LP-922056 is an orally active, potent and selective NOTUM pectinacetylesterase inhibitor that activates Wnt signaling. LP-922056 stimulates endocortical bone formation in rodents and in humanized NOTUM mouse line.
orally active, potent and selective NOTUM pectinacetylesterase inhibitor that activates Wnt signaling and stimulates bone formation
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A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.
The disability, mortality and costs caused by non-vertebral osteoporotic fractures are enormous. Existing osteoporosis therapies are highly effective at reducing vertebral but not non-vertebral fractures. Cortical bone is a major determinant of non-vertebral bone strength. To identify novel osteoporosis drug
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