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A small-molecule inhibitor of protein secretion has been found that targets Cdc42, a regulator of the secretory pathway. This compound acts through a previously undescribed mechanism—by recruiting a protein inhibitor.
Ion channels have essential roles in the nervous system. An engineered ligand-gated channel with a photoactivated switch will be useful for addressing several issues in neuronal signaling.
Neurotransmitter binding to a member of the Cys-loop receptor superfamily elicits opening of an ion channel by inducing a change in the configuration of a prolyl imide bond. Engineering a series of mutant receptors to contain proline analogues with a range of cis/trans preferences demonstrates the molecular basis for channel gating.
Methylation is a key regulatory event in several biological processes. The enzymatic transfer by methyltransferases of extended carbon chain analogs of S-adenosylmethionine to DNA opens up new avenues for investigating biological methylation.
Hedgehog signaling has important and pleiotropic roles in embryonic and adult tissues. A small-molecule agonist of this pathway has been shown to act by targeting the transmembrane protein Smoothened.