ライフサイエンスコーパス: immucillin-H

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1 immucillins, with the exception of 5'-deoxy-immucillin-H.

2 Immucillin-H (ImmH) and Immucillin-H 5'-PO(4) (ImmHP) resemble the transition st

3 5'-Methylthio-immucillin-H, a transition state analogue inhibitor that

4 orporation into DNA and RNA was abrogated by Immucillin H, an inhibitor of human purine nucleoside ph

5 basis for M. tuberculosis PNP inhibition by immucillin-H and by its component parts is reported in t

6 Immucillin-H and DADMe-Immucillin-H are 860 and 500 pM i

7 ed with transition-state analogue inhibitors Immucillin-H and DADMe-Immucillin-H synthesized with rib

8 nthin-9-yl)-1,4-dideoxy-1,4-imino-D-ribitol (immucillin-H) and (1S)-1-(9-deazaguanin-9-yl)-1,4-dideox

9 Immucillin-H and DADMe-Immucillin-H are 860 and 500 pM inhibitors against P. fa

10 NP failed until structure-based synthesis of immucillin-H (BCX-1777, forodesine), a transition-state

11 Analysis of the components of immucillin-H confirms that the inhibition gains most of

12 mH) and 4'-deaza-1'-aza-2'-deoxy-9-methylene Immucillin-H (DADMe-ImmH) are picomolar inhibitors of hu

13 5'-Deaza-1'-aza-2'-deoxy-1'-(9-methylene)-Immucillin-H (DADMe-ImmH) is a transition-state mimic fo

14 m Treatment of human erythrocytes with DADMe-Immucillin-H (DADMe-ImmH, 22 pm) causes complete inhibit

15 cillin-H (ImmH; K(d) = 56 pM) and DATMe-ImmH-Immucillin-H (DATMe-ImmH; K(d) = 8.6 pM).

16 sition-state theory has led to the design of Immucillin-H (Imm-H), a picomolar inhibitor of purine nu

17 Immucillin-H (ImmH) and 4'-deaza-1'-aza-2'-deoxy-9-methy

18 Immucillin-H (ImmH) and immucillin-G (ImmG) were previou

19 Immucillin-H (ImmH) and Immucillin-H 5'-PO(4) (ImmHP) re

20 n complex with the transition-state analogue immucillin-H (ImmH) and inorganic phosphate was solved a

21 Immucillin-H (ImmH) has a protonated N-7 and resembles t

22 ysis of bovine PNP led to the development of immucillin-H (ImmH), a powerful inhibitor of bovine PNP

23 Asp exhibited greatly decreased affinity for Immucillin-H (ImmH), binding this mimic of an early tran

24 e T. gondii is unaffected by up to 10 microm immucillin-H (ImmH), but mutants lacking the (redundant)

25 Immucillin-H (ImmH), DADMe-ImmH, and DADMe-ImmG mimic th

26 The crystal structure of PfPNP.Immucillin-H (ImmH).SO(4) reveals a homohexamer with Imm

27 ng tightly to the transition state analogues Immucillin-H (ImmH; K(d) = 56 pM) and DATMe-ImmH-Immucil

28 Immucillin-H [ImmH; (1S)-1-(9-deazahypoxanthin-9-yl)-1,4

29 valent attachment of these two components in immucillin-H increases equilibrium binding affinity by a

30 The K(m)/K(i)* value for immucillin-H is 9000, making this inhibitor the most pow

31 Immucillin-H is a 12 nM inhibitor of TvPNP but a 56 pM i

32 Immucillin-H is a rationally designed analogue of the tr

33 Immucillin-H is a slow onset tight binding inhibitor wit

34 Immucillin-H is a transition state analogue designed to

35 Immucillin-H is an inhibitor of both huPNP and PfPNPs.

36 Immucillin-H (K*i(1/4) 58 pM, first generation)contains

37 DADMe-Immucillin-H (K*i(1/4) 9 pM, second-generation),uses a m

38 dine cation with twoasymmetric centers.DATMe-Immucillin-H (K*i(1/4)9 pM, third-generation) contains a

39 5'-Methylthio-Immucillin-H (MT-ImmH) was designed to resemble the tran

40 Moreover, TgPNP is insensitive to methylthio-immucillin-H (MT-ImmH), which inhibits PfPNP with a Ki*

41 Immucillin-H reduces the incorporation of inosine but no

42 e analogue inhibitors Immucillin-H and DADMe-Immucillin-H synthesized with ribosyl mimics of l-stereo

43 The pH dependence of the K(i) value of immucillin-H to the M. tuberculosis PNP suggests that th

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