Zobrazeno 1 - 10
of 15
pro vyhledávání: '"FLIRI, A. F. J."'
Autor:
Raymond S. Hurst, Mihály Hajós, Dennis J. Hoover, William E. Hoffmann, Nandini Chaturbhai Patel, Christopher L. Shaffer, Xinjun J. Hou, Christopher J. O’Donnell, Dina McGinnis, Jayvardhan Pandit, Eric S. Marr, Randall James Gallaschun, Dianne K. Bryce, John T. Lazzaro, Longfei Xie, Jacob Bradley Schwarz, Fliri Anton F J, Justin L Gazard, Ashley N. Hanks, Renato J. Scialis
Publikováno v:
Journal of Medicinal Chemistry. 56:9180-9191
Positive allosteric modulators ("potentiators") of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors (AMPAR) enhance excitatory neurotransmission and may improve the cognitive deficits associated with various neurological disorde
Publikováno v:
Nature Chemical Biology. 1:389-397
The high failure rate of experimental medicines in clinical trials accentuates inefficiencies of current drug discovery processes caused by a lack of tools for translating the information exchange between protein and organ system networks. Recently,
Publikováno v:
Proceedings of the National Academy of Sciences. 102:261-266
Establishing quantitative relationships between molecular structure and broad biological effects has been a longstanding challenge in science. Currently, no method exists for forecasting broad biological activity profiles of medicinal agents even wit
Publikováno v:
Current Opinion in Chemical Biology. 2:535-540
The identification of a novel dopamine receptor subtype, referred to as the D4 receptor, which binds the atypical antipsychoti drug clozapine with high potency, has led to the initiation of a drug discovery program that aims to find novel inhibitors
Autor:
Fliri Anton F J, Kristopher Bosse, Robert A. Volkmann, Deane M. Nason, Barb E. Segelstein, Jason Marineau, Desai Kishor A
Publikováno v:
Tetrahedron Letters. 47:7285-7287
Use of alkyl substituted propylene linkers as a strategy for fine-tuning the biological activity of medicinal agents requires ready access to these substrates. Herein, a general strategy is described for stereospecifically generating 18 chiral mono-
Publikováno v:
ChemInform. 22
N-(5-Fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxam ide (1) is a member of a series of amides found to substantially increase lifespan in mice bearing established micrometastatic 3LL Lewis lung carcinoma. Amide 1 is effective after either or
Publikováno v:
Trends in pharmacological sciences. 31(11)
Current target-based drug discovery platforms are not able to predict drug efficacy and the full spectrum of drug effects in organisms. Hence, many experimental drugs do not survive the lengthy and costly process of drug development. Understanding ho
Publikováno v:
Journal of medicinal chemistry. 52(24)
Understanding how drugs affect cellular network structures and how resulting signals are translated into drug effects holds the key to the discovery of medicines. Herein we examine this cause-effect relationship by determining protein network structu
Autor:
Fliri Anton F J, Michelle Vanase-Frawley, Scot Richard Mente, Lorrie Lebel, Anne W. Schmidt, Randall James Gallaschun
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(23)
QSAR models have been used to evaluate activities for compounds in the phenoxyphenyl-methanamine (PPMA) class of compounds. These models utilize Hammett-type donating–withdrawing substituent values as well as simple parameters to describe substitue
Publikováno v:
ChemMedChem. 2(12)
Preclinical pharmacology studies conducted with experimental medicines currently focus on assessments of drug effects attributed to a drug's putative mechanism of action. The high failure rate of medicines in clinical trials, however, underscores tha