Výsledky vyhledávání - "Silvia L Delker"

Akademický článek

Naegleria fowleri: Protein structures to facilitate drug discovery for the deadly, pathogenic free-living amoeba.

Publikováno v: PLoS ONE, Vol 16, Iss 3, p e0241738 (2021)

Naegleria fowleri is a pathogenic, thermophilic, free-living amoeba which causes primary amebic meningoencephalitis (PAM). Penetrating the olfactory mucosa, the brain-eating amoeba travels along the olfactory nerves, burrowing through the cribriform

Externí odkaz: https://doaj.org/article/23d070499b154d11aa93fd5498f6c574

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Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs

Publikováno v: Nature Structural & Molecular Biology. 21:803-809

The Cul4-Rbx1-DDB1-Cereblon E3 ubiquitin ligase complex is the target of thalidomide, lenalidomide and pomalidomide, therapeutically important drugs for multiple myeloma and other B-cell malignancies. These drugs directly bind Cereblon (CRBN) and pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b131abf0f427feaba8ec6b36dad4572
https://doi.org/10.1038/nsmb.2874

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Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase

Autor: Jan J. Mataka, Silvia L. Delker, Thomas L. Poulos, James M. Kraus, Kristin J. Labby, Richard B. Silverman, Huiying Li, Pavel Martásek, Haitao Ji, Linda J. Roman, Fengtian Xue

Publikováno v: Bioorganic & Medicinal Chemistry. 21:1333-1343

Inhibitors of neuronal nitric oxide synthase have been proposed as therapeutics for the treatment of different types of neurological disorders. On the basis of a cis-3,4-pyrrolidine scaffold, a series of trans-cyclopropyl- and methyl-containing nNOS

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ad9b2acca38c563e0b5f71e1ae053d0
https://doi.org/10.1016/j.bmc.2012.12.019

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Improved Synthesis of Chiral Pyrrolidine Inhibitors and Their Binding Properties to Neuronal Nitric Oxide Synthase

Autor: Fengtian Xue, Richard B. Silverman, Kristin J. Labby, Pavel Martásek, Thomas L. Poulos, Haitao Ji, Guoyao Xia, Huiying Li, Linda J. Roman, James M. Kraus, Silvia L. Delker, Jan J. Mataka

Publikováno v: Journal of Medicinal Chemistry. 54:6399-6403

We report an efficient synthetic route to chiral pyrrolidine inhibitors of neuronal nitric oxide synthase (nNOS) and crystal structures of the inhibitors bound to nNOS and to endothelial NOS. The new route enables versatile structure activity relatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a3571ed8ff55e040aa553d1e4578a32
https://doi.org/10.1021/jm200411j

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Exploration of the Active Site of Neuronal Nitric Oxide Synthase by the Design and Synthesis of Pyrrolidinomethyl 2-Aminopyridine Derivatives

Autor: Linda J. Roman, Thomas L. Poulos, Pavel Martásek, Silvia L. Delker, Richard B. Silverman, Haitao Ji, Huiying Li

Publikováno v: Journal of Medicinal Chemistry. 53:7804-7824

Neuronal nitric oxide synthase (nNOS) represents an important therapeutic target for the prevention of brain injury and the treatment of various neurodegenerative disorders. A series of trans-substituted amino pyrrolidinomethyl 2-aminopyridine deriva

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a383852c18d28ed2367dca382a14c5a0
https://doi.org/10.1021/jm100947x

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Crystallographic studies of ligand binding by Zn-α2-glycoprotein

Autor: Lindsay C. McDermott, Silvia L. Delker, Pamela J. Bjorkman, Anthony P. West, Malcolm W. Kennedy

Publikováno v: Journal of Structural Biology. 148:205-213

Zn-alpha2-glycoprotein (ZAG) is a 41 kDa soluble protein that is present in most bodily fluids. The previously reported 2.8 A crystal structure of ZAG isolated from human serum demonstrated the structural similarity between ZAG and class I major hist

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e201f3523fce267aebc0b309357f0cd6
https://doi.org/10.1016/j.jsb.2004.04.009

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The mobility of a conserved tyrosine residue controls isoform-dependent enzyme-inhibitor interactions in nitric oxide synthases

Autor: Richard B. Silverman, Carla Plaza, Soosung Kang, Qing Jing, Haitao Ji, Thomas L. Poulos, Huiying Li, He Huang, Silvia L. Delker, Joumana Jamal

Publikováno v: Biochemistry

Many pyrrolidine-based inhibitors highly selective for neuronal nitric oxide synthase (nNOS) over endothelial NOS (eNOS) exhibit dramatically different binding modes. In some cases, the inhibitor binds in a 180° flipped orientation in nNOS relative

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f21a3d337f576646b49c6933de93d48
https://pubmed.ncbi.nlm.nih.gov/25089924

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Symmetric double-headed aminopyridines, a novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase

Autor: Richard B. Silverman, Huiying Li, Linda J. Roman, Fengtian Xue, Jianguo Fang, Thomas L. Poulos, Silvia L. Delker, Pavel Martásek

Publikováno v: Journal of medicinal chemistry. 54(7)

We report novel neuronal nitric oxide synthase (nNOS) inhibitors based on a symmetric double-headed aminopyridine scaffold. The inhibitors were designed from crystal structures of leads 1 and 2 (Delker, S. L.; Ji, H.; Li, H.; Jamal, J.; Fang, J.; Xue

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::959b0b7472d328e549471c1d258e7e2e
https://pubmed.ncbi.nlm.nih.gov/21410186

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