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Autor:
Kristin Kelly, Christopher John Helal, Tate Bonnie Frances, Mavis Diane Adam, Zhijun Kang, Marcia F. Peterson, Thomas G. Gant, Christopher B. Cooper, Michael K. Ahlijanian, Stanley William Kupchinsky, John C. Lucas, Frank S. Menniti, Sanner Mark Allen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5521-5525
High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320
Publikováno v:
Current Topics in Medicinal Chemistry. 2:395-415
Neurofibrillary tangles (NFTs) are a distinguishing neuropathological feature found in postmortem brains of Alzheimer s disease (AD) and tauopathy patients. The density of these lesions correlates with severity of AD and their distribution follows a
Autor:
Sanner Mark Allen
Publikováno v:
Expert Opinion on Therapeutic Patents. 8:383-393
The discovery that the atypical antipsychotic clozapine has higher affinity for the dopamine D4 receptor relative to the D2 receptor touched off a search for more potent, highly selective D4 antagonists as a new class of antipsychotics. Many compound
Publikováno v:
Psychopharmacology. 135:194-200
Recent evidence suggests that the dopamine D4 receptor may play a role in schizophrenia, and that the atypical properties of the antipsychotic clozapine may be attributable in part to its antagonistic actions at this receptor. In the present study, c
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:
Sanner Mark Allen, Robert W. Dugger, Cliff Meltz, Thomas Allen Chappie, Audrey R. Dunaiskis, T. Keltonic, Tom Staigers
Publikováno v:
ChemInform. 26
Autor:
A L A L Et Et, Sanner Mark Allen
Publikováno v:
ChemInform. 29
Autor:
Christopher J. Schmidt, Sanner Mark Allen, Karen M. Ward, Susan E. Drozda, James J. Valentine, John A. Lowe, Shari L. DeNinno, Don Tunucci, F. David Tingley
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(3)
We describe a novel series of inhibitors of the type 1 glycine transporter (GlyT1) as an approach to relieving the glutamatergic deficit that is thought to underlie schizophrenia. Synthesis and SAR follow-up of a series of octahydro-cyclopenta[c]pyrr
Autor:
Lowe, John A., III, DeNinno, Shari L., Drozda, Susan E., Schmidt, Christopher J., Ward, Karen M., David Tingley, F., III, Sanner, Mark, Tunucci, Don, Valentine, James
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2010 20(3):907-911