2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.

CD73 inhibitors are promising drugs for the (immuno)therapy of cancer. Here, we present the synthesis, structure-activity relationships, and cocrystal structures of novel derivatives of the competitive CD73 inhibitor α,β-methylene-ADP (AOPCP) substituted in the 2-position. Small polar or lipophilic residues increased potency, 2-iodo- and 2-chloro-adenosine-5'--[(phosphonomethyl)phosphonic acid] (, ) being the most potent inhibitors with values toward human CD73 of 3-6 nM.

Reading Your Mind While You Are Reading-Evidence for Spontaneous Visuospatial Perspective Taking During a Semantic Categorization Task.

Recent studies have demonstrated people's propensity to adopt others' visuospatial perspectives (VSPs) in a shared physical context. The present study investigated whether spontaneous VSP taking occurs in mental space where another person's perspective matters for mental activities rather than physical actions. Participants sat at a 90° angle to a confederate and performed a semantic categorization task on written words.

Out of your sight, out of my mind: Knowledge about another person's visual access modulates spontaneous visuospatial perspective-taking.

Accumulating evidence suggests that humans spontaneously adopt each other's visuospatial perspective (VSP), but many aspects about the underlying mechanisms remain unknown. The aim of this study was to investigate whether knowledge about another's visual access systematically modulates spontaneous VSP-taking. In a spatial compatibility task, a participant and a confederate sat at a 90°angle to each other, with visual stimuli being aligned vertically for the participants and horizontally for the confederate.

When do humans spontaneously adopt another's visuospatial perspective?

Perspective-taking is a key component of social interactions. However, there is an ongoing controversy about whether, when and how instances of spontaneous visuospatial perspective-taking occur. The aim of this study was to investigate the underlying factors as well as boundary conditions that characterize the spontaneous adoption of another person's visuospatial perspective (VSP) during social interactions.

α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5'-Nucleotidase (CD73) Inhibitors.

ecto-5'-Nucleotidase (eN, CD73) catalyzes the hydrolysis of extracellular AMP to adenosine. eN inhibitors have potential for use as cancer therapeutics. The eN inhibitor α,β-methylene-ADP (AOPCP, adenosine-5'-O-[(phosphonomethyl)phosphonic acid]) was used as a lead structure, and derivatives modified in various positions were prepared.