E. McEachern

发表

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

N. Hastings, B. Butts, R. Hargreaves, 2017, Molecular Neurodegeneration.

AMD070, a CXCR4 Chemokine Receptor Antagonist: Practical Large-Scale Laboratory Synthesis

Gang Chen, G. Bridger, B. Carpenter, 2008 .

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Dominique Schols, E. De Clercq, D. Schols, 2010, Journal of medicinal chemistry.

A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo.

G. Davies, Matthew S Macauley, D. Vocadlo, 2008, Nature chemical biology.

Formation of a novel thiopyranoindole ring system

J. Hutchinson, D. Macdonald, J. Scheigetz, 1992 .

Concise preparation of amino-5,6,7,8-tetrahydroquinolines and amino-5,6,7,8-tetrahydroisoquinolines via catalytic hydrogenation of acetamidoquinolines and acetamidoisoquinolines.

G. Bridger, R. Skerlj, Krystyna A. Skupinska, 2002, The Journal of organic chemistry.

Enzymatic resolution of bicyclic 1-heteroarylamines using Candida antarctica lipase B.

G. Bridger, R. Skerlj, I. Baird, 2003, The Journal of organic chemistry.

Analysis of transition state mimicry by tight binding aminothiazoline inhibitors provides insight into catalysis by human O-GlcNAcase† †Electronic supplementary information (ESI) available: Detailed experimental procedures, NMR spectra and additional figures illustrating Ki graphs, kinetic data, pKa

Y. He, G. Davies, C. Roth, 2016, Chemical science.

Structures of lactate dehydrogenase A (LDHA) in apo, ternary and inhibitor-bound forms.

L. Craig, S. Kolappan, D. Vocadlo, 2015, Acta crystallographica. Section D, Biological crystallography.

Intermolecular copper(I) chloride-mediated coupling of alkenyltrialkylstannane functions: A convenient synthesis of conjugated diene systems

E. Piers, M. Romero, E. McEachern, 1996 .

Intramolecular Michael Additions: Copper(I) Chloride-Mediated Conjugate Addition of Vinyltrimethylstannane Functions to .alpha.,.beta.-Unsaturated Ketones

E. Piers, E. McEachern, P. Burns, 1995 .

Cu(I)-Mediated Intramolecular Conjugate Addition of Alkenyltrimethylstannane Functions to α,β-Unsaturated Ketones: A Convenient Preparation of Functionalized cis-Fused Bicyclo[4.3.0]non-8-en-3-ones and Bicyclo[3.3.0]oct-6-en-3-ones.

E. Piers, E. McEachern, P. Burns, 2001 .

Intramolecular Michael Additions: Copper(I) Chloride‐Mediated Conjugate Addition of Vinyltrimethylstannane Functions to α,. beta.‐Unsaturated Ketones.

E. Piers, E. McEachern, P. Burns, 1995 .

Copper Chloride-Catalyzed and Hydrochloric Acid-Mediated Chemoselective Protiodestannylations of Alkyl (Z)- or (E)-2,3-Bis(trimethylstannyl)-2-alkenoates. Stereoselective Preparation of Alkyl (E)- and (Z)-3-Trimethylstannyl-2-alkenoates

E. Piers, M. Romero, E. McEachern, 1997 .

Copper(I) chloride-mediated oxidative coupling of alkenyltrialkylstannyl functions: efficient stereocontrolled syntheses of uniquely functionalized conjugated diene systems

E. Piers, M. Romero, P. Gladstone, 1997 .

Intermolecular Homocoupling of Alkenyltrimethylstannane Functions Mediated by CuCl: Preparation of Functionalized Conjugated Diene and Tetraene Systems.

E. Piers, J. G. K. Yee, P. Gladstone, 1998 .

Pharmacological inhibition of O-GlcNAcase (OGA) prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice

C. Gong, D. Vocadlo, N. Watson, 2014, Molecular Neurodegeneration.

MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy

Lynn A. Hyde, E. Hostetler, J. Uslaner, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Discovery of MK-8719, A Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.

D. Klein, J. Hess, D. Vocadlo, 2019, Journal of medicinal chemistry.

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

Lynn A. Hyde, N. Hastings, B. Butts, 2017, Molecular Neurodegeneration.

Inorganic Carbonates as Nucleophiles for the Asymmetric Synthesis of Vinylglycidols

B. Trost, E. McEachern, 1999 .

Asymmetric synthesis of oxygen heterocycles via Pd-catalyzed dynamic kinetic asymmetric transformations: application to nucleosides.

B. Trost, O. Kuhn, B. Brown, 2003, Chemistry.

Inorganic Carbonates as Nucleophiles for the Asymmetric Synthesis of Vinylglycidols.

B. Trost, E. McEachern, 2000 .

Asymmetric Synthesis of Oxygen Heterocycles via Pd‐Catalyzed Dynamic Kinetic Asymmetric Transformations: Application to Nucleosides.

B. Trost, O. Kuhn, B. Brown, 2004 .

Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.

D. Schols, R. Wong, S. Fricker, 2012, ACS medicinal chemistry letters.

PHARMACOKINETICS AND PHARMACODYNAMICS TO SUPPORT CLINICAL STUDIES OF MK-8719: AN O-GLCNACASE INHIBITOR FOR PROGRESSIVE SUPRANUCLEAR PALSY

Dawn M. Toolan, Joseph James Duffy, Sean M. Smith, 2016, Alzheimer's & Dementia.

A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo.

G. Davies, Matthew S Macauley, D. Vocadlo, 2008, Nature chemical biology.

EARLY CLINICAL RESULTS AND PRECLINICAL VALIDATION OF THE O-GLCNACASE (OGA) INHIBITOR MK-8719 AS A NOVEL THERAPEUTIC FOR THE TREATMENT OF TAUOPATHIES

Dawn M. Toolan, Joseph James Duffy, J. Renger, 2016, Alzheimer's & Dementia.