Zobrazeno 1 - 10
of 101
pro vyhledávání: '"Steven Sheriff"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e35ad654e0ca7192653d0e07258cff5
https://doi.org/10.1021/acsmedchemlett.2c00219
https://doi.org/10.1021/acsmedchemlett.2c00219
Autor:
Ching Kim Tye, Chunhong Yan, Sarah C. Traeger, Wayne Vaccaro, Yingru Zhang, Gerry Everlof, Jianqing Li, Henry Yip, Peng Li, John T. Hunt, Michael A. Poss, Gregory D. Vite, Mussari Christopher P, Steven Sheriff, Asoka Ranasinghe, Haiying Zhang, Richard A. Westhouse, Dharmpal S. Dodd, Richard Rampulla, Zheng Yang, Frank Marsilio, Derek J. Norris, Wen-Ching Han, Tram N. Huynh, Yufen Zhao, Patrice Gill, Nirmala Raghavan, Lalgudi S. Harikrishnan, Ashvinikumar V. Gavai, Susan Wee, John S. Tokarski, Dauh-Rurng Wu, Arvind Mathur, Mei-Li Wen, Huiping Zhang, David R. Tortolani, George V. Delucca, Krista Menard, Francis Y. Lee, Claude A. Quesnelle, Dawn Sun, Vijay T. Ahuja, Daniel O'malley, Christine Huang, Muthoni G. Kamau
Publikováno v:
Journal of Medicinal Chemistry. 64:14247-14265
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit 1, a combination of structure-activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6552024d7da4fe4ccaa968fbe1cf079
https://doi.org/10.1021/acs.jmedchem.1c00625
https://doi.org/10.1021/acs.jmedchem.1c00625
Autor:
John Morrison, Steven Sheriff, Mark D. Wittman, Gregory A. Locke, Bradley C. Pearce, Erika M. V. Araujo, Andrew P. Degnan, Christopher W. Allard, Dan You, Xin Li, Kurt Zimmermann, Anwar Murtaza, Benjamin M. Johnson, Caitlyn Stromko, Jinqi Liu, Gregory D. Vite, Godwin Kwame Kumi, Karen E. Parrish, Alan Futran, Johnson Walter Lewis
Publikováno v:
ACS Medicinal Chemistry Letters
While the discovery of immune checkpoint inhibitors has led to robust, durable responses in a range of cancers, many patients do not respond to currently available therapeutics. Therefore, an urgent need exists to identify alternative mechanisms to a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe8d6f32c2573a82ac07636c7d82958e
https://doi.org/10.1021/acsmedchemlett.0c00660
https://doi.org/10.1021/acsmedchemlett.0c00660
Autor:
Mian Gao, David J. Shuster, Hai-Yun Xiao, Christine B. Goldstine, Jing Chen, Zhonghui Lu, Victor R. Guarino, Khehyong Ngu, Lisa M. Kopcho, Deepa Calambur, Kurt R. Gregor, Andrew J. Tebben, Jingwu Duan, Luisa Salter-Cid, Hao Lu, Joseph A. Tino, Ning Li, John Hynes, James R. Burke, Joseph Yanchunas, John E. Macor, Steven Sheriff, Dauh-Rurng Wu, Bin Jiang, Patrick J. Shaw, ChiehYing Y. Chang, Jenny Xie, Vojkan Susulic, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 63:15050-15071
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4023f6e8b3a6052dbeee946d81173312
https://doi.org/10.1021/acs.jmedchem.0c01732
https://doi.org/10.1021/acs.jmedchem.0c01732
Autor:
Arunachalam Arumugam, Dietmar A. Seiffert, Arvind Mathur, Joanna J. Zheng, Ruth R. Wexler, Jeon Yoon T, Premsai Rai Neithnadka, Earl J. Crain, Paul J. Gilligan, Patrick Y.S. Lam, Yiming Wu, Mahammed Kaspady, Pancras C. Wong, Tianan Fang, Silvi A. Chacko, William R. Ewing, Pabbisetty Kumar Balashanmuga, Zhen Lou, Steven Sheriff, Joseph M. Luettgen, Joseph E. Myers, Wu Yang, Karen A. Rossi, Richard Rampulla, James R. Corte, Amy Lai, Charles G. Clark, Jeffrey M. Bozarth, Yufeng Wang, Sivashankaran Raju
Publikováno v:
Journal of Medicinal Chemistry. 63:7226-7242
Oral factor XIa (FXIa) inhibitors may provide a promising new antithrombotic therapy with an improved benefit to bleeding risk profile over existing antithrombotic agents. Herein, we report application of a previously disclosed cyclic carbamate P1 li
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58ab508367fcb2f182343eb9240eeb1b
https://doi.org/10.1021/acs.jmedchem.0c00464
https://doi.org/10.1021/acs.jmedchem.0c00464
Autor:
Jennifer Brown, Karen E. Parrish, Andrew J. Tebben, Jonathan Lippy, Kamalavenkatesh Palanisamy, Todd Kinsella, Chetan Padmakar Darne, Vinay K. Holenarsipur, Anwar Murtaza, Muthalagu Vetrichelvan, Chunhong Yan, Karen Augustine-Rauch, Max Ruzanov, Mark Fereshteh, Upender Velaparthi, Gopal Dhar, Gregory D. Vite, Peiying Liu, Steven Sheriff, Jayakumar Sankara Warrier, Aravind Anandam, Marina Gelman, Arvind Mathur, Barri Wautlet, Robert M. Borzilleri, Hasibur Rahaman, Zheng Yang, Anuradha Gupta, Arun Kumar Gupta, Rajinder Singh, Joseph Fargnoli, Jesse Swanson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, sel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57c0a6b7db9a564a606d22c0c365bdb7
https://doi.org/10.1021/acsmedchemlett.9b00552
https://doi.org/10.1021/acsmedchemlett.9b00552
Autor:
Karen A. Rossi, Ruth R. Wexler, Steven Sheriff, Dawn Sun, Jeffrey M. Bozarth, Jianqing Li, Elizabeth A. Dierks, James R. Corte, Yiming Wu, Donald J. P. Pinto, Silvi A. Chacko, Michael Galella, Joanna J. Zheng, Joseph E. Myers, Dauh-Rurng Wu, Tianan Fang, Joseph M. Luettgen, Pancras C. Wong, Xiaoping Hou, Pabbisetty Kumar Balashanmuga, Daniel Smith, Indawati De Lucca, Huiping Zhang, Wu Yang, Arvind Mathur, Yufeng Wang, Dilger Andrew K, William R. Ewing, Subramaniam Krishnananthan, Yeheng Zhu, Earl J. Crain, Theresa Ziemba
Publikováno v:
Journal of medicinal chemistry. 65(3)
Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclinical models and human genetics, an inhibitor of FXIa has the potential to be an antithrombotic agent wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bf4f1ea39b0f4f590f90003f6f693cc
https://pubmed.ncbi.nlm.nih.gov/34494428
https://pubmed.ncbi.nlm.nih.gov/34494428
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ada735600c02c9c410a77e52ab96e515
https://pubmed.ncbi.nlm.nih.gov/34560263
https://pubmed.ncbi.nlm.nih.gov/34560263
Autor:
Frank Marsilio, Chiehying Chang, Steven Sheriff, Bradley C. Pearce, Iyoncy Rodrigo, Max Ruzanov, Dasa Lipovsek, Jodi K. Muckelbauer, Mian Gao, Heather Malakian, Dianlin Xie, John A. Newitt, Wai L. Lau
Publikováno v:
Acta Crystallogr F Struct Biol Commun
Hematopoietic progenitor kinase 1 (HPK1) is an intracellular kinase that plays an important role in modulating tumor immune response and thus is an attractive target for drug discovery. Crystallization of the wild-type HPK1 kinase domain has been ham
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfd023143b3944f7c830323b7394ad11
https://pubmed.ncbi.nlm.nih.gov/33439152
https://pubmed.ncbi.nlm.nih.gov/33439152
Autor:
James R. Corte, Donald J. P. Pinto, Tianan Fang, Honey Osuna, Wu Yang, Yufeng Wang, Amy Lai, Charles G. Clark, Jung-Hui Sun, Richard Rampulla, Arvind Mathur, Mahammed Kaspady, Premsai Rai Neithnadka, Yi-Xin Cindy Li, Karen A. Rossi, Joseph E. Myers, Steven Sheriff, Zhen Lou, Timothy W. Harper, Christine Huang, Joanna J. Zheng, Jeffrey M. Bozarth, Yiming Wu, Pancras C. Wong, Earl J. Crain, Dietmar A. Seiffert, Joseph M. Luettgen, Patrick Y. S. Lam, Ruth R. Wexler, William R. Ewing
Publikováno v:
Journal of medicinal chemistry. 63(2)
Factor XIa (FXIa) inhibitors are promising novel anticoagulants, which show excellent efficacy in preclinical thrombosis models with minimal effects on hemostasis. The discovery of potent and selective FXIa inhibitors which are also orally bioavailab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e229aa9df6f6a4673eb0cc686f3666fe
https://pubmed.ncbi.nlm.nih.gov/31833761
https://pubmed.ncbi.nlm.nih.gov/31833761