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Sitte, Harald

Ausgewählte Publikationen

  • Mayer FP, Niello M, Cintulova D, Sideromenos S, Maier J, Li Y, Bulling S, Kudlacek O, Schicker K, Iwamoto H, Deng F, Wan J, Holy M, Katamish R, Sandtner W, Li Y, Pollak DD, Blakely RD, Mihovilovic MD, Baumann MH, Sitte HH. Serotonin-releasing agents with reduced off-target effects. Mol Psychiatry. 2022 Nov 9:1–11. doi: 10.1038/s41380-022-01843-w. 
  • Khanppnavar B, Maier J, Herborg F, Gradisch R, Lazzarin E, Luethi D, Yang JW, Qi C, Holy M, Jäntsch K, Kudlacek O, Schicker K, Werge T, Gether U, Stockner T, Korkhov VM, Sitte HH. Structural basis of organic cation transporter-3 inhibition. Nat Commun. 2022 Nov 7;13(1):6714. doi: 10.1038/s41467-022-34284-8.
  • Luethi D, Maier J, Rudin D, Szöllősi D, Angenoorth TJF, Stankovic S, Schittmayer M, Burger I, Yang JW, Jaentsch K, Holy M, Das AK, Brameshuber M, Camacho-Hernandez GA, Casiraghi A, Newman AH, Kudlacek O, Birner-Gruenberger R, Stockner T, Schütz GJ, Sitte HH. Phosphatidylinositol 4,5-bisphosphate (PIP2) facilitates norepinephrine transporter dimerization and modulates substrate efflux. Commun Biol. 2022 Nov 17;5(1):1259. doi: 10.1038/s42003-022-04210-1. 
  • Rudin D, McCorvy JD, Glatfelter GC, Luethi D, Szöllősi D, Ljubišić T, Kavanagh PV, Dowling G, Holy M, Jaentsch K, Walther D, Brandt SD, Stockner T, Baumann MH, Halberstadt AL, Sitte HH. (2-Aminopropyl)benzo[β]thiophenes (APBTs) are novel monoamine transporter ligands that lack stimulant effects but display psychedelic-like activity in mice. Neuropsychopharmacology. 2022 Mar;47(4):914-923. doi: 10.1038/s41386-021-01221-0.
  • Maier J, Rauter L, Rudin D, Niello M, Holy M, Schmid D, Wilson J, Blough BE, Gannon BM, Murnane KS, Sitte HH. α-PPP and its derivatives are selective partial releasers at the human norepinephrine transporter: A pharmacological characterization of interactions between pyrrolidinopropiophenones and high and low affinity monoamine transporters. Neuropharmacology. 2021 Jun 1;190:108570. doi: 10.1016/j.neuropharm.2021.108570. 
  • Niello M, Cintulová D, Raithmayr P, Holy M, Jäntsch K, Colas C, Ecker GF, Sitte HH, Mihovilovic MD. Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro. Front Pharmacol. 2021 Apr 9;12:654061. doi: 10.3389/fphar.2021.654061. 


Stand alone projects:

  • "Transporter-mediated efflux as therapeutic strategy”

Project number: P 35589
FWF Einzelprojekt
project lead: Harald H. SITTE

  • "Analysis of missense mutations in organic cation transporter”

Project number: P 34670
FWF Einzelprojekt
project lead: Harald H. SITTE

  • "Engineering Diffusion Barriers in the Plasma Membrane"

Project number: P 33955
FWF Einzelprojekt
project lead: Gerhard J. SCHÜTZ

Doctoral programmes: 

  • MolTag FWF W 1232 – project lead: Gerhard ECKER
  • NeuTrans EU-Marie Curie Sklodowska Actions – project lead: Thomas STOCKNER


Neurotransmitters transporters are located in presynaptic specializations. They inactivate neurotransmitter-mediated neurotransmission following exocytotic release by a simple reuptake mechanism. Recent crystallographic examination of the mammalian serotonin transporter provides a structural scaffold which supports transport by an alternative access mechanism.

Monoamine transporters are a target of clinically relevant drugs: (i) antidepressants competitively block the reuptake of monoamines. Thereby, these compounds enhance the extracellular monoamine concentration which is relevant for clinical success. (ii) amphetamines and cathinones, some of which behave as substrates of the transporters, trigger non-exocytotic neurotransmitter release (transporter-mediated efflux). The exact molecular mechanism of the psychostimulant action, however, still remains enigmatic. Neurotransmitter transporters are subject to regulation by constituents of the plasma membrane such as cholesterol and phosphoinositides.

In addition, neurotransmitter transporters engage in quaternary complexes, which are also determined by their interaction with lipids. 

Understanding the structure-activity relationships of neurotransmitter transporters (especially the monoaminergic, high-affinity and low capacity transporters such as transporters for dopamine, norepinephrine and serotonin – and also the low-affinity, high capacity transporters such as organic cation transporters), the trafficking processes to and at the plasma membrane, the functional impact of the lipids in the plasma membrane – this is the declared goal of my research.

Univ.-Prof. Dr. Harald Sitte