Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State

Autor: Christian Moestrup Jessen, Keith Pitts, Hossein Mohammad-Beigi, Martin Kurnik, Nikolai Lorenzen, Roland G.W. Staal, Cagla Sahin, Daniel E. Otzen, Scot Richard Mente, Frans A. A. Mulder, Jan Skov Pedersen, Camilla Bertel Andersen, Lise Giehm, Warren D. Hirst, Girija Krishnamurthy, Gunna Christiansen, Peter H. Reinhart, Steen V. Petersen

Publikováno v: Kurnik, M, Sahin, C, Andersen, C B, Lorenzen, N, Giehm, L, Mohammad-Beigi, H, Jessen, C M, Pedersen, J S, Christiansen, G, Petersen, S V, Staal, R, Krishnamurthy, G, Pitts, K, Reinhart, P H, Mulder, F A A, Mente, S, Hirst, W D & Otzen, D E 2018, ' Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State ', Cell Chemical Biology, vol. 25, no. 11, pp. 1389-1402 . https://doi.org/10.1016/j.chembiol.2018.08.005

α-Synuclein (αSN) aggregation is central to the etiology of Parkinson's disease (PD). Large-scale screening of compounds to identify aggregation inhibitors is challenged by stochastic αSN aggregation and difficulties in detecting early-stage oligo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d6e9912e43fa58913d068c4c4085319
https://pure.au.dk/portal/da/publications/potent-synuclein-aggregation-inhibitors-identified-by-highthroughput-screening-mainly-target-the-monomeric-state(5db8c797-9129-4ffc-9d50-99cacae6acc6).html

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

Autor: Binqing Wei, Erica VanderPorten, Peter S. Dragovich, Benjamin Fauber, Qin Yue, Jinhua Chen, Shiva Malek, Wang Jing, Charles Z. Ding, Anthony M. Giannetti, Liu Yingchun, Yichin Liu, Ivana Yen, Keith Pitts, Laura Corson, Charles Eigenbrot, Steve Sideris, Mark Ultsch, Sharada Labadie, David Peterson, Thomas Hunsaker

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:5533-5539

A 2-amino-5-aryl-pyrazine was identified as an inhibitor of human lactate dehydrogenase A (LDHA) via a biochemical screening campaign. Biochemical and biophysical experiments demonstrated that the compound specifically interacted with human LDHA. Str

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc4d24781e88cd125e83fc0a00cfb2f0
https://doi.org/10.1016/j.bmcl.2013.08.060

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

Autor: Erica VanderPorten, Binqing Wei, Keith Pitts, Shiva Malek, Benjamin Fauber, Sharada Labadie, Mark Ultsch, Anthony M. Giannetti, Steve Sideris, Huihui Zhang, Qin Yue, Thomas Hunsaker, Charles Z. Ding, Laura Corson, David Peterson, Xuying Zhang, Borlan Pan, Charles Eigenbrot, Yichin Liu, Hans E. Purkey, Peter S. Dragovich, HongXiu Ge, Ivana Yen, Qing Xu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:3186-3194

A novel 2-thio-6-oxo-1,6-dihydropyrimidine-containing inhibitor of human lactate dehydrogenase (LDH) was identified by high-throughput screening (IC50=8.1 μM). Biochemical, surface plasmon resonance, and saturation transfer difference NMR experiment

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7df75d8d3f03ed064874c5460705c89a
https://doi.org/10.1016/j.bmcl.2013.04.001

Getting the Most Value from Your Screens: Advances in Hardware, Software, and Methodologies to Enhance Surface Plasmon Resonance Based Fragment Screening and Hit-to-Lead Support

Autor: Mac Reiter, Keith Pitts, Donald P. Huddler, Houston N. Gilbert, Brandon J. Bravo, Chris Strande, Anthony M. Giannetti

Publikováno v: Fragment-Based Drug Discovery ISBN: 9781849739085

The development and adoption of fragment-based lead discovery is partly driven by the deployment and refinement of the technologies that enable this drug-discovery approach. Advances in the capabilities of the core discovery functions have historical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::82aa4c7b535ff040a4ae707d829acfca
https://doi.org/10.1039/9781782620938-00019

A Re-examination of the Circular Dichroism of the Calicheamicin Enediyne/Dienone Chromophoric Interaction

Autor: George A. Ellestad, Weidong Ding, Girija Krishnamurthy, Keith Pitts

Publikováno v: Organic Letters. 6:1801-1804

A series of calicheamicin derivatives have been made in an effort to delineate the origin of the strong circular dichroism (CD) of calicheamicin reported previously. The CD spectrum of calicheamicin (I) was compared with that of fragments II and III,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4fb4307e32cf07a8bccd07957bc2bdc2
https://doi.org/10.1021/ol0494919