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1 zymatic products (i.e., isocaproaldehyde and pregnenolone).
2 omovanillic acid, dehydroepiandrosterone, or pregnenolone.
3 ng are 2 pg for these steroids and 10 pg for pregnenolone.
4 lar to those for cholesterol conversion into pregnenolone.
5 lasmic linker protein 170 in the presence of pregnenolone.
6 ic factor 1, P450scc converts cholesterol to pregnenolone.
7 y for progesterone hydroxylation relative to pregnenolone.
8 onsiderably lower levels of androsterone and pregnenolone.
9 progesterone and dehydroepiandrosterone from pregnenolone.
10 re analyzed for sulfating activities towards pregnenolone.
11 yosis, displayed low activity (1-10%) toward pregnenolone.
12 n reported to be highly selective to sulfate pregnenolone.
13 H) and 20R,22R-(OH)(2) cholesterol, yielding pregnenolone.
14 activity of coded SULT2B1a allozymes toward Pregnenolone.
15 HEA than toward the 17alpha-hydroxylation of pregnenolone.
16 450 11A1 reaction to produce the key steroid pregnenolone.
17 onversion of lysosome-derived cholesterol to pregnenolone.
18 oidogenic pathway, converting cholesterol to pregnenolone.
20 h different affinities for dexamethasone and pregnenolone 16 alpha-carbonitrile and may explain the m
21 tional inducer and glucocorticoid antagonist pregnenolone 16 alpha-carbonitrile at 100 microM blocks
24 s induced on treatment with dexamethasone or pregnenolone-16 alpha-carbonitrile only if consensus II
28 Here we report that the activation of PXR by pregnenolone 16alpha-carbonitrile (PCN) in AKR/J mice ca
29 targeting the PXR, we activated the PXR with pregnenolone 16alpha-carbonitrile (PCN) in wild-type mic
30 ound to be induced in response to PXR ligand pregnenolone 16alpha-carbonitrile (PCN) treatment in mou
31 ecular target for catatoxic steroids such as pregnenolone 16alpha-carbonitrile (PCN), which induce cy
32 rongly induced by PB and modestly induced by pregnenolone 16alpha-carbonitrile in the RR strain but n
33 induction by the prototypical CYP3A inducer pregnenolone 16alpha-carbonitrile was restricted to cons
34 Notably, PXR.1 is efficaciously activated by pregnenolone 16alpha-carbonitrile, a glucocorticoid rece
35 phenobarbital (PB), Aroclor 1254, isoniazid, pregnenolone 16alpha-carbonitrile, and clofibrate) or th
36 mg/kg/day) of nicardipine, clotrimazole, or pregnenolone 16alpha-carbonitrile, but not microsomes fr
40 tment of wild-type mice with the PXR agonist pregnenolone-16alpha-carbonitrile (PCN) activated Akr1b7
41 sing isolated capillaries to the PXR ligands pregnenolone-16alpha-carbonitrile (PCN) and dexamethason
42 3a gene was induced using the mPXR activator pregnenolone-16alpha-carbonitrile (PCN) and was subseque
43 tment of animals with phenobarbital (PB) and pregnenolone-16alpha-carbonitrile (PCN) occurs via incre
44 ulation by the pregnane X receptor activator pregnenolone-16alpha-carbonitrile (PCN) or the Ah recept
46 control female, 19- and 20-day pregnant, and pregnenolone-16alpha-carbonitrile (PCN)-treated rats usi
47 old, asymptomatic hAPP mice over 7 days with pregnenolone-16alpha-carbonitrile to activate the nuclea
49 50 inducers, including 3-methylcholanthrene, pregnenolone-16alpha-carbonitrile, and ciprofibrate.
52 with deuterium-labeled substrates: 17-[(2)H]-pregnenolone; 17-[(2)H]-, 16alpha-[(2)H]-, 21,21,21-[(2)
53 and Preg, and P450 17A2 is more efficient in pregnenolone 17alpha-hydroxylation but does not catalyze
54 cytochrome P450scc (converts cholesterol to pregnenolone), 3beta-hydroxysteroid dehydrogenase (3beta
55 cytochrome P450scc (converts cholesterol to pregnenolone), 3beta-hydroxysteroid dehydrogenase (conve
56 at week 6 were associated with higher 17-OH-pregnenolone (7.78 vs 3.71 ng/mL, P = .0004) and lower t
57 iple species, streamlining the conversion of pregnenolone, a 3beta-hydroxy-5-ene and steroid hormone
60 progesterone on sperm release was specific; pregnenolone and 17alpha-OH-progesterone did not affect
61 determinations made after oral ingestion of pregnenolone and data from the literature suggest there
62 e identical for blocking DHEA formation from pregnenolone and for 17alpha-hydroxylation, suggestive o
68 , whereas SULT2B1a preferentially sulfonates pregnenolone and only minimally sulfonates cholesterol.
69 talyses not only the 17alpha-hydroxlation of pregnenolone and progesterone and the C17,20-side chain
70 catalyzing both the 17alpha-hydroxylation of pregnenolone and progesterone and the subsequent 17alpha
72 aboon CYP17 has apparent Km and V values for pregnenolone and progesterone of 0.9 micro m and 0.4 nmo
73 n by mediating four reactions: conversion of pregnenolone and progesterone to 17-hydroxypregnenolone
74 s 17alpha-hydroxylase activities, converting pregnenolone and progesterone to 17alpha-hydroxysteroids
75 hways; thus, Xenopus CYP17 rapidly converted pregnenolone and progesterone to dehydroepiandrosterone
76 me p450c17 (CYP17) converts the C21 steroids pregnenolone and progesterone to the C19 androgen precur
77 ated by naturally occurring steroids such as pregnenolone and progesterone, and synthetic glucocortic
78 ntal data reveal novel nongenomic targets of pregnenolone and provide important leads to understand i
79 f hydroxysteroids dehydroepiandrosterone and pregnenolone and their main metabolites in human plasma
81 NAD+ as a cofactor and oxidizes cholesterol, pregnenolone, and dehydroepiandrosterone to their respec
83 h cholesterol side-chain cleavage, producing pregnenolone, and hydroxylation of vitamin D3, producing
84 rticosterone, cortisol, deoxycorticosterone, pregnenolone, and progesterone in bovine adrenal zona gl
85 es the 17a-hydroxylation of progesterone and pregnenolone as well as the subsequent lyase cleavage of
88 subcutaneous pellets releasing DHEA or 17-OH pregnenolone at a constant rate failed to rescue P450c17
91 n the SULT2B1 isoforms, becomes ordered upon pregnenolone binding, covering the substrate binding poc
92 egnenolone-derivative MAP4343 (3beta-methoxy-pregnenolone) binds MAP-2 in vitro and increases its abi
95 The rat SULT2B1a isoform avidly sulfonates pregnenolone but poorly utilizes cholesterol as a substr
96 isms of the SULT2B1 gene on the sulfation of pregnenolone by SULT2B1a allozymes, 13 recombinant SULT2
98 lesterol is more efficiently sulfonated than pregnenolone by the SULT2B1b isoform; on the other hand,
99 This bifunctional enzyme is responsible for pregnenolone C17 hydroxylation, followed by a 17,20-lyas
100 adducts of the bifunctional steroid "reduced pregnenolone" (containing two hydroxyl groups) and its d
101 me (SCC or CYP11A1) catalyzes cholesterol to pregnenolone conversion, although its mechanism of actio
105 We found that human glial cells produced pregnenolone, detectable by mass spectrometry and ELISA,
107 e of the 17alpha-OH pregnenolone formed from pregnenolone did not dissociate from P450 17A1 before co
108 along with ACAT1/ACAT2 contribute to control pregnenolone ester content in different cell types and t
109 as the precursor for other steroid hormones, pregnenolone exerts its own effect as an anti-inflammato
110 the frontal cortex for allopregnanolone and pregnenolone following a swim stress and for allopregnan
111 absence of nonionic detergents, and assayed pregnenolone formation by HPLC-mass spectrometry of the
112 vity is present, i.e. some of the 17alpha-OH pregnenolone formed from pregnenolone did not dissociate
113 pression remission rates were greater in the pregnenolone group (61%) compared with the placebo group
118 The neurosteroid and major steroid precursor pregnenolone has therapeutical potential in various dise
119 f the neurosteroids pregnenolone sulfate and pregnenolone hemisuccinate, which potentiate NMDA recept
120 nist-stimulated conversion of cholesterol to pregnenolone (i.e., cytochrome P-450 cholesterol monooxy
121 or the intracellular catalytic production of pregnenolone, i.e. the genes and proteins for P450scc en
122 terone, testosterone, 5alpha,3alpha-THP, and pregnenolone in 1-2 ml of human cerebrospinal fluid (CSF
124 of genetic polymorphism on the sulfation of pregnenolone in individuals with different SULT2B1 genot
127 e drug abiraterone and the natural substrate pregnenolone, in the CYP17 active site together with mol
128 oduction from progesterone and for DHEA from pregnenolone, indicating a distributive character of the
133 he ability of adipocyte CYP11A1 in producing pregnenolone is demonstrated for the first time, renderi
134 of the male hormone dehydroepiandrosterone, pregnenolone is first hydroxylated by P450 CYP17A1 at th
138 n is stronger when the hydroxylase substrate pregnenolone is present in the CYP17A1 active site than
141 of steroidogenic tissues, the first steroid, pregnenolone, is synthesized in adrenal and gonadal tiss
144 dogenic organs, our recent study showed that pregnenolone must be synthesized by another mitochondria
145 on, participants were administered 400 mg of pregnenolone (n=16) or placebo (n=15) and underwent 3T f
147 rrent report, the effect of the neurosteroid pregnenolone on depressive symptoms in BPD was examined.
148 amined the effects of 3alpha,5alpha-THP, and pregnenolone on TLR4 activation in both the periphery an
149 t measurably alter the binding of 17alpha-OH pregnenolone or 17alpha-OH progesterone, as judged by th
150 progesterone but not the immediate precursor pregnenolone or estrogen, another major mammalian steroi
151 rmal pregnant females with pellets releasing pregnenolone or progesterone did not cause fetal demise.
154 positive allosteric modulators (zuranolone, pregnenolone, PEA), psychedelics (psilocybin, 5-MeO-DMT)
157 ical hydroxylation of its primary substrate, pregnenolone (PREG) and then also orchestrates a remarka
159 tion of the steroids progesterone (Prog) and pregnenolone (Preg) to glucocorticoids and androgens.
160 10 min of exposure to the steroids cortisol, pregnenolone, pregnenolone sulfate, or progesterone.
163 nlike testicular and adrenal cortical cells, pregnenolone production in glial cells was not inhibited
165 P1A1/CYP1B1 inhibitors significantly reduced pregnenolone production in the presence of 22(R)-hydroxy
166 dria-targeted CYP1B1 significantly increased pregnenolone production under basal conditions and in th
167 mine and deferiprone significantly inhibited pregnenolone production, indicating involvement of anoth
174 rometry (LC-MS/MS), we examined 11 steroids: pregnenolone, progesterone, corticosterone, dehydroepian
177 ase reactions, particularly with 17a-hydroxy pregnenolone, remains a challenge for the treatment of p
182 zyme converts cholesterol and campesterol to pregnenolone, suggesting that digoxin biosynthesis start
183 omers of dehydroepiandrosterone sulfate (1), pregnenolone sulfate (2), and (3alpha,5beta)-3-hydroxypr
185 of NMDARs include an endogenous neurosteroid pregnenolone sulfate (PES), but the binding site of PES
187 roid pregnenolone (PREG) and its metabolites pregnenolone sulfate (PregS) and allopregnanolone in ser
190 h models of the GABA-inhibitory neurosteroid pregnenolone sulfate (PREGS), suggesting common mechanis
192 nhibited by the endogenous sulfated steroids pregnenolone sulfate (PS) and dehydroepiandrosterone sul
193 o stimulation by the endogenous neurosteroid pregnenolone sulfate (PS) and heat, and altered response
201 We examined the effects of the neurosteroid pregnenolone sulfate (PS) on GABA(A) receptor-mediated s
208 iously shown that the sulfated neurosteroids pregnenolone sulfate and 3alpha-hydroxy-5beta-pregnan-20
209 parent lack of state dependence suggest that pregnenolone sulfate and 3alpha5betaP inhibit the GABA(A
212 his study shows that the inhibitory steroids pregnenolone sulfate and dehydroepiandrosterone sulfate
213 loreclezole, had different IC(50) values for pregnenolone sulfate and lanthanum, and were insensitive
214 sure alters the actions of the neurosteroids pregnenolone sulfate and pregnenolone hemisuccinate, whi
215 oth compounds competed with progesterone and pregnenolone sulfate and significantly reduced CatSper a
216 bserve enantioselectivity for the actions of pregnenolone sulfate and steroid sulfate 3 indicates tha
217 tsynaptic neuron depolarization, and an anti-pregnenolone sulfate antibody scavenger blocked this eff
219 lopregnanolone and/or the inhibitory steroid pregnenolone sulfate closely matched predicted open prob
220 l CatSper currents, whereas the neurosteroid pregnenolone sulfate exerted similar effects as progeste
221 ectrophysiological techniques, we found that pregnenolone sulfate increases the frequency of AMPA-med
222 report here that the excitatory neurosteroid pregnenolone sulfate induces a long-lasting strengthenin
228 nhanced responses to the neurosteroid ligand pregnenolone sulfate when co-expressed with wild-type TR
229 hermore, the GluN2A/B-selective potentiator (pregnenolone sulfate) and the GluN2C/D-selective potenti
231 teric potentiation of NMDA receptor pores by pregnenolone sulfate, 24(S)-hydroxycholesterol, and doco
232 resence of the steroids allopregnanolone and pregnenolone sulfate, although the steroids interact wit
234 s steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate, and beta-estradiol in the absence
235 ulfated and unsulfated neurosteroids such as pregnenolone sulfate, dehydroepiandrosterone sulfate (DH
238 ne mediating the effects of the neurosteroid pregnenolone sulfate, or the allosteric regulatory site
239 vity for activation by the endogenous ligand pregnenolone sulfate, pointing to an allosteric interact
256 he circulation of phosphates, which elevated pregnenolone synthesis by 2-fold by increasing the stabi
257 siRNA knockdown did not significantly reduce pregnenolone synthesis in human adrenal cortical cells,
261 and sterol biosynthesis pathways upstream of pregnenolone synthesis was coordinately downregulated in
262 gh the intermediacy of cAMP rapidly increase pregnenolone synthesis, and this rapid steroidogenic res
263 e, addition of hydroxycholesterols increased pregnenolone synthesis, suggesting desmolase activity th
264 d antioxidants had no significant effects on pregnenolone synthesis, suggesting it is not regulated b
267 es for an alternative pathway for glial cell pregnenolone synthesis: (1) regulation by reactive oxyge
268 oids (allopregnanolone, epiallopregnanolone, pregnenolone, testosterone, and dehydroepiandrosterone)
269 ive symptoms of schizophrenia with a dose of pregnenolone that elevates serum levels of the neuroacti
270 22 carbon-carbon bond of cholesterol to form pregnenolone, the first 21-carbon precursor of all stero
271 aves the side chain of cholesterol, yielding pregnenolone, the precursor of all steroid hormones.
272 er mitochondrial membrane to be converted to pregnenolone, the precursor of all steroid hormones.
273 catalyzes conversion of cholesterol (CH) to pregnenolone, the precursor to all steroid hormones.
274 n cleavage (P450scc) converts cholesterol to pregnenolone, the rate-limiting enzymatic reaction in ne
275 PD, depressed mood state, were randomized to pregnenolone (titrated to 500 mg/day) or placebo, as add
276 the two-step oxidations of progesterone and pregnenolone to androstenedione and dehydroepiandrostero
277 tein that converts dehydroepiandrosterone or pregnenolone to androstenedione or progesterone, respect
279 pe 2 (3betaHSD2) catalyzes the conversion of pregnenolone to progesterone and dehydroepiandrostenedio
280 osensors to improve the biotransformation of pregnenolone to progesterone in yeast and to regulate CR
281 xysteroid dehydrogenase (3beta-HSD, converts pregnenolone to progesterone), and the progesterone rece
282 3beta-hydroxysteroid dehydrogenase (converts pregnenolone to progesterone), and the progesterone rece
283 id synthesis by catalyzing the conversion of pregnenolone to progesterone, which is mediated by the i
286 urther, when the concentration of 17alpha-OH pregnenolone was held constant and the P450 concentratio
287 Although the anti-inflammatory property of pregnenolone was recognized several decades ago, its mec
290 Progesterone, pregnenolone, and 17alpha-OH-pregnenolone were potent inhibitors of Delta24-reduction
291 ia from PBR-negative cells failed to produce pregnenolone when supplied with exogenous cholesterol.
292 oidogenic pathway, converting cholesterol to pregnenolone, whereas CYP11B2 completes the final step i
293 olesterol but is also capable of sulfonating pregnenolone, whereas SULT2B1a preferentially sulfonates
294 preference for dehydroepiandrosterone versus pregnenolone with second-order rate constants (kcat/Km)
295 factor unequivocally as the nuclear receptor pregnenolone X receptor (PXR) and its human homologue, s
297 t by inhibiting the activation of NRs, human pregnenolone X receptor and constitutive androstene rece
298 tor SXR/PXR (steroid and xenobiotic receptor/pregnenolone X receptor) has been shown both biochemical