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Document Page 324 This intermediate is derived by nucleophilic attack of a water molecule on the scissile-bond carbonyl. Szelke pioneered the use of reduced-bond analog (-CH 2-NH-), which were incorporated into the 6–13 peptide of angiotensinogen [12]. Cocrystallisation with endothiapepsin revealed that the reduced-bond analog associates tightly with aspartate carboxyls (32 and 215) probably via a salt link. The naturally occurring transition-state analogue statine (-CHOH-CH 2-CO-NH-) [9] is a closer analogue of the putative intermediate and has been incorporated into many inhibitors [13]. The scissile bond has also been replaced by the ketone analogue (-CO-CH 2-) [12] or by a C-terminal aldehyde group in a series of tetrapeptides [14,15]. Although these appear to mimic the substrate more closely than the intermediate, the carbonyl probably binds to the enzyme in the hydrated gem-diol form (-C(OH) 2-CH 2) [16]. Use of the hydroxyethylene analog (-CHOH-CH 2-) has led to exceptionally potent inhibitors [17] as has substitution of fluorines into ketone analogs [16,18] giving, for example, -CO-CF 2- which undergoes hydration of the carbonyl to form -C(OH) 2-CF 2- and exhibits tight binding to renin. The hydrated gemdiol is thought to closely mimic the putative transition state -C(OH) 2-NH-. All inhibitors solved in complex with aspartic proteinases by x-ray diffraction are observed to adopt similar main-chain conformations and form a conserved set of hydrogen bonds involving the inhibitor's main-chain groups interacting with enzyme moieties. The inhibitors bind in extended conformations and residues in the P 3-P 1 region form antiparallel β-sheet-like interactions with residues 217–219 on the enzyme. A β-hairpin turn formed by residues 74–78 lies between the inhibitor and bulk solvent and forms a number of generally conserved hydrogen bonds with the bound peptide. These interactions are indicated in Figure 2. The binding pockets for the inhibitor's side chains are shallow and contiguous with a greater hydrophobic character towards the central region of the active site cleft. The elaboration of several classes of transition state analog are now considered in greater detail. Statine Analogs The natural transition analog statine possesses one less main chain atom than a dipeptide and has been shown by x-ray analysis of inhibitor cocrystals to occupy the S 1 and S 1' sites of the enzyme [19]. The hydroxyl group of statine binds symmetrically between the catalytic carboxyl groups displacing a solvent molecule bound to the native enzyme. The carboxyl diad, therefore, provides a stereospecific binding site for statine and hydroxyethylene analogues with preference for the S-enantiomer. Replacement of the hydroxyl by an ammonium group might be expected to improve the potency of an inhibitor by introduction of a salt link with the enzyme. The corresponding deoxy-aminostatine (ASTA) analogs have been synthesised [20, 21] and were found to be nearly as potent as http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_324.html [4/5/2004 5:24:37 PM]
Document Figure 2 A schematic diagram of the putative hydrogen bonds formed between oligopeptide inhibitors and the fungal aspartic proteinase endothiapepsin. The latter enzyme provided a useful model system for structural studies of interactions formed by renin inhibitors with the active site cleft of aspartic proteinases prior to the determination of the human renin structure. The inhibitor is shown horizontally with enzyme groups above and below. Intervening hydrogen bonds are indicated by dashed lines. Note the extensive hydrogen-bond interactions made between the transition state analogs and the catalytic apparatus of the enzyme. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_325.html [4/5/2004 5:24:51 PM] Page 325
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Structure-based Drug Design 14 Stru
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Document Analysis of various HIV-1
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Document Page 54 Table 2) [12,54].
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Document 106. Cirino NM, Cameron CE
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Document 122. Marshall WS, Beaton G
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Document dine) and didanosine (dide
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Document 163. Lacey SF, Larder BA.
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Document Page 108 mulate during tre
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Document Table 1 Inhibition Data fo
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Document Page 166 As predicated, th
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Document References 1. Parks RE Jr.
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Document 17. Ealick SE, Rule SA, Ca
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Document 6 Structural Implications
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Page 363 and 364: Document 12 Polypeptide Modulators
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Page 413 and 414: Document 2. Blundell TL, Cooper J,
Page 415 and 416: Document 17. Szelke M. Chemistry of
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Page 421 and 422: Document Page 343 14 Structural Asp
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Document 17 Structure and Functiona
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Document Table 1 Approval Indicatio
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Document Page 438 proteins. One pot
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Document 21. Both GW, Sleigh MJ, Co
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Document Subsequent studies have sh
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Document Page 495 of the RNA and pr
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Document Figure 4 A ribbon diagram
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Document Acknowledgments Page 620 I
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Document Med Biol 1991; 306:9-21; (
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Document Page 629 ML, Clare M, Decr
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Document Cyclotheonamide A (CtA), 2
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Document D ddI, 152 tumour necrosis
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Document antistasin peptides, 281 c
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Document fragment-based programs, 5
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Document Kininogen, 119 high molecu
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Document RT inhibitor, 41, 56 Nonpe
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Document Phosphoglycerate kinase (P
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Document [Protease targets] serinyl
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