in vitro analysis Articles
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121 - Development of Protease Proprotein Convertase Subtilisin-Like Kexin Type 9 Antagonists
Abstract Protease proprotein convertase subtilisin-like kexin type 9 (PCSK9) is an important target for the treatment of hypercholesterolemia. Several pharmaceutical companies have focused on the development of mAbs. Yet, our approach has focused on developing orally bioavailable small molecule antagonists. PCSK9 is a serine protease that is synthesized as a zymogen that undergoes autocatalytic ...
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CYP‐mediated warfarin metabolic ability is not a critical determinant of warfarin sensitivity in avian species; in vitro assays in several birds and in vivo assays in chicken
Coumarin derivative anticoagulant rodenticides used for rodent control are posing a serious risk to wild bird populations. For warfarin (WF) a classic coumarin derivative, chicken have a high LD50 while mammalian species generally have much lower LD50. Large interspecies differences in sensitivity to WF are to be expected. We previously reported substantial differences in WF metabolism among ...
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Evaluation of the scientific underpinnings for identifying estrogenic chemicals in nonmammalian taxa using mammalian test systems
The US Environmental Protection Agency has responsibility for assessing endocrine activity of more than 10 000 chemicals, a task that cannot reasonably be achieved solely through use of available mammalian and nonmammalian in vivo screening assays. Hence, it has been proposed that chemicals be prioritized for in vivo testing using data from in vitro high‐throughput assays for specific ...
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