Monday, March 23, 2009
GPCR crystallization : trick or science
The scientific community has been wondering about the know how for GPCR crystallization. It has took decades to arrive at the first structure of a GPCR: bovine rhodopsin. Though the structure was deciphered in 2000, the structure represented only an inactive form of the protein. Time took its toll and it was after another 8 years of hard work and dedication by brilliant scientists that the second structure of GPCR (the beta-2- adrenergic receptor) was published in 2008. The trick involved in introducing T4-lysozyme fused within the i3 loop of the receptor molecule to aid the stabilization of detergent solubilized receptor as well as the crystallization phenomenon. This structure also had the high affinity antagonist carazolol bound to it and thus defined the overall architecture of beta2AR and the structure of the ligand-binding pocket.
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