Eric Raimbaud
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View article: Estimation of Drug-Target Residence Time by Targeted Molecular Dynamics Simulations
Estimation of Drug-Target Residence Time by Targeted Molecular Dynamics Simulations Open
Drug-target residence time has emerged as a key selection factor in drug discovery since the binding duration of a drug molecule to its protein target can significantly impact its in vivo efficacy. The challenge in studying the residence t…
View article: Targeting NOX2 via p47/phox-p22/phox Inhibition with Novel Triproline Mimetics
Targeting NOX2 via p47/phox-p22/phox Inhibition with Novel Triproline Mimetics Open
On the basis of the knowledge that the proline-rich hot spot PPPRPP region of P(151)PSNPPPRPP(160), an oligopeptide derived from the cytosolic portion of p22phox (p22), binds to the single functional bis-SH3 domain of the regulatory protei…
View article: Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa)
Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa) Open
Selective and potent inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) have the potential to increase endogenous and therapeutic fibrinolysis and to behave like profibrinolytic agents without the risk of major hem…