drug designdual agonistsGLP-1obesitystructure-activity relationshipsThe two gut hormones GLPand PYY 3 , which are both secreted from the Lヽells upon food stimuli, have a stronger inhibitory effect on food intake when they are combined, compared to their individual effects as single agonists. ...
The Design of a GLP‐1/PYY Dual Acting Agonist Birgitte Schjellerup WulffSøren ØstergaardMarina Kjaergaard GerstenbergJohan F. Paulsson Mar 2021 The two gut hormones GLP-1 and PYY3–36, which are both secreted from the L-cells upon food stimuli, have a stronger inhibitory effect on fo...
One concept is to design multifunctional agents that possess GLP-1RA pharmacology as a foundation, but that also target alternative pathways to expand the therapeutic index [16., 17., 18.]. A compelling approach may be to combine GLP-1 with an additional pharmacology that promotes the ...
Briefly, several peptides are derived from the gastrointestinal tract, most of which inhibit food intake, namely cholecystokinin (CCK), glucagon-like peptide 1 (GLP-1), peptide tyrosine tyrosine (PYY),2 and the recently discovered nesfatin-1,3 while only one peripherally prod...
For example, in contrast to the over secretion of gas- trin linked to TA, TAAR1 activation by a selective small molecule agonist was associated with elevated plasma levels of peptide tyrosine tyrosine (PYY) and glucagon- like peptide-1 (GLP-1) [186], which may be protective, as decreased...
(CART), which inhibit food intake. Because of the semipermeable blood–brain barrier in this region, peripheral signals indicative of energy balance—including glucose, insulin, leptin, a number of gut-derived factors including glucagon-like peptide-1 (GLP-1), peptide YY (PYY), oxyntomodulin and...
For example, in contrast to the over secretion of gas- trin linked to TA, TAAR1 activation by a selective small molecule agonist was associated with elevated plasma levels of peptide tyrosine tyrosine (PYY) and glucagon- like peptide-1 (GLP-1) [186], which may be protective, as decreased...
Use of pyy and glp-1, or an agonist thereof, for the modification of feeding behaviourMichael CowleyRoger ConeMalcolm LowAndrew ButlerStephen Robert BloomCaroline Jane SmallRachel Louise BatterhamMohammad Ali Ghatei
The methods include peripheral administration of a therapeutically effective amount of PYY or an agonist thereof to the subject, thereby decreasing the subject's caloric intake.MICHAEL COWLEYROGER CONEMALCOLM LOWANDREW BUTLERSTEPHEN ROBERT BLOOMCAROLINE JANE SMALL...
Stadlbauer U, Weber E, Langhans W, Meyer U (2014) The Y2 receptor agonist PYY(3-36) increases the behavioural response to novelty and acute dopaminergic drug challenge in mice. Int J Neuropsychopharmacol 17(3):407-419. https://doi.org/10.1017/ S1461145713001223...