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The second important site in this helix is K288 4.64b , which, when mutated to Ala or Leu in rat GLP-1R, respectively, resulted in a 79- and 63-fold reduction in affinity with a 251- and 79-fold lower potency (Al-Sabah and Donnelly, 2003b)
Structural Dynamics of DPP-4 and Its Influence on the Projection of Bioactive Ligands
Participants who followed the full escalation schedule tolerated the compound significantly better than those in earlier trials where escalation was faster
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