Výsledky vyhledávání - "L. Grunewald"

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Notfallmedizin in der Deutschen Gesellschaft zur Rettung Schiffbrüchiger – Auswertung medizinischer Notfälle auf der Nord- und Ostsee über 2 Jahre

Autor: S. Schemke, L. Grunewald, H. Schwalbe, H. Maurer

Publikováno v: Der Anaesthesist

The logistic peculiarities of an emergency maritime location and the frequent additional threat of accidental hypothermia mean that the treatment of medical emergencies at sea are particularly demanding. This article describes the characteristics of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::517f0ada7f2cea937e5564ca57e7598a
https://doi.org/10.1007/s00101-020-00885-5

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Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine N-Methyltransferase Possessing Low Nanomolar Affinity at Both Substrate Binding Domains1

Autor: Qian Wu, Gary L. Grunewald, Michael J. McLeish, Jian Lu, Kevin R. Criscione, Emily E. Scott, Aaron G. Bart

Publikováno v: Journal of Medicinal Chemistry. 63:13878-13898

The enzyme phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28) catalyzes the final step in the biosynthesis of epinephrine and is a potential drug target, primarily for the control of hypertension. Unfortunately, many potent PNMT inhibitors al

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3f81629ebc9f59e2bc015723a28fdcaa
https://doi.org/10.1021/acs.jmedchem.0c01475

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Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine

Autor: Jian, Lu, Aaron G, Bart, Qian, Wu, Kevin R, Criscione, Michael J, McLeish, Emily E, Scott, Gary L, Grunewald

Publikováno v: J Med Chem

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f4e8060263b4b8969f035009b95b3db7
https://pubmed.ncbi.nlm.nih.gov/33147410

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Akademický článek

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Molecular recognition of physiological substrate noradrenaline by the adrenaline-synthesizing enzyme PNMT and factors influencing its methyltransferase activity

Autor: Jennifer L. Martin, Munish Puri, Christine L. Gee, Nyssa Drinkwater, Kevin R. Criscione, Gary L. Grunewald, Michael J. McLeish

Publikováno v: Biochemical Journal. 422:463-471

Substrate specificity is critically important for enzyme catalysis. In the adrenaline-synthesizing enzyme PNMT (phenylethanolamine N-methyltransferase), minor changes in substituents can convert substrates into inhibitors. Here we report the crystal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22d13e4f180179949f4264abeb20d516
https://doi.org/10.1042/bj20090702

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Quand adresser un enfant chez l’orthodontiste ?

Autor: T. Davit-Béal, A. Vanderzwalm, A. Beslot, A. Lautrou, L. Grunewald

Publikováno v: Archives de Pédiatrie. 15:1242-1248

Orthodontic treatments aim at improving the positions of teeth, the form of dental arches and their reports relations. Determining the age to perform these treatments consists in defining the ideal moment to achieve them in the shortest time possible

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::33cf2b0a795708546ca925895bbe1b2b
https://doi.org/10.1016/j.arcped.2008.04.002

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Application of the Goldilocks Effect to the Design of Potent and Selective Inhibitors of Phenylethanolamine N-Methyltransferase: Balancing pKa and Steric Effects in the Optimization of 3-Methyl-1,2,3,4-tetrahydroisoquinoline Inhibitors by β-Fluorination

Autor: Kevin R. Criscione, Mitchell R. Seim, Mariam Makboul, Gary L. Grunewald, Jian Lu

Publikováno v: Journal of Medicinal Chemistry. 49:2939-2952

3-Methyl-1,2,3,4-tetrahydroisoquinolines (3-methyl-THIQs) are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT), but are not selective due to significant affinity for the α2-adrenoceptor. Fluorination of the methyl group lowers the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::502296631154e53e44a846cee123dd6c
https://doi.org/10.1021/jm051262k

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Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity

Autor: Cosmas O. Okoro, Kevin R. Criscione, Jian Lu, Gary L. Grunewald

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:5319-5323

A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the alpha(2)-adrenoceptor. Although their PNMT inhibitory potency

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57beb88675c6415b8d781e8f5747fb00
https://doi.org/10.1016/j.bmcl.2005.08.033

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Disulfide-linked dimers of human adrenaline synthesizing enzyme PNMT are catalytically active

Autor: Amanda Nourse, Christine L. Gee, Qian Wu, Michael J. McLeish, A-Yen Hsin, Joel D. A. Tyndall, Jennifer L. Martin, Gary L. Grunewald

Publikováno v: Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1750:82-92

The crystal structure of human phenylethanolamine N-methyltransferase (hPNMT) reveals a disulfide-linked dimer, despite the presence of reducing agent in the crystallisation conditions. By removing the reducing agent, hPNMT crystals grow more rapidly

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7746706a68a5f848331c7b67a1f1e43
https://doi.org/10.1016/j.bbapap.2005.03.006

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