monereau, John Morrison, Nirmala Raghavan, Eric E. Shields, Jean Simmermacher-Mayer, Michael Sinz, Ching Kim Tye, Richard Westhouse, Chunshan Xie, Haiying Zhang, Lisa Zhang, Tatyana Zvyaga, Francis Lee, Ashvinikumar V. Gavai, Andrew P. Degnan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1165-1171
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies
Autor:
Emily Luk, Karen E. Parrish, Yue-Zhong Shu, Anwar Murtaza, Yongnian Sun, Jinwen Huang, Robert M. Borzilleri, Paul Stetsko, Mary Ellen Cvijic, Jonathan G. Pabalan, Lihong Cheng, Zheng Yang, Jesse Swanson, James R. Burke, Tatyana Zvyaga, James Smalley, Karen A. Augustine
Publikováno v:
Biopharmaceutics & Drug Disposition. 42:137-149
Transforming growth factor beta (TGF-β) is a pleiotropic cytokine that has a wide array of biological effects. For decades, tumor biology implicated TGF-β as an attractive therapeutic target due to its immunosuppressive effects. Toward this end, mu
Autor:
Nicholas A. Meanwell, Ravi Kumar Trivedi, Tatyana Zvyaga, Richard Rampulla, Sarkunam Kandhasamy, Debarati Mazumder Tagore, Sureshbabu Vishwakrishnan, Arvind Mathur, Sunitha Puttaswamy, Abhijith Rao, Hua Fang, Sankar Sivaprasad, Susan Jenkins, Eric Mull, Kathy Mosure, Kaushik Ghosh, Barbara Zheng, Subba Reddy, Fiona McPhee, Chaoqun Chen, Bowsher Michael S, James Loy, Ying-Kai Wang, Amit Kumar, Ramkumar Rajamani, Kishore Rendunchintala, Paul Michael Scola, Gillis Eric P, Salil D. Desai, Li-Qiang Sun, Rushith Kumar Anumula, Nagalakshmi Pulicharla, Sheldon Hiebert, Venkata Rao Baratam, Paul Falk, Sarmistha Sinha, Stanley D'andrea
Publikováno v:
Journal of Medicinal Chemistry. 63:14740-14760
The discovery of a pan-genotypic hepatitis C virus (HCV) NS3/4A protease inhibitor based on a P1–P3 macrocyclic tripeptide motif is described. The all-carbon tether linking the P1–P3 subsites of 21...
Autor:
Andrew P. Degnan, Haiquan Fang, Tatyana Zvyaga, Zuzana Haarhoff, Claude A. Quesnelle, Melissa Kramer, Frank Marsilio, Richard A. Westhouse, John S. Tokarski, Shilpa Madari, Jiuqiao Zhao, Amy Wiebesiek, Chunhong Yan, Francis Y. Lee, Michael Sinz, John Morrison, Jean Simmermacher-Mayer, Carolynn Fanslau, Steven Sheriff, Lisa Huang, Ashvinikumar V. Gavai, Chunshan Xie, Matthew D. Hill, Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 51
We describe our efforts to introduce structural diversity to a previously described triazole-containing N1-carboline series of bromodomain and extra-terminal (BET) inhibitors. N9 carbolines were designed to retain favorable binding interactions that
Autor:
John E. Macor, Yunhui Zhang, James E. Grace, Lorin A. Thompson, Jeremy H. Toyn, Lawrence R. Marcin, Subramaniam Krishnananthan, Jianliang Shi, Dmitry Zuev, Daniel Smith, Jianqing Li, Yong-Jin Wu, Jason M. Guernon, Xiaoliang Zhuo, Tatyana Zvyaga, Xu Li, Arvind Mathur, John Morrison, Jere E. Meredith, Charles F. Albright, S. Roy Kimura, Mendi A. Higgins, Kimberley A. Lentz, Richard E. Olson, Rex Denton, Kenneth M. Boy, Catherine R. Burton, Ashok K. Trehan, Michael K. Ahlijanian
Publikováno v:
ACS Medicinal Chemistry Letters
A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the bicyclic pyrimidine γ-secretase modulator BMS-932481. The compound showed robust reductions of
Autor:
Chunhong Yan, Francis Y. Lee, Ashvinikumar V. Gavai, Melissa Kramer, Frank Marsilio, Eric Shields, Laura Monereau, Zuzana Haarhoff, Richard A. Westhouse, Lisa Zhang, Gerry Everlof, John S. Tokarski, Matthew D. Hill, Tatyana Zvyaga, Asoka Ranasinghe, Carolynn Fanslau, Ching Kim Tye, Steven Sheriff, Christine Huang, Andrew P. Degnan, Krista Menard, John Morrison, Haiquan Fang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 44:128108
We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 “cap” phenyl moiety with various heteroaryls, coupled with additiona
Autor:
Dawn D. Parker, Karen Rigat, Kyle J. Eastman, Umesh Hanumegowda, Katharine A. Grant-Young, Nicholas A. Meanwell, Maria Tuttle, Tao Wang, Tatyana Zvyaga, Susan B. Roberts, Hua Fang, Kap-Sun Yeung, Mengping Liu, Julie A. Lemm, Kathy Mosure, Xiaoliang Zhuo, Maria Donoso, Kyle Parcella, Zhongxing Zhang, Matthew G. Soars, Zuzana Haarhoff, Zhiwei Yin, Ying-Kai Wang, John F. Kadow, Juliang Zhu
Publikováno v:
ACS Medicinal Chemistry Letters. 8:771-774
Iterative structure–activity analyses in a class of highly functionalized furo[2,3-b]pyridines led to the identification of the second generation pan-genotypic hepatitis C virus NS5B polymerase primer grip inhibitor BMT-052 (14), a potential clinic
Autor:
Dieter M. Drexler, Andrew Dennis Wagner, Zuzana Haarhoff, Pierre Picard, Tatyana Zvyaga, Wilson Z. Shou
Publikováno v:
SLAS Discovery. 21:165-175
The move toward label-free screening in drug discovery has increased the demand for mass spectrometry (MS)-based analysis. Here we investigated the approach of coupling acoustic sample deposition (ASD) with laser diode thermal desorption (LDTD)-tande
Autor:
Cheryl Klakouski, Wilson Z. Shou, Yue-Zhong Shu, Ismael Zamora, Benjamin M. Johnson, Anthony A. Paiva, Tatyana Zvyaga, Shu Li, Jonathan L. Josephs
Publikováno v:
Bioanalysis. 9(7)
Aim: High clearance is a commonly encountered issue in drug discovery. Here we present a centralized metabolic soft spot identification assay with adequate capacity and turnaround time to support the metabolic optimization needs of an entire discover