A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT 6 receptor
binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pK i 9) …

This study describes the in vitro characterization of two potent and selective 5‐HT 6 receptor
antagonists at the rat and human recombinant 5‐HT 6 receptor. In binding assays with [ 3 H]…

Although current antipsychotic drugs are effective at treating the psychotic (positive) symptoms
of schizophrenia, they have one or more serious side effects, including extrapyramidal …

ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B
plays essential roles in the autophagosome formation and the autophagy pathway. Herein we …

Ro 63–0563 [4-amino-N-(2,6 bis-methylamino-pyridin-4-yl)-benzene sulfonamide] is a high
affinity 5-hydroxytryptamine 6 (HT 6 ) receptor antagonist with more than 100-fold selectivity …

Autophagy is an evolutionarily conserved homeostasis process through which aggregated
proteins or damaged organelles are enveloped in a double-membrane structure called an …

The synthesis of an array of 8-amino-2-aryl-[1,2,4]triazolo[1,5-a]pyridine-6-carboxyl amide
derivatives is described for the first time. A subset of 20 derivatives were compared to their …

RO-04-6790 (6a) has been identified in a random screen for 5-HT 6 receptor antagonists. In
a medicinal chemistry optimisation program a series of analogs comprising N-heteroaryl- …

Recent clinical trials have indicated that neurokinin 3 receptor antagonists (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)-piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-…

Glioblastoma is an invariably deadly disease. A subpopulation of glioma stem-like cells (GSCs)
drives tumor progression and treatment resistance. Two recent studies demonstrated …