Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Stephen Margosiak"'
Autor:
Todd VanArsdale, RoseAnn Ferre, David A. Matthews, Ian Popoff, Marakovits Joseph T, Brion W. Murray, Joseph Piraino, Barbara Mroczkowski, Dong Liming, Stephen Margosiak, Xinjun Hou, M. Catherine Johnson, James Arthur Thomson, Gerrit Los, Eleanor Dagostino, Chuangxing Guo, Samantha Elizabeth Greasley, Hans E. Parge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5613-5616
Pin1 is a member of the cis-trans peptidyl-prolyl isomerase family with potential anti-cancer therapeutic value. Here we report structure-based de novo design and optimization of novel Pin1 inhibitors. Without a viable lead from internal screenings,
Autor:
Victor I. Nikulin, Sam Chu, Martina E. Tedder, Kelly Sprankle, Kraig M. Yager, Mitra Khalili, Krzysztof Appelt, Li Xiaoming, James Levin, Victoria A. Feher, Stephen Margosiak, Robert Almassy, Zhe Nie
Publikováno v:
Journal of Medicinal Chemistry. 46:5663-5673
The structure-based design, synthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homocysteine/methylthioadenosine (SAH/MTA) nucleosidase are described. Use of 5-aminoindazole as the core scaffold provided
Autor:
Yali Deng, Patrick M O'Connor, Chen-Chen Kan, Pamela Myers, James Register, Luo Chun, Stephen Margosiak, Binh Nguyen, Kevin Ryan, Ping Chen, Karen Lundgren, Anna Tempczyk-Russell
Publikováno v:
Cell. 100(6):681-692
The checkpoint kinase Chk1 is an important mediator of cell cycle arrest following DNA damage. The 1.7 Å resolution crystal structures of the human Chk1 kinase domain and its binary complex with an ATP analog has revealed an identical open kinase co
Autor:
R. Ferre, Varney Michael D, William H. Romines, Theodore Boritzki, Eleanor J. Howland, Cheryl Ann Janson, Stephen Margosiak, Cindy L. Palmer, Robert Almassy, Charlotte A. Bartlett
Publikováno v:
Journal of Medicinal Chemistry. 40:2502-2524
The design, synthesis, biochemical, and biological evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crysta
Autor:
Eleanor F. Howland, Robert C. Jackson, Cindy L. Palmer, Cathy Zhang, Charlotte A. Barlett, Stephen Margosiak, William H. Romines, Theodore J. Boritzki
Publikováno v:
Investigational New Drugs. 14:295-303
The glycinamide ribonucleotide formyltransferase (GARFT) inhibitor, 4-[2-(2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimidino[5,4-6] [1,4]thiazin-6-yl)-(S)-ethyl]-2,5-thienoyl-L-glutamic acid (AG2034), was designed from the X-ray structure of the GARFT do
Autor:
Vanderpool Darin Louis, Jeanine C. Gutowski, Brad Condon, Christopher Pinko, Chen-Chen Kan, Stephen Margosiak
Publikováno v:
Journal of Biological Chemistry. 270:23634-23640
We report here the production of active recombinant single-chain human cytomegalovirus protease in Escherichia coli and development of a continuous assay for this protease. In order to produce the human cytomegalovirus (HCMV) protease for structural
Autor:
Eleanor J. Howland, Varney Michael D, Theodore Boritzki, William H. Romines, Stephen Margosiak, Charlotte A. Bartlett
Publikováno v:
Journal of Heterocyclic Chemistry. 32:1493-1498
The synthesis and biological evaluation of N-[4-(2-trans-[([2,6-diamino-4(3H)-oxopyrimidin-5-yl]methyl)thio]cyclobutyl)benzoyl]-L-glutamic acid (1) is reported. Compound 1 is a potent dihydrofolate reductase (DHFR) inhibitor (Kj = 12 nM) with excelle
Autor:
Theodore Boritzki, Eleanor J. Howland, Varney Michael D, William H. Romines, Charlotte A. Bartlett, Stephen Margosiak
Publikováno v:
ChemInform. 27
Autor:
Cindy L. Palmer, Robert Almassy, R. Ferre, Theodore Boritzki, Charlotte A. Bartlett, Stephen Margosiak, Varney Michael D, Eleanor J. Howland, Cheryl Ann Janson, William H. Romines
Publikováno v:
ChemInform. 28
The design, synthesis, biochemical, and biological evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crysta
Autor:
Carin L. Perretta, April Averill, Shaosong Chu, Robert Almassy, Stephen Margosiak, Jia Lu, Zhe Nie, Erickson Philip Eugene
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(2)
A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo[1,5-a] [1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo[1,5-a] [1,3,5]tria