Latest Publications
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
Deposition of hyperphosphorylated and aggregated tau protein in the central nervous system is characteristic of Alzheimer disease and other tauopathies. Tau is subject to O-linked N-acetylglucosamine (O-GlcNAc) modification, and O-GlcNAcylation of tau has been shown [...]
Discovery of MK-8719, A Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies
Inhibition of O-GlcNAcase (OGA) has emerged as a promising therapeutic approach to treat tau pathology in neurodegenerative diseases such as Alzheimer’s disease and progressive supranuclear palsy. Beginning with carbohydrate-based lead molecules, we pursued an optimization [...]
Mutant Huntingtin Disrupts the Nuclear Pore Complex
Huntington's disease (HD) is caused by an expanded CAG repeat in the Huntingtin (HTT) gene. The mechanism(s) by which mutant HTT (mHTT) causes disease is unclear. Nucleocytoplasmic transport, the trafficking of macromolecules between the nucleus [...]
The Discovery and Characterization of [18F]MK‐8553, a Novel PET Tracer for Imaging O‐GlcNAcase (OGA)
[18F]MK-8553 is a high affinity, selective OGA inhibitor with properties suitable for imaging OGA and determining central enzyme occupancy in both preclinical and clinical studies. Currently [18F]MK‐8553 is being utilized in humans as a PET [...]
Alectos Therapeutics Announces FDA Orphan Drug Designation for MK-8719: An Investigational Small-molecule OGA Inhibitor for Treatment of Progressive Supranuclear Palsy
Advances Novel Tau-directed Strategy for Treating Neurodegenerative Disease Phase 1 Clinical Trial Completed Vancouver, British Columbia (April 20, 2016) – Alectos Therapeutics Inc. today announced that the U.S. Food and Drug Administration (FDA) has granted [...]
Preclinical Data Disclosed for Tau PET Tracer MK-6240: A Potential Clinical Biomarker for OGA Inhibitor MK-8719
Apr 18, 2016 – Alectos Therapeutics partner Merck, known as MSD outside the U.S. and Canada, today disclosed preclinical data for potential clinical biomarker [18F]-MK-6240, a highly selective and specific tau PET tracer useful as an [...]