Article
Variants of human thymidylate synthase with loop 181-197 stabilized in the inactive conformation.
Protein science : a publication of the Protein Society - 1 Aug 2009
Lovelace Leslie L, Johnson Saphronia R, Gibson Lydia M, Bell Brittnaie J, Berger Sondra H, Lebioda Lukasz
Abstract excerpt
Loop 181-197 of human thymidylate synthase (hTS) populates two major conformations, essentially corresponding to the loop flipped by 180 degrees . In one of the conformations, the catalytic Cys195 residue lies distant from the active site making the enzyme inactive. Ligands stabilizing this inactive conformation may function as allosteric inhibitors. To facilitate the search for such inhibitors, we have expressed...
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