Abstract：
:It has now been more than 30 years since the laboratory verification of the localization of estrogen in certain animal tissues. Much has been learned since that time regarding the details of this process, including the presence of specific receptors for these hormones in target tissues, the mechanism of ligand binding, the association of the ligand-receptor complex with unique chromatin sequences, and the activation of transcription. A concrete use of this knowledge has been the exploitation of these receptors as a targeting mechanisms for radiopharmaceuticals. This is an exciting area that encompasses both diagnosis and therapy. This review will summarize the in vitro and in vivo data obtained from evaluation of the many compounds that have been examined as radiolabeled receptor ligands, and will also discuss the chemistry necessary for their preparation. In particular, relative binding affinity values for relevant compounds will be tabulated, grouped according to molecular class. For those materials for which biodistributions have been performed, uterine (target), liver (nontarget, clearance), and, when available, tumor tissue uptake values are presented. These data should provide a reminder of what has been accomplished, and should serve as a working reference for those engaged in the pursuit of new candidates for these applications.
journal_name
Steroidsjournal_title
Steroidsauthors
Cummins CHdoi
10.1016/0039-128x(93)90069-ysubject
Has Abstractpub_date
1993-06-01 00:00:00pages
245-59issue
6eissn
0039-128Xissn
1878-5867pii
0039-128X(93)90069-Yjournal_volume
58pub_type
杂志文章,评审相关文献
STEROIDS文献大全abstract：:Here we report on the progress we have made in elucidating the mechanisms through which estrogen alters synaptic responses in hypothalamic neurons. We examined the modulation by estrogen of the coupling of various receptor systems to inwardly rectifying and small conductance, Ca(2+)-activated K(+) (SK) channels. We us...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/s0039-128x(01)00181-7
更新日期：2002-05-01 00:00:00
abstract：:Brassinosteroids (BRs) are an important class of plant hormones with a multitude of functions. They have been intensively investigated for their biosynthesis, distribution and physiological functions. The aim of this study was to examine possible effects of BRs on the plant plasma membrane cation conductances and Ca(2...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.10.008
更新日期：2015-05-01 00:00:00
abstract：:The palladium-catalyzed coupling of various 17-iodo-delta 16 steroids (17-iodo-androst-16-ene, 17-iodo-4-methyl-4-aza-androst-16-en-3-one, and 17-iodo-4-aza-androst-16-en-3-one) with dialkyl phosphites (dimethyl phosphite, diethyl phosphite, and diisopropyl phosphite) was examined in detail. The only successful condit...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(95)00121-6
更新日期：1995-12-01 00:00:00
abstract：:Cortisol 21-amine (21-amino-11beta,17-dihydroxy-4-pregnene-3,20-dione) was prepared and an enzyme immunoassay for cortisol in serum was established using cortisol 21-amine conjugated with alkaline phosphatase. The minimal amount of cortisol detected was 1ng/tube and the measurable range was from 1 to 80 microgram/d1, ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(78)90106-x
更新日期：1978-07-01 00:00:00
abstract：:By the conventional methods of gas liquid chromatography (GLC) as well as mass spectrometry, 3beta,7alpha-dihydroxychol-5-en-24-oic acid (delta5-acid), a key intermediate of chenodeoxycholic acid biogenesis and its metabolic by-product, 3alpha,7alpha-dihydroxychol-4-en-24-oic acid (delta4-acid) have not yet been ident...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(78)90102-2
更新日期：1978-07-01 00:00:00
abstract：:Catalytic cycloalumination of (3β,5α)-3-vinylcholestane and (3α,5α)-3-allylcholestane with Et3Al catalyzed by Cp2ZrCl2 was performed for the first time to give previously unknown aluminacyclopentanes in ∼90% yield; these products were converted in situ to carbo- and heterocyclic (5α)-cholestane derivatives. ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2016.01.015
更新日期：2016-04-01 00:00:00
abstract：:Dioscorea panthaica is a traditional Chinese medicinal herb used in the treatment of various physiological conditions, including cardiovascular disease, gastropathy and hypertension. Steroidal saponins (SS) are the main active ingredients of this herb and have effects on myocardial ischemia and cancer. The phytochemic...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.12.023
更新日期：2015-03-01 00:00:00
abstract：:Preimplantation rabbit embryos were incubated with pregnenolone and dehydroisoandrosterone under conditions which gave formazan precipitation by the histochemical technique. The metabolic fate of the labeled steroids was assessed simultaneously. There was no concomitant transformation of pregnenolone to progesterone a...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(81)80012-8
更新日期：1981-02-01 00:00:00
abstract：:Inhibition of concise enzymes in ergosterol biosynthesis is one of the most prominent strategies for antifungal chemotherapy. Nevertheless, the enzymes sterol C5-desaturase and sterol C22-desaturase, which introduce double bonds into the sterol core and side chain, have not been fully investigated yet for their potent...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2015.05.004
更新日期：2015-09-01 00:00:00
abstract：:4- to 8-cell mouse PIE's (preimplantation embryos) were cultured in vitro for 48 hr in media containing various concentrations of the anti-estrogen CI-628. Graded effects of the various concentrations were observed with the highest concentration (1.5 microng/ml) being 100% effective in blocking development to the blas...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(77)90005-8
更新日期：1977-03-01 00:00:00
abstract：:The importance of computer-aided drug design and development is clear nowadays. These approaches smooth the way of designing some efficient candidates based on drugs in use. At this place, we studied the mechanism of D4-abiraterone (D4A), the active metabolite of Abiraterone (Abi), binding to CYP17A1 compared with Abi...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2021.108799
更新日期：2021-01-17 00:00:00
abstract：:7 alpha- and 7 beta-carboxymethyl-derivatives of 17-hydroxyprogesterone and 11-deoxycortisol have been synthesized. After coupling to bovine serum albumin, they were used to elicit antibodies in rabbits. No major difference in the steroid specificity of the antisera was observed when either 7 alpha- or 7 beta-epimers ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(80)90112-9
更新日期：1980-01-01 00:00:00
abstract：:A new spirostane steroidal saponin, govanoside A (1) along with three known compounds borassoside E (2) pennogenin (3) and diosgenin (4) were isolated from rhizomes of Trillium govanianum. Their structures were elucidated through 1D, 2D-NMR spectroscopic data analysis and acid hydrolysis. Compound (2) in genus Trilliu...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2015.10.013
更新日期：2015-12-01 00:00:00
abstract：:Breast cancer risk is strongly related to several reproductive and hormonal factors, but the nature of the effects of endogenous oestrogens has been difficult to establish. Data are now available from several large prospective studies with biobanks of stored serum, enabling better characterization of the associations ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.02.029
更新日期：2011-07-01 00:00:00
abstract：:At the development of receptivity the endometrium undergoes specific changes. Several factors have been suggested as markers of endometrial receptivity. A common feature for most of these factors is that they are directly, or indirectly, regulated by progesterone. The effect of various doses and regimens of mifepristo...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/s0039-128x(03)00131-4
更新日期：2003-11-01 00:00:00
abstract：:The hormone 1alpha,25(OH)2vitamin D3 (1,25-D) produces biological responses via both genomic and rapid mechanisms. The genomic responses are linked to a nuclear receptor, while the rapid responses are believed to utilize other signal transduction pathways that are likely linked to a putative cell membrane receptor for...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/s0039-128x(98)00091-9
更新日期：1999-01-01 00:00:00
abstract：:Recent reports demonstrate neurotrophic properties of dehydroepiandrosterone sulfate (DHEAS) in men at rest, as well as profound neurotrophic responses to stress in both men and women. Little is known of neuroprotective-neurotrophic effects of DHEAS during stress exposure, either in men or women. This translational st...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.05.011
更新日期：2014-09-01 00:00:00
abstract：:Periodontitis is a complication of diabetes mellitus, and the two diseases are highly associated with the dysfunction of inflammatory mediators. 25-hydroxyvitamin D(3) (25(OH)D(3)) plays a pivotal role in inflammatory modulation, but little is known about its effects on the progression of diabetic periodontitis and th...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2012.10.015
更新日期：2013-02-01 00:00:00
abstract：:We have investigated the metabolism of deoxycorticosterone in A6 cells, a continuous cell line derived from the kidney of Xenopus laevis. A6 cells at confluence were incubated with serum-free culture media containing 2.5 microM [3H] deoxycorticosterone. When radioactive compounds in incubation media were separated by ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(95)00038-r
更新日期：1995-07-01 00:00:00
abstract：:Spinasterol and schottenol, two phytosterols present in argan oil and in cactus pear seed oil, were synthesized from commercially available stigmasterol by a four steps reactions. In addition, the effects of these phytosterols on cell growth and mitochondrial activity were evaluated on 158N murine oligodendrocytes, C6...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2015.01.005
更新日期：2015-07-01 00:00:00
abstract：:Six naturally occurring C27 ecdysteroids were isolated and identified from the tobacco hornworm during pupal-adult development five days after peak titer of molting hormone activity. In order of decreasing quantities the hormones were: 20,26-dihydroxyecdysone, 3-epi-20-hydroxyecdysone, 20hydroxyecdysone, 3-epi-20,26-d...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(79)90084-9
更新日期：1979-09-01 00:00:00
abstract：:From the aerial parts of Euphorbia sogdiana Popov, obtusifoliol (1) and two related steroids (2-3) have been isolated and characterized along with a known cycloartane derivative (4). The chemical structure of the obtusifoliol-related compounds, obtained by 1D and 2D NMR, and MS measurements, have been determined as: 3...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2016.07.008
更新日期：2016-11-01 00:00:00
abstract：:Many flavonoids and isoflavonoids have anti-diabetic effects in animal models. However, the mechanisms that are involved are generally unclear. Since 11β-hydroxysteroid dehydrogenases (HSD11Bs) play important roles in diabetes, we hypothesize that flavonoids and isoflavonoids may affect diabetes by targeting two isofo...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2018.01.013
更新日期：2018-04-01 00:00:00
abstract：:The preparation of 3-oxo-4-azasteroid from A-nor-3,5-secosteroid-3-oic acid is described in a solventless condition catalysed by Lewis acid under microwave irradiation. We utilized urea as an environmentally benign source for the generation of ammonia for the aza cyclization reaction. ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2008.01.022
更新日期：2008-07-01 00:00:00
abstract：:Dehydroepiandrosterone (DHEA) fatty acyl esters once incorporated in high density lipoprotein (HDL) induce a stronger vasodilatory response in rat mesenteric arteries ex vivo compared to native HDL. We studied the role of HDL receptor, scavenger receptor class B, type 1 (SR-B1), as well as estrogen and androgen recept...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2010.12.007
更新日期：2011-03-01 00:00:00
abstract：:Steroid hormones are involved in the regulation of a variety of processes like embryonic development, sex differentiation, metabolism, immune responses, circadian rhythms, stress response, and reproduction in vertebrates. Teleost fishes and humans show a remarkable conservation in many developmental and physiological ...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2015.06.011
更新日期：2015-11-01 00:00:00
abstract：:The free sterol mixture of the sponge Psammaplysilla purpurea was shown to contain aplysterol as the major constituent. In addition to other sterols such as 5,7-cholestadien-3beta-ol, cholesterol, 5alpha-cholestan-3beta-ol, 24epsilon-methylcholesta-5,22-dien-3beta-ol, 24epsilon--methylcholesterol, 24epsilon-ethylchole...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(78)80046-4
更新日期：1978-06-01 00:00:00
abstract：:Human placental 17 beta, 20 alpha-hydroxysteroid dehydrogenase was completely inactivated by the affinity alkylator, 3-bromoacetoxy-1,3,5(10)-estratrien-17-one (estrone 3-bromoacetate). The inactivated enzyme was then reactivated to 100% of the enzyme activity by base-catalyzed hydrolysis of the steroidalester-enzyme ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(84)90039-4
更新日期：1984-02-01 00:00:00
abstract：:During our studies of the hepatic androgen receptor in cynomolgus monkeys, tritiated mibolerone +/- a 200-fold excess of unlabeled mibolerone has been used to determine specific binding in cytosol. During time-course studies, high-capacity, unsaturable binding of [3H]mibolerone was noted after short-term incubations (...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(95)00116-8
更新日期：1995-11-01 00:00:00
abstract：:The main purpose of this review article is threefold (a) to try to address the question "why are two adrenal glucocorticoids, cortisol and corticosterone, secreted by humans and other mammalian species?", (b) to outline a hypothesis that under certain physiological conditions, corticosterone has additional biochemical...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2015.06.017
更新日期：2015-10-01 00:00:00
