ライフサイエンスコーパス: pregnenolone

1 zymatic products (i.e., isocaproaldehyde and pregnenolone).

2 lar to those for cholesterol conversion into pregnenolone.

3 ic factor 1, P450scc converts cholesterol to pregnenolone.

4 y for progesterone hydroxylation relative to pregnenolone.

5 450 11A1 reaction to produce the key steroid pregnenolone.

6 onsiderably lower levels of androsterone and pregnenolone.

7 HEA than toward the 17alpha-hydroxylation of pregnenolone.

8 oidogenic pathway, converting cholesterol to pregnenolone.

9 omovanillic acid, dehydroepiandrosterone, or pregnenolone.

10 ng are 2 pg for these steroids and 10 pg for pregnenolone.

11 h different affinities for dexamethasone and pregnenolone 16 alpha-carbonitrile and may explain the m

12 tional inducer and glucocorticoid antagonist pregnenolone 16 alpha-carbonitrile at 100 microM blocks

13 The inability of pregnenolone 16 alpha-carbonitrile to fully compete with

14 of CYP3A1 mediated by high concentrations of pregnenolone 16 alpha-carbonitrile.

15 s induced on treatment with dexamethasone or pregnenolone-16 alpha-carbonitrile only if consensus II

16 In female rats, dexamethasone and pregnenolone-16 alpha-carbonitrile treatment elevated ri

17 examethasone or with rifampicin but not with pregnenolone-16 alpha-carbonitrile.

18 Treatment with PXR activator pregnenolone 16alpha-carbonitrile (PCN) down-regulated t

19 Here we report that the activation of PXR by pregnenolone 16alpha-carbonitrile (PCN) in AKR/J mice ca

20 ecular target for catatoxic steroids such as pregnenolone 16alpha-carbonitrile (PCN), which induce cy

21 induction by the prototypical CYP3A inducer pregnenolone 16alpha-carbonitrile was restricted to cons

22 Notably, PXR.1 is efficaciously activated by pregnenolone 16alpha-carbonitrile, a glucocorticoid rece

23 phenobarbital (PB), Aroclor 1254, isoniazid, pregnenolone 16alpha-carbonitrile, and clofibrate) or th

24 mg/kg/day) of nicardipine, clotrimazole, or pregnenolone 16alpha-carbonitrile, but not microsomes fr

25 ,5-dichloropyridyloxy)]benzene (TCPOBOP) and pregnenolone 16alpha-carbonitrile, respectively.

26 The dexamethasone- and pregnenolone 16alpha-carbonitrile-dependent induction of

27 yridyloxy)] (TCPOBOP) but not the PXR ligand pregnenolone 16alpha-carbonitrile.

28 tment of wild-type mice with the PXR agonist pregnenolone-16alpha-carbonitrile (PCN) activated Akr1b7

29 sing isolated capillaries to the PXR ligands pregnenolone-16alpha-carbonitrile (PCN) and dexamethason

30 tment of animals with phenobarbital (PB) and pregnenolone-16alpha-carbonitrile (PCN) occurs via incre

31 ulation by the pregnane X receptor activator pregnenolone-16alpha-carbonitrile (PCN) or the Ah recept

32 Treatment of rats with pregnenolone-16alpha-carbonitrile (PCN), a ligand for th

33 control female, 19- and 20-day pregnant, and pregnenolone-16alpha-carbonitrile (PCN)-treated rats usi

34 old, asymptomatic hAPP mice over 7 days with pregnenolone-16alpha-carbonitrile to activate the nuclea

35 (3) and the catatoxic synthetic steroid PCN (pregnenolone-16alpha-carbonitrile).

36 50 inducers, including 3-methylcholanthrene, pregnenolone-16alpha-carbonitrile, and ciprofibrate.

37 In C57L mice given the PXR agonist, pregnenolone-16alpha-carbonitrile, or the herbal medicin

38 prototypic inducers such as dexamethasone or pregnenolone-16alpha-carbonitrile.

39 with deuterium-labeled substrates: 17-[(2)H]-pregnenolone; 17-[(2)H]-, 16alpha-[(2)H]-, 21,21,21-[(2)

40 and Preg, and P450 17A2 is more efficient in pregnenolone 17alpha-hydroxylation but does not catalyze

41 cytochrome P450scc (converts cholesterol to pregnenolone), 3beta-hydroxysteroid dehydrogenase (3beta

42 cytochrome P450scc (converts cholesterol to pregnenolone), 3beta-hydroxysteroid dehydrogenase (conve

43 determinations made after oral ingestion of pregnenolone and data from the literature suggest there

44 e identical for blocking DHEA formation from pregnenolone and for 17alpha-hydroxylation, suggestive o

45 ed T(H)2 CD4 T cells significantly decreased pregnenolone and IL13 mRNA and protein levels.

46 catalyzes the oxidations of progesterone and pregnenolone and is the major source of androgens.

47 of its carbon-carbon bond cleavage products, pregnenolone and isocaproaldehyde .

48 , whereas SULT2B1a preferentially sulfonates pregnenolone and only minimally sulfonates cholesterol.

49 talyses not only the 17alpha-hydroxlation of pregnenolone and progesterone and the C17,20-side chain

50 catalyzing both the 17alpha-hydroxylation of pregnenolone and progesterone and the subsequent 17alpha

51 Second, both hydroxylase substrates pregnenolone and progesterone hydrogen bond to Asn(202)

52 aboon CYP17 has apparent Km and V values for pregnenolone and progesterone of 0.9 micro m and 0.4 nmo

53 n by mediating four reactions: conversion of pregnenolone and progesterone to 17-hydroxypregnenolone

54 s 17alpha-hydroxylase activities, converting pregnenolone and progesterone to 17alpha-hydroxysteroids

55 hways; thus, Xenopus CYP17 rapidly converted pregnenolone and progesterone to dehydroepiandrosterone

56 me p450c17 (CYP17) converts the C21 steroids pregnenolone and progesterone to the C19 androgen precur

57 ated by naturally occurring steroids such as pregnenolone and progesterone, and synthetic glucocortic

58 f hydroxysteroids dehydroepiandrosterone and pregnenolone and their main metabolites in human plasma

59 Progesterone, pregnenolone, and 17alpha-OH-pregnenolone were potent in

60 NAD+ as a cofactor and oxidizes cholesterol, pregnenolone, and dehydroepiandrosterone to their respec

61 rticosterone, cortisol, deoxycorticosterone, pregnenolone, and progesterone in bovine adrenal zona gl

62 1b in the presence of the acceptor substrate pregnenolone at 2.3 A.

63 subcutaneous pellets releasing DHEA or 17-OH pregnenolone at a constant rate failed to rescue P450c17

64 cts of the endogenous ligands lipoxin A4 and pregnenolone at CB1Rs.

65 n the SULT2B1 isoforms, becomes ordered upon pregnenolone binding, covering the substrate binding poc

66 egnenolone-derivative MAP4343 (3beta-methoxy-pregnenolone) binds MAP-2 in vitro and increases its abi

67 sely, the SULT2B1a isoform avidly sulfonates pregnenolone but not cholesterol.

68 Pregnenolone but not lipoxin A4 displaced [(3)H]SR141716

69 The rat SULT2B1a isoform avidly sulfonates pregnenolone but poorly utilizes cholesterol as a substr

70 lesterol is more efficiently sulfonated than pregnenolone by the SULT2B1b isoform; on the other hand,

71 This bifunctional enzyme is responsible for pregnenolone C17 hydroxylation, followed by a 17,20-lyas

72 adducts of the bifunctional steroid "reduced pregnenolone" (containing two hydroxyl groups) and its d

73 Internal standards, pregnenolone-d4 sulfate and dehydroepiandrosterone-d2 (D

74 The synthetic pregnenolone-derivative MAP4343 (3beta-methoxy-pregnenol

75 However, we observed processivity in pregnenolone/DHEA pulse-chase experiments.

76 e of the 17alpha-OH pregnenolone formed from pregnenolone did not dissociate from P450 17A1 before co

77 along with ACAT1/ACAT2 contribute to control pregnenolone ester content in different cell types and t

78 the frontal cortex for allopregnanolone and pregnenolone following a swim stress and for allopregnan

79 vity is present, i.e. some of the 17alpha-OH pregnenolone formed from pregnenolone did not dissociate

80 pression remission rates were greater in the pregnenolone group (61%) compared with the placebo group

81 in neurosteroid levels were observed in the pregnenolone group but not in the placebo group.

82 In the pregnenolone group, baseline-to-exit change in the HRSA

83 f the neurosteroids pregnenolone sulfate and pregnenolone hemisuccinate, which potentiate NMDA recept

84 nist-stimulated conversion of cholesterol to pregnenolone (i.e., cytochrome P-450 cholesterol monooxy

85 or the intracellular catalytic production of pregnenolone, i.e. the genes and proteins for P450scc en

86 terone, testosterone, 5alpha,3alpha-THP, and pregnenolone in 1-2 ml of human cerebrospinal fluid (CSF

87 The levels of 5alpha, 3alpha-THP and pregnenolone in human CSF were higher than those of monk

88 Levels of pregnenolone in serum were reduced in parallel.

89 rial membranes, where it is metabolized into pregnenolone in steroidogenic cells.

90 e drug abiraterone and the natural substrate pregnenolone, in the CYP17 active site together with mol

91 oduction from progesterone and for DHEA from pregnenolone, indicating a distributive character of the

92 Notably, titration of b5 to CYP17A1.pregnenolone induced a set of conformational states clos

93 tochondria where cholesterol is converted to pregnenolone, initiating steroidogenesis.

94 he ability of adipocyte CYP11A1 in producing pregnenolone is demonstrated for the first time, renderi

95 of the male hormone dehydroepiandrosterone, pregnenolone is first hydroxylated by P450 CYP17A1 at th

96 Pregnenolone is formed via three sequential monooxygenat

97 M under chronic exposure conditions, whereas pregnenolone is ineffective.

98 n is stronger when the hydroxylase substrate pregnenolone is present in the CYP17A1 active site than

99 of steroidogenic tissues, the first steroid, pregnenolone, is synthesized in adrenal and gonadal tiss

100 xylase activity while in contrast 17alpha-OH-pregnenolone lyase activity was stimulated by b5.

101 The results suggest that pregnenolone may improve depressive symptoms in patients

102 on, participants were administered 400 mg of pregnenolone (n=16) or placebo (n=15) and underwent 3T f

103 rrent report, the effect of the neurosteroid pregnenolone on depressive symptoms in BPD was examined.

104 rmal pregnant females with pellets releasing pregnenolone or progesterone did not cause fetal demise.

105 Precursors of DHEA such as pregnenolone or six of its major metabolites, had no sig

106 ma tumor cells in culture biosynthesize both pregnenolone (P) and D.

107 Pregnenolone (PREG) and dehydroepiandrosterone (DHEA) ha

108 The neurosteroid pregnenolone (PREG) and its metabolites pregnenolone sul

109 ical hydroxylation of its primary substrate, pregnenolone (PREG) and then also orchestrates a remarka

110 Pregnenolone (PREG) can be converted to PREG esters (PE)

111 tion of the steroids progesterone (Prog) and pregnenolone (Preg) to glucocorticoids and androgens.

112 10 min of exposure to the steroids cortisol, pregnenolone, pregnenolone sulfate, or progesterone.

113 Recombinant His-tag StAR stimulated pregnenolone production in a dose- and time-dependent ma

114 esulted in an approximately 50% reduction in pregnenolone production.

115 ngiotensin II (5 nM)-induced aldosterone and pregnenolone production.

116 iated with psychiatric disorders and reduced pregnenolone production.

117 The pregnenolone, progesterone, and dehydroepiandrosterone c

118 by upstream CYP11A1-dependent intraturmoral pregnenolone/progesterone synthesis.

119 Wild-type MLN64 increased pregnenolone secretion in this system 2-fold.

120 The exploitation of pregnenolone steroid for benzoquinolines and terephthala

121 trates while the human enzyme favors Delta5 (pregnenolone) substrates.

122 omers of dehydroepiandrosterone sulfate (1), pregnenolone sulfate (2), and (3alpha,5beta)-3-hydroxypr

123 The ability of pregnenolone sulfate (a positive modulator) and epipregn

124 roid pregnenolone (PREG) and its metabolites pregnenolone sulfate (PregS) and allopregnanolone in ser

125 TRPM3 can be activated by the neurosteroid pregnenolone sulfate (PregS) and heat.

126 Pregnenolone sulfate (PREGS), one of the most abundantly

127 h models of the GABA-inhibitory neurosteroid pregnenolone sulfate (PREGS), suggesting common mechanis

128 ates serum levels of the neuroactive steroid pregnenolone sulfate (PregS).

129 ted by heat and chemical agonists, including pregnenolone sulfate (PS) and nifedipine (Nif).

130 Sulfated steroids like pregnenolone sulfate (PS) are found endogenously in the

131 Pregnenolone sulfate (PS) is a sulfated neurosteroid whi

132 Pregnenolone sulfate (PS) is an abundant neurosteroid th

133 Pregnenolone sulfate (PS) is an abundant neurosteroid th

134 Pregnenolone sulfate (PS) is an endogenous neurosteroid

135 The endogenous neurosteroid pregnenolone sulfate (PS) is known to enhance memory and

136 We examined the effects of the neurosteroid pregnenolone sulfate (PS) on GABA(A) receptor-mediated s

137 Here, we report that pregnenolone sulfate (PS) uses a unique mechanism for en

138 The effects of the neurosteroid pregnenolone sulfate (PS) were studied in 3- to 9-week-o

139 One of these neurosteroid, pregnenolone sulfate (PS), depends on six identified M1

140 Pregnenolone sulfate (PS), one of the most commonly occu

141 exceeds that of the canonical TRPM3 agonist, pregnenolone sulfate (PS).

142 The steroid pregnenolone sulfate activates the transcription factor

143 iously shown that the sulfated neurosteroids pregnenolone sulfate and 3alpha-hydroxy-5beta-pregnan-20

144 Sig-1R agonists such as pregnenolone sulfate and cocaine caused the dissociation

145 loreclezole, had different IC(50) values for pregnenolone sulfate and lanthanum, and were insensitive

146 sure alters the actions of the neurosteroids pregnenolone sulfate and pregnenolone hemisuccinate, whi

147 oth compounds competed with progesterone and pregnenolone sulfate and significantly reduced CatSper a

148 bserve enantioselectivity for the actions of pregnenolone sulfate and steroid sulfate 3 indicates tha

149 tsynaptic neuron depolarization, and an anti-pregnenolone sulfate antibody scavenger blocked this eff

150 The neurosteroids alphaxalone and pregnenolone sulfate appropriately modulated GABAR curre

151 l CatSper currents, whereas the neurosteroid pregnenolone sulfate exerted similar effects as progeste

152 ectrophysiological techniques, we found that pregnenolone sulfate increases the frequency of AMPA-med

153 report here that the excitatory neurosteroid pregnenolone sulfate induces a long-lasting strengthenin

154 Pregnenolone sulfate inhibited GABA-evoked currents with

155 The mechanism of action of pregnenolone sulfate involved a short-term increase in t

156 Moreover, the actions of pregnenolone sulfate on type A gamma-aminobutyric acid a

157 modulation by 3alpha5alphaP but not that by pregnenolone sulfate or beta-estradiol.

158 These results indicate that (i) pregnenolone sulfate together with progesterone are the

159 hermore, the GluN2A/B-selective potentiator (pregnenolone sulfate) and the GluN2C/D-selective potenti

160 teric potentiation of NMDA receptor pores by pregnenolone sulfate, 24(S)-hydroxycholesterol, and doco

161 s steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate, and beta-estradiol in the absence

162 ulfated and unsulfated neurosteroids such as pregnenolone sulfate, dehydroepiandrosterone sulfate (DH

163 sure to the steroids cortisol, pregnenolone, pregnenolone sulfate, or progesterone.

164 ne mediating the effects of the neurosteroid pregnenolone sulfate, or the allosteric regulatory site

165 Neurosteroids, such as pregnenolone sulfate, were previously shown to modulate

166 c-Jun-specific short hairpin RNA attenuated pregnenolone sulfate-induced AP-1 activation.

167 We conclude that pregnenolone sulfate-induced TRPM3 channel activation ch

168 This finding indicates that a pregnenolone sulfate-like neurosteroid is a previously u

169 fected the negative allosteric modulation by pregnenolone sulfate.

170 ally, testosterone antagonized the effect of pregnenolone sulfate.

171 t postulated for the inhibitory neurosteroid pregnenolone sulfate.

172 that is unique to SULT2B1a has no effect on pregnenolone sulfotransferase activity.

173 is synthesized, whereas if exon 1A is used, pregnenolone sulfotransferase is produced.

174 ivated by heat, and chemical ligands such as pregnenolone sulphate (PregS) and CIM0216.

175 een paired stimuli or between ACSF and 1 mum pregnenolone sulphate (PREGS).

176 he circulation of phosphates, which elevated pregnenolone synthesis by 2-fold by increasing the stabi

177 His-tag StAR proteins stimulated pregnenolone synthesis to the same extent as wild-type S

178 gh the intermediacy of cAMP rapidly increase pregnenolone synthesis, and this rapid steroidogenic res

179 orylation site at serine 57 had no effect on pregnenolone synthesis.

180 r, Tom22 knockdown by siRNA had no effect on pregnenolone synthesis.

181 oids (allopregnanolone, epiallopregnanolone, pregnenolone, testosterone, and dehydroepiandrosterone)

182 ive symptoms of schizophrenia with a dose of pregnenolone that elevates serum levels of the neuroacti

183 22 carbon-carbon bond of cholesterol to form pregnenolone, the first 21-carbon precursor of all stero

184 aves the side chain of cholesterol, yielding pregnenolone, the precursor of all steroid hormones.

185 er mitochondrial membrane to be converted to pregnenolone, the precursor of all steroid hormones.

186 catalyzes conversion of cholesterol (CH) to pregnenolone, the precursor to all steroid hormones.

187 n cleavage (P450scc) converts cholesterol to pregnenolone, the rate-limiting enzymatic reaction in ne

188 PD, depressed mood state, were randomized to pregnenolone (titrated to 500 mg/day) or placebo, as add

189 tein that converts dehydroepiandrosterone or pregnenolone to androstenedione or progesterone, respect

190 into mitochondria, where it is converted to pregnenolone to initiate steroidogenesis.

191 pe 2 (3betaHSD2) catalyzes the conversion of pregnenolone to progesterone and dehydroepiandrostenedio

192 osensors to improve the biotransformation of pregnenolone to progesterone in yeast and to regulate CR

193 xysteroid dehydrogenase (3beta-HSD, converts pregnenolone to progesterone), and the progesterone rece

194 3beta-hydroxysteroid dehydrogenase (converts pregnenolone to progesterone), and the progesterone rece

195 id synthesis by catalyzing the conversion of pregnenolone to progesterone, which is mediated by the i

196 droepiandrostenedione to androstenedione and pregnenolone to progesterone.

197 Pregnenolone was well tolerated.

198 24S-Hydroxysterol and pregnenolone were also present in the retina, but at muc

199 Progesterone, pregnenolone, and 17alpha-OH-pregnenolone were potent inhibitors of Delta24-reduction

200 ia from PBR-negative cells failed to produce pregnenolone when supplied with exogenous cholesterol.

201 olesterol but is also capable of sulfonating pregnenolone, whereas SULT2B1a preferentially sulfonates

202 preference for dehydroepiandrosterone versus pregnenolone with second-order rate constants (kcat/Km)

203 factor unequivocally as the nuclear receptor pregnenolone X receptor (PXR) and its human homologue, s

204 The pregnenolone X receptor (PXR), a new member of the nucle

205 t by inhibiting the activation of NRs, human pregnenolone X receptor and constitutive androstene rece

206 tor SXR/PXR (steroid and xenobiotic receptor/pregnenolone X receptor) has been shown both biochemical