Research: Structure of the Gilenya Receptor

Michael A. Hanson MA et al. Crystal Structure of a Lipid G Protein–Coupled Receptor. Science 2012: 335:851-855


You need to have studied some biology to understand this:


The lyso-phospholipid sphingosine 1-phosphate modulates lymphocyte trafficking (or movement), endothelial (blood vessel) development and integrity, heart rate, and blood vessel tone (size of  the vessel) and maturation by activating G protein–coupled sphingosine 1-phosphate receptors on cells (G-proteins are a signalling molecule that translates a signal from outside the cell into the cell).


Here, the investigators present the crystal structure of the sphingosine 1-phosphate receptor.




The identification of the structure of the SP1P1 receptor will allow more agents to be designed that could act like Gilenya, which hits SP1P1, SP1P3 SP1P4 and SP1P5 receptors. Newer and better designed drugs could reduce the side effect profile, but if the recent sudden deaths prove to be caused by Gilenya through its action on SP1P1 then it will not matter too much, as the importance of SP1P1 as a therapeutic target could be a thing of the past



Let us hope not!

Labels: