Transition state analysis and inhibitor design for enzymatic reactions
نویسندگان
چکیده
منابع مشابه
Transition state analysis of model and enzymatic prenylation reactions.
Protein prenylation involves the attachment of C15 (farnesyl) or C20 (geranylgeranyl) groups to proteins and is catalyzed by a class of enzymes known as prenyltransferases.1 The observation that inhibition of Ras farnesylation arrests the growth of tumor cells has been the motivating factor in developing inhibitors of prenyltransferases that can serve as anticancer drugs; currently, several can...
متن کاملEnzymatic transition state theory and transition state analogue design.
The incredible catalytic rate enhancements caused by enzymes led Linus Pauling (1) to suggest that enzymes bind tightly to substrates distorted toward the transition state, thereby concentrating them and enforcing catalysis. Wolfenden (2) explained that chemically stable analogues that resemble the transition state would be expected to bind more tightly than substrate by factors resembling the ...
متن کاملEnzymatic transition states and transition state analog design.
All chemical transformations pass through an unstable structure called the transition state, which is poised between the chemical structures of the substrates and products. The transition states for chemical reactions are proposed to have lifetimes near 10(-13) sec, the time for a single bond vibration. No physical or spectroscopic method is available to directly observe the structure of the tr...
متن کاملEnzymatic transition states and transition state analogues.
Transition states are the balance point of catalysis. Bonds are partially made and/or broken at the transition state, and the energy of the extended system provides near-equal probability that the system forms products or reverts to reactants. Enzymatic catalytic sites provide dynamic electronic environments that increase the probability that the transition state will be formed. Alignment of re...
متن کاملGround State and Transition State Contributions to the Rates of Intramolecular and Enzymatic Reactions
reactions, rate enhancements of 108 M have been observed (Table 1).2 Intramolecular reactions where severe ground state strain is relieved upon formation of the transition state are known to be as large as 1016 M.3 Kirby4 has compiled a compendium of intramolecular reactions and has pointed out the relationship of rate to exothermicity. The importance of ground state conformations and the lack ...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1994
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(17)32294-9