Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Christopher E. Heise"'
Autor:
Dawei Sun, Kelly M. Storek, Dimitry Tegunov, Ying Yang, Christopher P. Arthur, Matthew Johnson, John G. Quinn, Weijing Liu, Guanghui Han, Hany S. Girgis, Mary Kate Alexander, Austin K. Murchison, Stephanie Shriver, Christine Tam, Hiroshi Ijiri, Hiroko Inaba, Tatsuya Sano, Hayato Yanagida, Junichi Nishikawa, Christopher E. Heise, Wayne J. Fairbrother, Man-Wah Tan, Nicholas Skelton, Wendy Sandoval, Benjamin D. Sellers, Claudio Ciferri, Peter A. Smith, Patrick C. Reid, Christian N. Cunningham, Steven T. Rutherford, Jian Payandeh
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-15 (2024)
Abstract BamA is the central component of the essential β-barrel assembly machine (BAM), a conserved multi-subunit complex that dynamically inserts and folds β-barrel proteins into the outer membrane of Gram-negative bacteria. Despite recent advanc
Externí odkaz:
https://doaj.org/article/bf48c6d78a39468c81c644c4c61faa56
Autor:
J. Hiroshi Morisaki, Peter A. Smith, Shailesh V. Date, Kimberly K. Kajihara, Chau Linda Truong, Zora Modrusan, Donghong Yan, Jing Kang, Min Xu, Ishita M. Shah, Robert Mintzer, Eric M. Kofoed, Tommy K. Cheung, David Arnott, Michael F. T. Koehler, Christopher E. Heise, Eric J. Brown, Man-Wah Tan, Wouter L. W. Hazenbos
Publikováno v:
mBio, Vol 7, Iss 5 (2016)
ABSTRACT The type I signal peptidase of Staphylococcus aureus, SpsB, is an attractive antibacterial target because it is essential for viability and extracellularly accessible. We synthesized compound 103, a novel arylomycin-derived inhibitor of SpsB
Externí odkaz:
https://doaj.org/article/3b9f916136964f4eb118797ed067be1e
Autor:
Yuan Chen, Matthew R. Durk, Lionel Rouge, Peter A. S. Smith, Man-Wah Tan, John S. Wai, Jacob Schwarz, Tucker C. Roberts, Jing Kang, Donghong Yan, Hany S. Girgis, Summer Park, John G. Quinn, Min Xu, Prasuna Paraselli, Christopher E. Heise, Jeremy Murray, Wilson Phung, Yongsheng Chen, James J. Crawford, Robert I. Higuchi, Zhiyong Yu, Michael F. T. Koehler, Elizabeth Skippington, Hua Zhang
Publikováno v:
Nature. 561:189-194
Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts no new class of antibiotic with activity against Gram-negative bacteria has been approved in over fifty years. Natural products and their derivatives have a k
Autor:
Daniel J. Burdick, Lauren Goeser, Jianping Yin, Shumei Wang, John Moffat, Steven Magnuson, Weiru Wang, Jeff Blaney, Huifen Chen, Borlan Pan, Christopher E. Heise, Jake Drummond
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4728-4732
A fragment-based lead discovery approach was used to discover novel ERK2 inhibitors. The crystal structure of N-benzyl-9H-purin-6-amine 1 in complex with ERK2 elucidated its hinge-binding mode. In addition, the simultaneous binding of an imidazole mo
Autor:
Jing Kang, Robert Mintzer, Kimberly Kajihara, Wouter L. W. Hazenbos, Shailesh V. Date, Peter A. S. Smith, J. Hiroshi Morisaki, Eric M. Kofoed, Man-Wah Tan, Eric J. Brown, Tommy K. Cheung, Donghong Yan, Chau Linda Truong, David Arnott, Ishita M. Shah, Michael F. T. Koehler, Zora Modrusan, Min Xu, Christopher E. Heise
Publikováno v:
mBio, Vol 7, Iss 5 (2016)
Microbial Cell
mBio, Vol 7, Iss 5, p e00412-16 (2016)
mBio
Microbial Cell
mBio, Vol 7, Iss 5, p e00412-16 (2016)
mBio
The type I signal peptidase of Staphylococcus aureus, SpsB, is an attractive antibacterial target because it is essential for viability and extracellularly accessible. We synthesized compound 103, a novel arylomycin-derived inhibitor of SpsB with sig
Autor:
Wendy Lee, Lionel Rouge, Joachim Rudolph, Sreemathy Ramaswamy, Klaus P. Hoeflich, Suzanne Tay, Lesley J. Murray, Ignacio Aliagas, Christopher E. Heise, Hank La, Weiru Wang, Robert Mintzer, James J. Crawford, Simon Mathieu
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(15)
A series of 4-azaindole-containing p21-activated kinase-1 (PAK1) inhibitors was prepared with the goal of improving physicochemical properties relative to an indole starting point. Indole 1 represented an attractive, non-basic scaffold with good PAK1
Autor:
Jennifer Epler, Joachim Rudolph, Joy Drobnick, Roxanne Vega, Ignacio Aliagas, Sreemathy Ramaswamy, Elizabeth Blackwood, Klaus P. Hoeflich, Diana Jakubiak, Wendy Lee, Haiming Zhang, Xianrui Zhao, Weiru Wang, Christopher E. Heise, David Favor, Chudi Ndubaku, Thomas W. O'Brien, Gary A. Cain, Lesley J. Murray, Paroma Chakravarty, Hank La, Christy C. Ong, Ping Dong, Connie Chan, James J. Crawford, Angela Oh, Yu Zhong, Dolores Díaz, Lewis J. Gazzard
Publikováno v:
Journal of medicinal chemistry. 59(11)
p21-activated kinase 1 (PAK1) has an important role in transducing signals in several oncogenic pathways. The concept of inhibiting this kinase has garnered significant interest over the past decade, particularly for targeting cancers associated with
Autor:
Amy Gustafson, Maureen Beresini, Linda O. Elliott, Robert Mintzer, Kevin R Clark, Christopher E. Heise, Cristina Lewis, Kinjalkumar Shah, Marya Liimatta, Yichin Liu, Adam R. Johnson, Stephen Schmidt
Publikováno v:
SLAS Discovery. 17:225-236
Identifying chemical lead matter by high-throughput screening (HTS) has been a common practice in early stage drug discovery. Evolution of small-molecule library composition to include more drug-like molecules with desirable physical chemical propert
Publikováno v:
ASSAY and Drug Development Technologies. 8:497-503
The Ras, Raf, mitogen-activated protein kinase kinase (MEK) and extracellular signal-regulated kinase (ERK) signaling cascade is critically involved in cellular signaling with activating mutations in Ras and Raf present in many human tumors. Each con
Autor:
Jason Haelewyn, Brian Dyck, Troy Vickers, Junko Tamiya, Mingzhu Zhang, Linh Nguyen, Martin W. Rowbottom, David A. Schwarz, Val S. Goodfellow, Monica S. Mistry, Christopher E. Heise, Jonathan Grey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2535-2539
A series of thienopyrimidinone bis-aminopyrrolidine ureas were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor-1. These compounds exhibit potent binding affinity (K(i)=3 nM) and good in vitro meta