Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
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Drug
Enzyme
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Target Concepts:
Gene/Protein
Disease
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Enzyme
Compound
Query: UMLS:C0338671 (
Steroids
)
9,479
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
An improved synthesis of spin-labeled cortisol, cortisone, and testosterone using N,N'-cyclohexylcarbodiimide (
DCC
) is reported. The spin labeled steroids are shown to result from the esterification at the most reactive C(21) and C(17) hydroxyl groups. A mild and high yield oxidation of cortisol spin label to cortisone spin label by chromium trioxide-pyridine is also discussed.
Steroids
1983 Sep
PMID:Synthesis of some steroid spin labels. 632 18
In MCF-7 breast cancer cells, hydroxytamoxifen (OH-Tam) up-regulates the estrogen receptor (ER) in a form unable to bind [(3)H]estradiol (E(2)). We show here that this property is not restricted to this antiestrogen. [(3)H]E(2) binding assays (whole cell assays,
DCC
assays on cell extracts) and enzyme immunoassays (Abbott) performed in parallel, establish the permanent presence of such unusual ERs in the absence of any exposure of the cells to a ligand. E(2) and the pure antiestrogen RU 58 668, which down-regulate ER, also decrease [(3)H]E(2) binding. In control cells, these ERs represent about the half of the whole receptor population; they also display a tendency to stabilize within the cell nucleus. Loss of E(2) binding ability appears irreversible, since we failed to label receptor accumulated under OH-Tam with [(3)H]E(2) or [(3)H]tamoxifen aziridine (TAZ). Cycloheximide (CHX), which blocks E(2)-induced down regulation of ER, failed to stabilize [(3)H]E(2) binding (whole cell assay) after an [(3)H]E(2) pulse (1 h), confirming that regulation of E(2) binding and peptide level are related to different regulatory mechanisms. Loss of binding ability could not be ascribed to any ER cleavage as demonstrated by Western blotting with a panel of ER antibodies raised against its various domains (67 kDa ER solely detected). We propose that loss of E(2) binding ability is related to the aging process of the receptor, i.e. it is progressively converted to a form devoted to degradation after it has accomplished its physiological role. Ligands may favor (E(2), RU 58 668) or impede (OH-Tam) this elimination process.
Steroids
2000 Dec
PMID:Evidence of an estrogen receptor form devoid of estrogen binding ability in MCF-7 cells. 1107 89
The preparation of a steroidal heterocycle linked to the tripeptide Cys-Gly-Cys is described. Initially, an estrane-derived steroidal heterocycle containing an aminopyrimidine ring fused to the 16,17-position of the steroidal nucleus was synthesized. Thereafter, protected amino acids were coupled iteratively by the
DCC
method, commencing at the amino group of the aminopyrimidine unit.
Steroids
2003 Oct
PMID:Estrano[17,16-e]pyrimidine-peptide conjugates. 1462 7