ライフサイエンスコーパス: bioactivation

1 ediated toxicity, drug interactions, and low bioactivation.

2 derivatives can act as substrates for CYP1A1 bioactivation.

3 s renal phosphate reabsorption and vitamin D bioactivation.

4 ue hypoxia, hemoglobin allostery and nitrite bioactivation.

5 impact via its ability to inhibit carcinogen bioactivation.

6 ol as well as acivicin, an inhibitor of GSNO bioactivation.

7 ugh enhanced polycyclic aromatic hydrocarbon bioactivation.

8 not related to greater extents of carcinogen bioactivation.

9 ces CYP2B6, a key enzyme responsible for CPA bioactivation.

10 hip between prodrugs and cell line-dependent bioactivation.

11 ne methide mechanism involving metal or haem bioactivation.

12 on as a nitrite reductase, abolishes nitrite bioactivation.

13 racellular ATP without interfering with APAP bioactivation.

14 indicating that the drug interfered with GTN bioactivation.

15 ed chemotherapy by selectively promoting its bioactivation.

16 peutic AM without the need for P450-mediated bioactivation.

17 medicinal chemists when attempting to avoid bioactivation.

18 pired by the mechanisms underlying cisplatin bioactivation.

19 uman liver 3A enzymes in AFB1 metabolism and bioactivation, a combination of approaches including seq

20 The combined data suggest that the extent of bioactivation across P450 enzymes does not correlate wit

21 In vitro studies indicated that the NA bioactivation activities in OM and lung of the CYP2A13/2

22 potential contributing roles of AOR-mediated bioactivation and adduct stability to the cytotoxicity o

23 rug-related risk factors include metabolism, bioactivation and covalent binding, and the inhibition o

24 ehydrogenase (XO/XDH) also contribute to the bioactivation and cytotoxicity of RH1 in human tumor cel

25 The balance between bioactivation and degradation of 1,25-dihydroxyvitamin D

26 ic metabolism is complex, and accounting for bioactivation and detoxification processes of chemicals

27 d liver injury (AILI) without affecting APAP bioactivation and detoxification.

28 small family of selenoenzymes catalyzing the bioactivation and disposal of thyroid hormone.

29 vitro, was used to explore the potential for bioactivation and enzyme inactivation of additional P450

30 P) gene family catalyzes drug metabolism and bioactivation and is therefore relevant to drug developm

31 dence for the essential role of ALDH2 in GTN bioactivation and may have implications to other fields

32 in vivo function of CYP2A13 and CYP2F1 in NA bioactivation and NA-induced respiratory tract toxicity

33 Rates of microsomal NA bioactivation and the effects of an anti-CYP2A antibody

34 e hepatocyte clock dramatically reduces APAP bioactivation and toxicity in vivo and in vitro because

35 ell cycle progression, apoptosis, carcinogen bioactivation, and DNA repair.

36 e thiol (S-nitrosothiol, SNO) that subserves bioactivation, and in transfer of the NO moiety from S-n

37 rated that isoquine does not undergo in vivo bioactivation, as evidenced by the complete lack of glut

38 ian cells may not be due solely to decreased bioactivation, as has been hypothesized previously, but

39 Bioactivation assays using LNCaP cytosols showed that en

40 Whilst bioactivation at the carboxylate group is widely hypothe

41 sted except CYP2E1 was capable of raloxifene bioactivation, based on glutathione adduct formation.

42 nic anhydrase) results in diminished nitrite bioactivation, but the role of carbonic anhydrase is abr

43 ne diethyl ester, bypasses the need for GSNO bioactivation by gamma-glutamyl transpeptidase to increa

44 hly cytotoxic dialkynylcarbinols, involves a bioactivation by HSD17B11, a short-chain dehydrogenase/r

45 oxide synthase at the remote site or nitrite bioactivation by myoglobin within the target organ abrog

46 and immunotoxic effects, as a consequence of bioactivation by P-450 cytochromes to dihydrodiol epoxid

47 tathione S-transferase (GST) conjugation and bioactivation by renal cysteine beta-lyase (CCBL1).

48 properties of redox status and intracellular bioactivation can be leveraged by rational combinatorial

49 the deconvolution of key steps in the Cyt1Aa bioactivation cascade.

50 tracellular role of this enzyme in mitomycin bioactivation, Chinese hamster ovary cell transfectants

51 However, their biotransformation capability (bioactivation/detoxification processes) is rarely report

52 mechanism of CPR-CP-mediated organic nitrate bioactivation, EPR, chemiluminescence NO analyzer, NO el

53 he oxazaphosphorine ring to avoid cytochrome bioactivation favoring the release of the active entity

54 (CP) play important roles in organic nitrate bioactivation; however, the mechanism by which they conv

55 eventive strategies is whether procarcinogen bioactivation in an extrahepatic target tissue (e.g., th

56 nhibited CYP1A1-mediated benzo(a)pyrene diol bioactivation in both oral SCC cells and intact oral muc

57 tance in endogenous metabolism and herbicide bioactivation in crops and weeds discussed.

58 erstand the mechanisms of heterocyclic amine bioactivation in humans, the most mass abundant heterocy

59 the principal enzymatic determinants of RH1 bioactivation in MDA468 tumor cells and that b5R, P450R,

60 ivins, that undergo cytochrome-p450-mediated bioactivation in nematodes.

61 ifen-metabolizing enzymes suggests tamoxifen bioactivation in the endometrial vasculature in vivo.

62 Following bioactivation in the liver, N-hydroxyaristolactam and N-

63 oavailability, consistent with decreased NNK bioactivation in the lung.

64 modified hydroxamate moieties are subject to bioactivation in vitro.

65 ormation is necessary and sufficient for GTN bioactivation in VSMC.

66 Carboxylate bioactivation into reactive metabolites (e.g., acyl gluc

67 n the wide range of cellular targets, but if bioactivation is insufficient in vivo, it may also help

68 culating and tissue storage form of NO whose bioactivation is mediated by the enzymatic action of xan

69 etween the groups, suggesting that increased bioactivation is not the mechanism for this amplified to

70 The final step in the proposed bioactivation is the formation of a platinum-cysteine S-

71 itumor prodrugs that require cytochrome P450 bioactivation leading to 4-hydroxy derivatives.

72 Combination oncolysis and prodrug bioactivation leads to significant prolongation of survi

73 sis coupled with an in vitro assay to assess bioactivation led to replacement of the fluoroquinazolin

74 cytotoxicity (IC(50) value and biomarker of bioactivation levels, respectively: 10beta-(p-fluorophen

75 ssion through WhiB7, creating a feed-forward bioactivation loop, which increases FF-ac accumulation a

76 suggested that thiol-dependent nonenzymatic bioactivation may be responsible for the superior antitu

77 hin the designed glutathione-induced prodrug bioactivation mechanism (Scheme 9).

78 f imidazo[3.2-b]pyrazoles, we elucidated the bioactivation mechanism causing CYP3A4/5 time-dependent

79 gue dihydro-2-pyridone 1 maintains a similar bioactivation mechanism concluding with covalent labelin

80 upport for a cytochrome P450 (P450)-mediated bioactivation mechanism involving the initial formation

81 employ the newly discovered reaction in the bioactivation mechanism.

82 otherapeutic prodrugs that undergoes hepatic bioactivation mediated predominantly by cytochrome P450

83 Consistent with hypoxia-dependent nitrite bioactivation, nitrite was reduced to NO, S-nitrosothiol

84 f FpD, with greater cell kill occurring when bioactivation occurs in the proximity of its target, nuc

85 Bioactivation occurs through the sequential actions of c

86 Denitration and bioactivation of 1-2 microM GTN, assayed as 1,2-glycerol

87 he cytochrome P450 responsible for metabolic bioactivation of 3-MI.

88 In contrast, HSV1yCD-mediated bioactivation of another prodrug, ganciclovir, impairs v

89 in, suggesting that heparin did not diminish bioactivation of APAP.

90 and has multifunctional properties including bioactivation of arachidonic acid to epoxyeicosatrienoic

91 Results suggest that bioactivation of ArNH(2) follows the anionic pathway.

92 we will present contemporary examples of the bioactivation of atypical structures usually regarded as

93 esults reveal a mechanism by which metabolic bioactivation of B[a]P may mediate RyR dysfunction of pa

94 wever, it has not yet been described for the bioactivation of BaP-7,8-diol.

95 nelucidated, cytochrome P450 enzyme-mediated bioactivation of BBR to electrophilic reactive metabolit

96 Although the bioactivation of benzbromarone (BBR) to reactive metabol

97 table to individual differences in enzymatic bioactivation of benzo(a)pyrene.

98 ated to estimate relative rates of genotoxic bioactivation of benzo[a]pyrene (BP) for several differe

99 showed 3-fold higher activity for genotoxic bioactivation of BP than myoglobin.

100 ine can provide useful information about the bioactivation of chemical carcinogens and can be used to

101 at could be therapeutically exploited in the bioactivation of chemotherapeutic prodrugs through desig

102 hypothesis that mitAspAT plays a role in the bioactivation of cisplatin.

103 (CYP1As) are involved in detoxification and bioactivation of common environmental pollutants.

104 Bioactivation of curcumin occurred readily in vitro, whi

105 erivatives has been synthesized to study the bioactivation of cytotoxic fatty acids by the mitochondr

106 -CoA hydratase is an important enzyme in the bioactivation of DCTFTH-CoA, in a pathway which does not

107 ich has implications for chemoprotection and bioactivation of DNA-damaging antitumor agents.

108 1) is implicated in both chemoprevention and bioactivation of DNA-damaging antitumor agents.

109 generated endogenously, or via the metabolic bioactivation of drugs and other environmental chemicals

110 posed as an early unifying event linking the bioactivation of drugs to hepatotoxicity and as a more d

111 a very important role in the metabolism and bioactivation of drugs, carcinogens, and other xenobioti

112 derivative of the proposed intermediate from bioactivation of FK317 that is responsible for DNA cross

113 ons that are still unresolved, mitochondrial bioactivation of GTN in blood vessels is still lacking e

114 n the present study, we investigated whether bioactivation of GTN is affected by the subcellular loca

115 The data indicate that vascular bioactivation of GTN is catalyzed by cytosolic ALDH2.

116 Bioactivation of halothane occurred similarly in all thr

117 many procarcinogens, serve as a mechanism of bioactivation of HONH-AalphaC.

118 on is dependent on thrombospondin-1-mediated bioactivation of latent TGF-beta.

119 ve a more important role than CYP 3A4 in the bioactivation of low AFB(1) concentrations associated wi

120 of cytochrome P450s that may be involved in bioactivation of malathion.

121 Metabolic bioactivation of many different chemicals results in the

122 ired post-translational modification for the bioactivation of many neuropeptides, entails sequential

123 icrosomal P450 enzymes, is essential for the bioactivation of many procarcinogens.

124 ue among members of this superfamily because bioactivation of MIS via proteolytic processing is hypot

125 an cells results in efficient processing and bioactivation of MIS.

126 suggesting that NQO1 may play a role in the bioactivation of mitomycin C in these tumors.

127 ylpyridine (MPP+) which is formed during the bioactivation of MPTP by monoamine oxidase B.

128 is enzyme is also of great importance in the bioactivation of mutagens, including the N-hydroxylation

129 The bioactivation of nitrate involves its active accumulatio

130 the central importance of host microbiota in bioactivation of nitrate.

131 he vasodilator properties and mechanisms for bioactivation of nitrite in the human forearm.

132 dehyde dehydrogenase-2 (ALDH2) catalyzes the bioactivation of nitroglycerin (glyceryl trinitrate, GTN

133 els, which requires O2-regulated binding and bioactivation of NO by Hb and transfer of NO equivalents

134 ategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][

135 nstrate that the rate-limiting enzyme in the bioactivation of peptide messengers is differentially re

136 e to gain a mechanistic understanding of the bioactivation of plant secondary metabolites by the huma

137 The bioactivation of polycyclic aromatic hydrocarbons (PAHs)

138 Cytochrome P4501B1 is highly active in the bioactivation of polycyclic aromatic hydrocarbons (PAHs)

139 human skin will probably result in enhanced bioactivation of polycyclic aromatic hydrocarbons and ot

140 The bioactivation of procarcinogens by cytochrome P450 2W1 m

141 d factors that determine the tissue-specific bioactivation of ProTide prodrugs by comparing the dispo

142 D(P)H:quinone oxidoreductase 1 (NQO1) in the bioactivation of quinone prodrugs has been shown through

143 p78/AMFR knockout can enhance P450-dependent bioactivation of relevant cancer chemotherapeutic prodru

144 mes have shown that SULT1A2 can catalyze the bioactivation of several procarcinogens, indicating a po

145 le in the processes of detoxification and/or bioactivation of specific pharmaceuticals and xenobiotic

146 Bioactivation of styrene to its metabolite styrene oxide

147 When bioactivation of substrates in the films gives reactive

148 oxia (1% O(2)) increases gene expression and bioactivation of TGF-beta2 and induces its downstream ef

149 cating that an autocrine mechanism driven by bioactivation of TGF-beta2 leads to its gene expression

150 e dehydrogenase-2 (ALDH2) catalyzes vascular bioactivation of the antianginal drug nitroglycerin (GTN

151 e dehydrogenase-2 (ALDH2) catalyzes vascular bioactivation of the antianginal drug nitroglycerin (GTN

152 and to the associated regional shift in the bioactivation of the APAP challenge dose from centrilobu

153 gamma binding potency was observed following bioactivation of the dust using rat hepatic S9 fractions

154 vitro biotransformation which will result in bioactivation of the lipophilic compounds into THD hydro

155 :cytochrome b5 reductase in the differential bioactivation of the mitomycins and indicate that the su

156 enerated by the mitomycins, we proposed that bioactivation of the mitomycins in the nucleus close to

157 osylceramide synthase (GCS), responsible for bioactivation of the proapoptotic mediator ceramide to a

158 the rat CYP2B1 transgene responsible for the bioactivation of the prodrugs, cyclophosphamide and ifos

159 It was expected that the bioactivation of these prodrugs would initiate a cascade

160 oforms of NOS [inducible NOS (NOSII)] in the bioactivation of this DNA-damaging antitumor agent.

161 II iodothyronine 5'-deiodinase catalyzes the bioactivation of thyroid hormone in the brain.

162 e or more of the enzymes responsible for the bioactivation of TPZ is/are thought to be at or near the

163 Bioactivation of vitamin D consists of two sequential hy

164 al processes, including: 1) deactivation and bioactivation of xenobiotics, 2) inactivation of hormone

165 gh CYP3A4-dependent pathways involved in RTV bioactivation, oxidative stress, and endoplasmic reticul

166 ite identification studies revealed a latent bioactivation pathway associated with 4.

167 d in the cytidine transport, metabolism, and bioactivation pathway contribute to this variation in re

168 orm 5,6-EET-EA represents an endocannabinoid bioactivation pathway in the context of immune cell func

169 e, robust, and a powerful tool for assessing bioactivation potential.

170 ction products, including oxidants, and this bioactivation process is essential for vasodilation.

171 njugates constitutes an integral part of the bioactivation processes for clopidogrel.

172 In the case of ifosfamide (IFO), the bioactivation produces two toxic metabolites: acrolein,

173 Systematic exploration of their bioactivation profile revealed that glucose-based prodru

174 a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 inducti

175 mes and CYP1A2 supersomes showed the highest bioactivation rate for adduct formation, in which all fo

176 specifically tested 3 proposed mechanisms of bioactivation: reduction to nitric oxide by xanthine oxi

177 ofactor, etc.), chemical reaction mechanism, bioactivation requirements, key references, and reversib

178 This shift in APAP bioactivation results in less-intense covalent binding t

179 n D 25-hydroxylase responsible for the first bioactivation step.

180 ystem led to modulation of reactivity toward bioactivation, studied by HPLC-MS/MS analysis of reactio

181 y player in the control of second-line drugs bioactivation such as ethionamide and has been shown to

182 that NQO2 may be particularly relevant as a bioactivation system for RH1 in NQO1-deficient tumors su

183 expression and place toxicant and carcinogen bioactivation systems in overdrive?

184 cid promoieties offered the benefit of rapid bioactivation that translated into low circulating level

185 Through sequential enzymatic bioactivation, the Tyr-Lys dipeptide is released in a su

186 iency of vitamin D, genetic disorders of its bioactivation to 1,25-dihydroxyvitamin D [1,25(OH)2D], o

187 Clozapine undergoes bioactivation to a chemically reactive nitrenium ion, wh

188 yclic amine found in cooked meats, undergoes bioactivation to a nitrenium ion, which alkylates guanin

189 (3) Does my compound undergo bioactivation to a reactive metabolite?

190 AalphaC undergoes bioactivation to form electrophilic N-oxidized metabolit

191 Lysosomal accumulation and bioactivation to generate reactive quinoneimine metaboli

192 and other heterocyclic arylamines and their bioactivation to mutagens.

193 s observed to correlate with thiol-dependent bioactivation to produce NO(2)(-), but not with depletio

194 , in certain instances, sulfation results in bioactivation to reactive electrophilic or therapeutical

195 O1) demonstrated that beta-lap requires NQO1 bioactivation to regulate the cellular metabolism of PP-

196 )H:quinone oxidoreductase 1 (NQO1) metabolic bioactivation, triggering a massive induction of reactiv

197 We conclude that the paradigm of metabolic bioactivation uncovered here should be considered for th

198 d GAPDH, enzymes implicated in nitroglycerin bioactivation via an E-Cys-NO(2) intermediate, catalyze

199 ently a proherbicide that requires metabolic bioactivation via cleavage of the benzyl-ether side chai

200 family that have been implicated in hormone bioactivation via proteolytic processing after dibasic a

201 edicinal chemistry strategies used to derisk bioactivation will be discussed, and an emphasis will be