ライフサイエンスコーパス: NMT

1 NMT function is essential for viability in all cell type

2 ad an IC50 > 1000 microM against C. albicans NMT did not exhibit antifungal activity and produced no

3 e nonpeptidic inhibitors of Candida albicans NMT has been synthesized starting from the octapeptide A

4 and selective inhibitors of Candida albicans NMT.

5 identity (76-77%), indicating that NMT-1 and NMT-2 comprise two distinct families of N-myristoyltrans

6 Comparisons between the NMT-1 and NMT-2 proteins revealed reduced levels of sequence ident

7 Two NMT isoforms (NMT-1 and NMT-2) are expressed in mammalian cells.

8 n excellent tool for validation of T. brucei NMT as a drug target for HAT as well as a valuable lead

9 We have previously validated T. brucei NMT as a promising druggable target for the treatment of

10 ent, brain penetrant inhibitors of T. brucei NMT.

11 Comparative analyses of caffeine NMTs demonstrate that these genes expanded through seque

12 ounds 16, 17, and 18 are competitive Candida NMT inhibitors that bind to the peptide recognition site

13 nd 61a are competitive inhibitors of Candida NMT with respect to the octapeptide substrate GNAASARR-N

14 in the discovery of the most potent Candida NMT inhibitor 61a reported to date with an IC50 of 20 nM

15 Inc., Murray Hill, New Jersey), CardioSEAL (NMT Medical Inc., Boston, Massachusetts), and STARFlex (

16 Recognition of different NMT isoforms by these viral and cellular substrate prote

17 s indicated the presence of several distinct NMTs in vivo, often varying in either apparent molecular

18 These studies validate L. donovani NMT as a potential target for development of new therape

19 The open reading frame of L. donovani NMT has been amplified and used to overproduce active re

20 in novel, highly potent Leishmania donovani NMT inhibitors with good selectivity over the human enzy

21 The mouse and human versions of each NMT are highly homologous, displaying greater than 95% a

22 specific inhibition or regulation of either NMT in vivo may in turn allow for the selective control

23 Escherichia coli, having no endogenous NMT, is used for the coexpression of both the transferas

24 wever, specific details concerning VIP-ergic NMT are limited, largely because of difficulties in sele

25 onstrated that the approximately 60-kDa FLAG-NMT binds ribosomes with higher affinity than the approx

26 nsert identified a approximately 50-kDa FLAG-NMT predominantly in the cytosolic fraction.

27 affinity than the approximately 50-kDa FLAG-NMT.

28 d containing the larger insert revealed FLAG-NMT primarily in the ribosomal fraction with an apparent

29 erial dilutions of purified recombinant FLAG-NMTs demonstrated that the approximately 60-kDa FLAG-NMT

30 en optimization of compound 1 from a focused NMT inhibitor library led to the identification of two e

31 e recognition and catalysis is not known for NMTs involved in BIA metabolism.

32 zed 15 patients who were diagnosed as having NMT or MoS as a comparative group.

33 1%) from the cohort were diagnosed as having NMT.

34 pecifically immunoblotted with an anti-human NMT (hNMT) peptide antibody.

35 tion of a second, genetically distinct human NMT (hNMT-2), as well as the isolation of the respective

36 C1 contained nmt487D plus 10 copies of human NMT.

37 potency and excellent selectivity over human NMT.

38 While a single human NMT cDNA has been isolated and characterized (hNMT-1), b

39 ivity of 560- and 2200-fold versus the human NMT.

40 56 nM and 250-fold selectivity versus human NMT.

41 -purinergic, non-nitrergic (NNNP) inhibitory NMT and the role of VIP in this response.

42 ntified an ultraslow component of inhibitory NMT in the IAS mediated by VIP.

43 Two NMT isoforms (NMT-1 and NMT-2) are expressed in mammalian cells.

44 Crystal structures bound to Leishmania major NMT were obtained, and the active diastereoisomer of one

45 t functionally distinct N-methyltransferase (NMT) from opium poppy (Papaver somniferum) that primaril

46 expansions, among them N-methyltransferases (NMTs) involved in caffeine production, defense-related g

47 ionine (SAM)-dependent N-methyltransferases (NMTs) play critical roles in BIA biosynthesis, but the m

48 Moreover, NMT inhibitors effectively cure T. brucei infection in r

49 ell as the isolation of the respective mouse NMT homologue for each human enzyme.

50 ids possess a single N-myristoyltransferase (NMT) and multiple palmitoyl acyltransferases, and these

51 N-Myristoyltransferase (NMT) catalyses the attachment of the 14-carbon saturated

52 N-Myristoyltransferase (NMT) catalyzes the cotranslational acylation with myrist

53 MyristoylCoA:protein N-myristoyltransferase (NMT) covalently attaches the 14-carbon saturated fatty a

54 t and specific human N-myristoyltransferase (NMT) inhibition.

55 N-Myristoyltransferase (NMT) is a prospective drug target against parasitic prot

56 N-Myristoyltransferase (NMT) is an attractive antiprotozoan drug target.

57 N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive

58 N-Myristoyltransferase (NMT) represents a promising drug target for human Africa

59 N-Myristoyltransferase (NMT) represents a promising drug target within the paras

60 N-Myristoyltransferase (NMT) transfers myristate to an amino-terminal glycine of

61 bitors of Leishmania N-myristoyltransferase (NMT), a potential target for the treatment of leishmania

62 gn of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in P

63 zyme A (CoA):protein N-myristoyltransferase (NMT), an enzyme ubiquitous in eukaryotes that is up-regu

64 tion is catalysed by N-myristoyltransferase (NMT), an essential and druggable target in Trypanosoma c

65 an enzyme activity, N-myristoyltransferase (NMT), which transfers myristic acid from myristoyl coenz

66 yristoyl-CoA:protein N-myristoyltransferase (NMT).

67 yristoylCoA: protein N-myristoyltransferase (NMT; EC 2.1.3.97).

68 N-myristoyltransferases (NMT) catalyze co- or posttranslational myristoylation of

69 ion is catalyzed by N-myristoyltransferases (NMTs), which transfer myristate from myristoyl coenzyme

70 The Nef-NMT-1 complex is most likely a transient intermediate of

71 e copy of a conditional lethal C. neoformans NMT allele was introduced into the fungal genome by homo

72 ned a single copy of wild type C. neoformans NMT.

73 ological syndromes, including neuromyotonia (NMT), Morvan syndrome (MoS), and limbic encephalitis.

74 ; 100 mum) to block purinergic and nitrergic NMT to characterize non-purinergic, non-nitrergic (NNNP)

75 s) were mediated by purinergic and nitrergic NMT.

76 The NNNP NMT was abolished by VIP6-28 (30 mum), absent in the VIP

77 tanding substrate specificity among numerous NMTs involved in the biosynthesis of BIAs and other spec

78 on 2 devices (STARFlex [umbrella occluder] [NMT Medical, Inc., Boston, Massachusetts] and Amplatzer

79 in trypanosomatids, and genetic ablation of NMT compromises virulence.

80 on ratios >1.8, indicating an association of NMT with putative ribosomal particle(s)/subunit(s).

81 of 73a and 73b is due to the attenuation of NMT activity and that NMT represents an attractive tar

82 itory profile exhibited by this new class of NMT ligands is a function of the pKa of the imidazole su

83 omplex with the redox-active anionic form of NMT.

84 tools for the pharmacological inhibition of NMT in living cells.

85 resulted in the expression of high levels of NMT enzyme activity.

86 vity of NMTs and cross-species reactivity of NMTs without resorting to the use of radioactive isotope

87 f interest, proof of activity/selectivity of NMTs and cross-species reactivity of NMTs without resort

88 e distribution of transcripts encoding other NMTs, which occur predominantly in aerial plant organs.

89 Pavine NMT converted racemic THP to laudanosine, but the enzyme

90 this issue, the crystal structure of pavine NMT from Thalictrum flavum was solved using selenomethio

91 um falciparum (Pf) and Plasmodium vivax (Pv) NMT.

92 Inc., Boston, Massachusetts), and STARFlex (NMT Medical Inc.) closure devices for simple ASDs was pe

93 Through these studies, NMT-1 was identified as an abundant Nef-associated prote

94 to the attenuation of NMT activity and that NMT represents an attractive tar

95 Genetic experiments have established that NMT is needed to maintain the viability of Candida albic

96 Here, we provide genetic evidence that NMT is likely to be essential for viability in insect st

97 sequence identity (76-77%), indicating that NMT-1 and NMT-2 comprise two distinct families of N-myri

98 Genetic studies have shown that NMT is essential for the viability of the principal fung

99 The NMT was similar across preparations, which suggested tha

100 Comparisons between the NMT-1 and NMT-2 proteins revealed reduced levels of sequ

101 Under these conditions, the NMT was predictive of contraction duty cycle but was una

102 We examined the NMT in the cardiac system of the lobster Homarus america

103 s of potent peptidomimetic inhibitors of the NMT from one such fungal pathogen, Candida albicans.

104 trategies in the presence and absence of the NMT inhibitor DDD85646, we identified 56 proteins enrich

105 Second, we assessed the ability of the NMT to predict changes in motor output induced by the ne

106 ch preparation and the nonlinear form of the NMT.

107 and found that Gag bound preferentially the NMT-2 isoform, while Hck bound mostly to NMT-1.

108 the NMT-2 isoform, while Hck bound mostly to NMT-1.

109 This assay should be broadly applicable to NMTs from a range of organisms.

110 detected in Nmt1-/- ES cells, but the total NMT activity levels were reduced by approximately 95%, s

111 viors is called the neuromuscular transform (NMT).

112 es in inhibitory neuromuscular transmission (NMT) in the internal anal sphincter (IAS).

113 Two NMT isoforms (NMT-1 and NMT-2) are expressed in mammalia

114 racterization of a third functionally unique NMT involved in benzylisoquinoline alkaloid metabolism w

115 the loosening of a flap, which in unliganded NMT structures, occludes the protein substrate binding s

116 These data further validate NMT as an exciting drug target in malaria and support 34

117 Most of the in vitro NMT activity (60-85%) in isoosmotic cell homogenates of

118 r of both Plasmodium falciparum and P. vivax NMT and displays activity in vivo against a rodent malar

119 ul discovery of a series of Plasmodium vivax NMT inhibitors by high-throughput screening.

120 second group, 9 of 15 patients (60.0%) with NMT or MoS were male and had a median (range) age of 51

121 tructure of the hit compound in complex with NMT was obtained, allowing understanding of its novel bi

122 Conversely, patients with NMT and MoS have anti-CASPR2 antibodies only in the seru

123 erum but not in the CSF of all patients with NMT or MoS.