AI Article Synopsis
- Ortho-biphenyl carboxamides were initially developed to inhibit a protein involved in fat transfer (MTP), but have since been discovered to also inhibit the Hedgehog signaling pathway.
- Research on these compounds showed that modifying their structure reduced their effectiveness as MTP inhibitors while enhancing their activity as Hedgehog inhibitors, achieving effectiveness in very low concentrations.
- Binding tests indicated that these compounds work by blocking the Smoothened receptor, and they are effective in both human and mouse models.
Article Abstract
Ortho-biphenyl carboxamides, originally prepared as inhibitors of microsomal triglyceride transfer protein (MTP) have been identified as novel inhibitors of the Hedgehog signaling pathway. Structure-activity relationship studies for this class of compounds reduced MTP inhibitory activity and led to low nanomolar Hedgehog inhibitors. Binding assays revealed that the compounds act as antagonists of Smoothened and show cross-reactivity for both the human and mouse receptor.
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| http://dx.doi.org/10.1016/j.bmcl.2008.11.096 | DOI Listing |
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