Výsledky vyhledávání - "Terence P. Keenan"

Rapid identification of a novel phosphodiesterase 7B tracer for receptor occupancy studies using LC─MS/MS

Autor: Jeffrey Vivian, Ali Tabatabaei, Mi Chen, Lindsay Heger, Vincent J. Santora, Chung Demichael, Terence P. Keenan, James Guy Breitenbucher, Jie Chen, Joel Renick, Douglas Zook, Trevor Scott, Guibao Gu, Kathe Stauber

Publikováno v: Neurochemistry International. 137:104735

Phosphodiesterase 7B (PDE7B) inhibition has been considered as a therapeutic target for the treatment of several neurological disorders. Currently, there are no radio-labeled tracers available to determine receptor occupancy (RO) of this target. Deve

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0931dae78e13249d61dbd2990bb2eb1e
https://doi.org/10.1016/j.neuint.2020.104735

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Identification of 5-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)thiophene-2-Carboxamides as Novel and Selective Monoamine Oxidase B Inhibitors Used to Improve Memory and Cognition

Autor: Andrew J. Mcriner, Xianbo Zhou, Mark E. Wilson, Dong Lee, Roderick E.M. Scott, Gary Anderson, Matthew Bletsch, John Nikpur, Rusiko Bourchouladze, Jennifer Stanley, Terence P. Keenan, Alan P. Kaplan, Regina Miller, Darlene Romashko, Adia Zhang

Publikováno v: ACS chemical neuroscience. 8(12)

Initial work in Drosophila and mice demonstrated that the transcription factor cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) is a master control gene for memory formation. The relationship between CREB and memory has a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f7b476ea0c941ce74c09b616a304f20
https://pubmed.ncbi.nlm.nih.gov/28857544

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Hydrogenation of Imino‐bisnitriles—Synthesis of Novel Triamines

Autor: Raji Sundaramoorthi, Terence P. Keenan

Publikováno v: Synthetic Communications. 37:417-423

The hydrogenation of iminonitriles and iminobisnitriles of type 1a–f is a particularly difficult process as the intermediate dieneamines are highly susceptible to addition reactions. A short general method of preparation and purification of 2‐ami

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1ad5b79d9d3e3380c45f9b637399b3d9
https://doi.org/10.1080/00397910601038970

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Bone-Targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:3071-3074

The design of bone-targeted pyrido[2,3-d]pyrimidin-7-ones as Src tyrosine kinase inhibitors is described. Leveraging SAR from known compounds and using structure-based methods, we were able to rapidly incorporate bone binding components, which mainta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::557b75ac7c90bb0fb12e38e1f0a1e1cc
https://doi.org/10.1016/s0960-894x(03)00649-8

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Novel Protein Kinase Inhibitors: SMART Drug Design Technology

Autor: David C. Dalgarno, Surinder S. Narula, Terence P. Keenan, Tomi K. Sawyer, Regine S. Bohacek, William C. Shakespeare, Chester A. Metcalf, Raji Sundaramoorthi, Yihan Wang, Manfred Weigele

Publikováno v: BioTechniques. 34:S2-S15

In retrospect, the emergence of protein kinase drug discovery dates to the identification of the first oncogenic protein kinase, Src, about 25 years ago. This work has led to worldwide research efforts to investigate the genomic and proteomic relatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6db91a14d17fed30378777b30369b8d2
https://doi.org/10.2144/sawyerjun03revised

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A ligand-reversible dimerization system for controlling protein–protein interactions

Autor: Carl T. Rollins, Terence P. Keenan, Marie Rose van Schravendijk, Tim Clackson, Marcos Hatada, David Yaeger, Michael Z. Gilman, Dennis A. Holt, Victor M. Rivera, Lawrence J. Andrade, Derek N. Woolfson, Susan Adams

Publikováno v: Proceedings of the National Academy of Sciences. 97:7096-7101

Chemically induced dimerization provides a general way to gain control over intracellular processes. Typically, FK506-binding protein (FKBP) domains are fused to a signaling domain of interest, allowing crosslinking to be initiated by addition of a b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e3635e4e24a7f917d014ff5f49461f0
https://doi.org/10.1073/pnas.100101997

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Synthesis of chiral nonracemic 4-trans-substituted pipecolic acid derivatives

Autor: Terence P. Keenan, Dennis A. Holt, David Yaeger

Publikováno v: Tetrahedron: Asymmetry. 10:4331-4341

The syntheses and resolutions of enantiomerically enriched 4-phenyl, 4-tert-butyl, and 4-isopropyl pipecolic acids are described. Optically active diastereomers were prepared by diastereomeric salt formation with the chiral base, l -tyrosine hydrazid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9486ec7f999c487268b76f615f29bd41
https://doi.org/10.1016/s0957-4166(99)00473-5

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Synthesis and activity of bivalent FKBP12 ligands for the regulated dimerization of proteins

Autor: Michael Z. Gilman, Nancy L. Courage, Wu Yang, David Yaeger, Jane F. Amara, Terence P. Keenan, Dennis A. Holt, Victor M. Rivera, Carl T. Rollins, Tao Guo, Tim Clackson, Mary Ellen Pavone

Publikováno v: Bioorganic & Medicinal Chemistry. 6:1309-1335

The total synthesis and in vitro activities of a series of chemical inducers of dimerization (CIDs) is described. The use of small-molecule CIDs to control the dimerization of engineered FKBP12-containing fusion proteins has been demonstrated to have

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::854141bcdc68dc29d3ccb0c4c12eec86
https://doi.org/10.1016/s0968-0896(98)00125-4

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