title: N'-benzylidene-benzohydrazides as novel and selective tau-PHF ligands.
abstract: The structure activity relationship of N'-benzylidene-benzohydrazide (NBB) binding to tau and paired helical filament (PHF) proteins as well as amyloid-β₁₋₄₂ fibrils indicate differential selectivity for these protein aggregates. The ability of the compounds to stain neurofibrillary tangles and senile plaques isolated from human AD brain was investigated histochemically. These studies resulted in several tau-PHF and amyloid-β₁₋₄₂ fibril selective ligands respectively. Supported by these results, we rationalized a model for the design of selective ligands for tau, PHF, and amyloid-β₁₋₄₂ fibrils.
authors: Clemens Schöpf-Institute of Chemistry and Biochemistry, Technische Universtität Darmstadt, Darmstadt, Germany.
authors: Ali
authors: A
authors: Taghavi
authors: Samir
authors: S
authors: Nasir
authors: Marcus
authors: M
authors: Pickhardt
authors: Roland
authors: R
authors: Heyny-von Haussen
authors: Gerhard
authors: G
authors: Mall
authors: Eckhard
authors: E
authors: Mandelkow
authors: Eva-Maria
authors: EM
authors: Mandelkow
authors: Boris
authors: B
authors: Schmidt
mesh_terms: D000369:Aged, 80 and over; D000544:Alzheimer Disease / Q000473:pathology*; D016229:Amyloid beta-Peptides / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism*; D005260:Female; D006801:Humans; D006834:Hydrazines / Q000737:chemistry / Q000493:pharmacokinetics*; D007211:Indoles; D020128:Inhibitory Concentration 50; D008024:Ligands; D008297:Male; D016874:Neurofibrillary Tangles / Q000187:drug effects*; D010446:Peptide Fragments / Q000493:pharmacokinetics; D058225:Plaque, Amyloid / Q000378:metabolism; D016875:tau Proteins / Q000378:metabolism*
chemical_list: D016229:Amyloid beta-Peptides; D006834:Hydrazines; D007211:Indoles; D008024:Ligands; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42); D016875:tau Proteins; C056565:1,2-dibenzoyl-tert-butylhydrazine; C007293:DAPI