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Browsing by Author "Sahlholm, Kristoffer"

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Dopamine D 2 receptor agonist binding kinetics-role of a conserved serine residue

Ågren, Richard; Stepniewski, Tomasz Maciej, 1988-; Zeberg, Hugo; Selent, Jana; Sahlholm, Kristoffer (MDPI, 2021)

The forward (kon) and reverse (koff) rate constants of drug-target interactions have important implications for therapeutic efficacy. Hence, time-resolved assays capable of measuring these binding rate constants may be ...
Ligand with two modes of interaction with the dopamine D2 receptor-an induced-fit mechanism of insurmountable antagonism

Ågren, Richard; Zeberg, Hugo; Stepniewski, Tomasz Maciej, 1988-; Free, R. Benjamin; Reilly, Sean W.; Luedtke, Robert R.; Århem, Peter; Ciruela, Francisco; Sibley, David R.; Mach, Robert H.; Selent, Jana; Nilsson, Johanna; Sahlholm, Kristoffer (American Chemical Society (ACS), 2020)

A solid understanding of the mechanisms governing ligand binding is crucial for rational design of therapeutics targeting the dopamine D2 receptor (D2R). Here, we use G protein-coupled inward rectifier potassium (GIRK) ...
Mechanistic insights into dopaminergic and serotonergic neurotransmission - concerted interactions with helices 5 and 6 drive the functional outcome

Stepniewski, Tomasz Maciej, 1988-; Mancini, Arturo; Ågren, Richard; Torrens Fontanals, Mariona; Semache, Meriem; Bouvier, Michel; Sahlholm, Kristoffer; Breton, Billy; Selent, Jana (Royal Society of Chemistry, 2021)

Brain functions rely on neurotransmitters that mediate communication between billions of neurons. Disruption of this communication can result in a plethora of psychiatric and neurological disorders. In this work, we combine ...

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Browsing by Author "Sahlholm, Kristoffer"

Browsing by Author "Sahlholm, Kristoffer"

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