2fa3: Difference between revisions

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==Overview==

3-Hydroxy-3-methylglutaryl CoA synthase (HMGS) catalyzes the first, committed step in the mevalonate metabolic pathway for isoprenoid, biosynthesis and serves as an alternative target for cholesterol-lowering, and antibiotic drugs. We have determined a previously undescribed crystal, structure of a eukaryotic HMGS bound covalently to a potent and specific, inhibitor F-244, [(E,E)-11-[3-(hydroxymethyl)-4-oxo-2-oxytanyl]-3,5,7-trimethyl-2,4-undecad, ienenoic acid]. Given the accessibility of synthetic analogs of the F-244, natural product, this inhibited eukaryotic HMGS structure serves as a, necessary starting point for structure-based methods that may improve the, potency and species-specific selectivity of the next generation of F-244, analogs designed to target particular eukaryotic and prokaryotic HMGS.

3-Hydroxy-3-methylglutaryl CoA synthase (HMGS) catalyzes the first committed step in the mevalonate metabolic pathway for isoprenoid biosynthesis and serves as an alternative target for cholesterol-lowering and antibiotic drugs. We have determined a previously undescribed crystal structure of a eukaryotic HMGS bound covalently to a potent and specific inhibitor F-244 [(E,E)-11-[3-(hydroxymethyl)-4-oxo-2-oxytanyl]-3,5,7-trimethyl-2,4-undecad ienenoic acid]. Given the accessibility of synthetic analogs of the F-244 natural product, this inhibited eukaryotic HMGS structure serves as a necessary starting point for structure-based methods that may improve the potency and species-specific selectivity of the next generation of F-244 analogs designed to target particular eukaryotic and prokaryotic HMGS.

==About this Structure==

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[[Category: Brassica juncea]]

[[Category: Single protein]]

[[Category: Ferrer, J.L.]]

[[Category: Ferrer, J L.]]

[[Category: Noel, J.P.]]

[[Category: Noel, J P.]]

[[Category: Pojer, F.]]

[[Category: Richard, S.B.]]

[[Category: Richard, S B.]]

[[Category: ACO]]

[[Category: acetyl-coa]]

[[Category: hmgs1]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Tue Jan 29~~ 19:~~31:42~~ 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:19:17 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
--Hydroxy-3-methylglutaryl CoA synthase (HMGS) catalyzes the first, committed step in the mevalonate metabolic pathway for isoprenoid, biosynthesis and serves as an alternative target for cholesterol-lowering, and antibiotic drugs. We have determined a previously undescribed crystal, structure of a eukaryotic HMGS bound covalently to a potent and specific, inhibitor F-244, [(E,E)-11-[3-(hydroxymethyl)-4-oxo-2-oxytanyl]-3,5,7-trimethyl-2,4-undecad, ienenoic acid]. Given the accessibility of synthetic analogs of the F-244, natural product, this inhibited eukaryotic HMGS structure serves as a, necessary starting point for structure-based methods that may improve the, potency and species-specific selectivity of the next generation of F-244, analogs designed to target particular eukaryotic and prokaryotic HMGS.
+-Hydroxy-3-methylglutaryl CoA synthase (HMGS) catalyzes the first committed step in the mevalonate metabolic pathway for isoprenoid biosynthesis and serves as an alternative target for cholesterol-lowering and antibiotic drugs. We have determined a previously undescribed crystal structure of a eukaryotic HMGS bound covalently to a potent and specific inhibitor F-244 [(E,E)-11-[3-(hydroxymethyl)-4-oxo-2-oxytanyl]-3,5,7-trimethyl-2,4-undecad ienenoic acid]. Given the accessibility of synthetic analogs of the F-244 natural product, this inhibited eukaryotic HMGS structure serves as a necessary starting point for structure-based methods that may improve the potency and species-specific selectivity of the next generation of F-244 analogs designed to target particular eukaryotic and prokaryotic HMGS.
 ==About this Structure==
@@ Line 13: / Line 13: @@
 [[Category: Brassica juncea]]
 [[Category: Single protein]]
-[[Category: Ferrer, J.L.]]
+[[Category: Ferrer, J L.]]
-[[Category: Noel, J.P.]]
+[[Category: Noel, J P.]]
 [[Category: Pojer, F.]]
-[[Category: Richard, S.B.]]
+[[Category: Richard, S B.]]
 [[Category: ACO]]
 [[Category: acetyl-coa]]
 [[Category: hmgs1]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jan 29 19:31:42 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:19:17 2008''