Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00627 (MAP)
 15,705 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

MAP was used in high doses (1 g/die up to a total dose of 45-50 g) in 44 cases of advanced mammary carcinoma (IIIrd and IVth stage of the T.N.M. classification), evaluated according to the criteria proposed by CBCG. The excellent tolerance to the drug, even at such high doses, is stressed. Therapeutic responses were best in cases of metastasis in the soft and bony tissues and in cases of pulmonary metastasis. It is pointed out that the effectiveness of the treatment is particularly evident in patients in whom the free interval has exceeded two years and in patients in the menopause for more than five years. In the light of results obtained, the possibility of introducing the drug into the therapeutic strategy of this condition is discussed.
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PMID:[Use of high doses of medroxyprogesterone acetate in the palliative treatment of advanced breast cancer. Clinical experience with 44 cases]. 7 11

Cytosol from human benign hyperplastic and carcinomatous prostatic tissue has been shown to contain a progestin receptor with a dissociation constant of approximately 10(-9) M. The receptor was measured using 3H-labeled R 5020 (17 alpha, 21-dimethyl-19-nor-4,9-pregnadiene-3,20-dione) as ligand. Progesterone, cyproterone acetate, and R 1881 (methyltrienolone) were efficient competitors to R 5020 for binding sites on the receptor whereas testosterone, 5 alpha--dihydrotestosterone, estradiol, cortisol, and several hydroxylated and saturated derivatives of progesterone did not compete. The [3H]R 2020-receptor-complex had a sedimentation coefficient of approximately 4 S, an isoelectric point of approximately 5, was heat-labile, and was destroyed by treatment with trypsin but not with deoxyribonuclease or ribonuclease. Seventeen of 21 patients with benign prostatic hyperplasia and three patients with prostatic carcinoma had 1 to 40 fmoles of specific R 5020-binding sites per mg of cytosol protein. One sample of normal prostatic tissue did not contain significant amounts of progesting receptor. Tissue specimens removed by transvesical adenoma enucleation displayed a larger number of specific R 5020-binding sites than electroresected specimens. The progestin receptor in hyperplastic prostate may be involved in the mechanism of the action of progestins used in the medical treatment of benign prostatic hyperplasia. Quantitation of progestin receptor in cancer of the prostate may form part of the basis of a predictive test program for endocrine therapy of prostatic malignancy.
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PMID:Demonstration of a progestin receptor in human benign prostatic hyperplasia and prostatic carcinoma. 7 18

Cells of sarcoma 180 and of Ehrlich's carcinoma were maintained by serial transplantation in male and female Swiss mice. Either estrogen, progesterone, or testosterone were injected im at doses of 1 mg/mouse. Ascitic fluid was aspirated at intervals of 1, 3, 6, 24, and 48 hours following hormone injections. Enzyme activities were analyzed by subjective grading according to the intensity of staining reaction. Estrogen produced enhancement of alkaline phosphatase activity in both types of cells in both sexes of mice. Progesterone produced increased alkaline phosphatase activity in both types of cells from female hosts but an inhibitory effect in male hosts' cells. Testosterone produced no change in enzyme activity in tumor cells of female hosts but in male hosts it inhibited enzyme activity of sarcoma 180 cells and activated activity in carcinoma cells. The effect of all 3 hormones on acid phosphatase activity was activation. With adenosine triphosphatase, estrogen stimulated the activity in both types of tumor in both sexes. Progesterone stimulated cells from male hosts with little or no effect on cells from female hosts. This enzyme was resistant to testosterone. Succinate dehydrogenase activity under similar conditions was different. Estrogen reduced this activity and progesterone produced some inhibition of activity. Testosterone inhibited the sarcoma cells but had no effect on carcinoma cells of either sex. Others have shown that sex hormones affect the enzyme activities beyond the target tissues, particularly in the liver, kidney, and pancreas. Different responses of the enzymes seemed to depend on the endogenous hormonal status of the mice.
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PMID:Enzymatic responses of transplanted tumour cells towards estrogen, progesterone and testosterone. 13 8

The growth of transplanted carcinomas originating in a gonadectomized C3H male mouse was much faster in intact male mice than in intact or gonadectomized females. Administration of 17beta-estradiol or testosterone propionate in pellets resulted in a marked acceleration of the carcinoma growth in intact female mice. Progesterone and deoxycorticosterone acetate exerted no influence on the carcinoma growth. Neither gonadotropins (pregnant mare's serum gonadotropin plus human chorionic gonadotropin) nor ACTH accelerated the growth. In contrast, cortisone acetate in pellets markedly reduced the growth rate of carcinoma transplants when administered simultaneously with the transplantation. Cortisone acetate also arrested the growth-accelerating effect of 17beta-estradiol on transplanted carcinomas.
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PMID:Effect of steroid hormones on growth of adrenocortical carcinoma transplants in mice;. 16 15

Progesterone was converted in vitro to 16alpha- and 17alpha-hydroxyprogesterones in the presence of NADPH by the testicular microsomal fraction (precipitate at 10 000 x g-105 000 x g) obtained from patients with prostatic carcinoma. 16alpha-Hydroxyprogesterone was not metabolized by either the microsomal or the cytosol fractions, and accumulated in the incubation medium. 16alpha-Hydroxyprogesterone competitively inhibited the activity of the C-17-C-20 lyase in the testicular microsomal fraction with an estimated inhibitor constant of 72 micron. Moreover, the 16alpha-hydroxyprogesterone non-competitively inhibited the activity of the 20alpha-hydroxysteroid dehydrogenase in the testicular cytosol fraction and had an estimated inhibitor constant of 52.9 micron. Other testicular enzymes related to steroid metabolism, such as delta5-3beta-hydroxysteroid dehydrogenase coupled with the delta4-delta5 isomerase, 16alpha-hydroxylase, 17alpha-hydroxylase, and 17beta-hydroxysteroid dehydrogenase were not influenced in vitro by 16alpha-hydroxyprogesterone at the concentration of 0.1 mM. From these findings, it is concluded that 16alpha-hydroxyprogesterone inhibit specifically the cleavage of the side-chain of 17alpha-hydroxypregnenes in the course of androgen formation from pregnenolone in vitro.
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PMID:In vitro effect of 16alpha-hydroxyprogesterone on the enzyme activities related to androgen production in human testes. 58 Nov 17

The effects of prolactin, estradiol, and progesterone on 3-methyl-cholanthrene (MCA)-induced cervical carcinogenesis in the NMRI strain of mice are reported. Females were ovariectomized at 6-9 weeks of age. 1 week later cotton threads impregnated with a mixture of MCA and beeswax were inserted into the uterine cervix. In 1 group animals were injected with 5 mcg of ovine prolactin in a solvent. A 2nd group received 5 mcg of estradiol-17beta in the same solvent. A 3rd group received both prolactin and estradiol. The control group received only the solvent. Injections were started on the day of operation and given for 6 days. Some animals were killed on the day after the last injection, others 4 weeks later. In other groups progesterone was injected every 3rd day after the estradiol and progesterone injections. Animals which were killed 1 week after insertion of the MCA threads had stratified squamous epithelium with mild atypica in some areas. A few scattered epithelial ''buds'' were seen to penetrate the stroma. In estradiol-injected animals, 2 of 8 had similar ''buds'' and signs of direct stromal invasion of cells from the basal epithelial layer. In 9 animals receiving only prolactin, 2 showed ''buds'' and doubtful basal membrane invasion. In 6 of 9 animals injected with both prolactin and estradiol, larger ''buds'' were present and overt invasion was seen. In animals killed 4 weeks after operation, squamous cervical carcinomas were found significantly more frequently among animals injected with both estradiol and prolactin (p less than .001) than in other groups. Progesterone had no definite effect on the incidence of carcinoma.
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PMID:A synergistic effect of oestradiol and prolactin influencing the incidence of 3-methylcholanthrene induced cerivical carcinomas in mice. 97 Jan 26

The effect of steroid hormones on modulating the secretion rates of three human breast gross cystic disease fluid proteins (GCDFP-15, GCDFP-24, and GCDFP-44) by T47D breast carcinoma cells in tissue culture was evaluated. Androgens (dihydrotestosterone or fluoxymesterone) were capable of stimulating the secretion rates for all three GCDFP's while showing a minimal trend toward slowing the growth rate of T47D cells. This is the first study which shows that androgens can specifically stimulate all three of the major breast GCDFP's concomitantly. Progesterone, and three synthetic progestins, all showed inhibition of the growth rate of T47D cells while causing enhancement of the secretion of GCDFP-15 and GCDFP-44, and only minimal effect on the secretion rate of GCDFP-24. Estradiol was essentially neutral to the growth rate of the T47D cells in our test system. Estradiol did cause a mild enhancement of GCDFP-44 secretion rate, with no appreciable effect on GCDFP-15 or GCDFP-24 secretion rates. These findings suggest that an androgenic stimulus may be involved in the secretion of GCDFP's associated with breast gross cystic disease.
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PMID:Secretion of breast gross cystic disease fluid proteins by T47D breast cancer cells in culture--modulation by steroid hormones. 144 56

With the purpose of studying changes in the expression of glycoconjugate structures in nonmalignant and cancerous lesions of urothelium the lectins ConA, TKA, PNA, DBA, STA, LFA, UEA, MPA, RCA, LCA, GSA1, SBA, GSA2, WGA, PHA and Lot were tested in formalin-fixed, paraffin-embedded tissue sections of (1) cold biopsies from normal urothelium and bladder cancer of different grades (G1-G3) in humans, (2) normal transitional epithelium and N-butyl-N(4-hydroxybutyl)nitrosamine (BBN)-induced bladder cancer in animal experiments (Wistar rat), and (3) human transitional cancer cell line HT 1376. In human urothelium TKA and SBA were positive markers demonstrating positive staining reactions in all tumor grades without binding to normal epithelium. They stained also the human transitional carcinoma cell line HT 1376 (G3). In Wistar rats DBA, ConA, LCA, SBA, GSA2 and WGA had a specific affinity to BBN-induced carcinoma. Findings of positive lectin marker in transitional cell cancer may offer progress in diagnostics and therapy.
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PMID:Lectins in diagnosis of bladder carcinoma. 158 9

One hundred and six prostatic tissue samples obtained from transurethral resection were analysed for androgen and estrogen receptors. In 62 of these, progesterone and glucocorticoid receptors were also assayed. Steroid receptors were assayed using single saturation dose 3H-labelled ligand assays. Ninety percent of the 97 prostatic hyperplasia tissues and six of the nine prostatic carcinoma tissues were positive for androgen receptors. Estrogen receptors were only present in 19% and 33% respectively. Progesterone receptors were present in 70% of the tissues, but glucocorticoid receptors were present in only 16% of prostatic hyperplasia and none in prostatic carcinoma.
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PMID:Steroid hormone receptors in prostatic hyperplasia and prostatic carcinoma. 172 53

The effects of three hormonal agents with a different mechanism of action (tamoxifen [TAM], medroxyprogesterone acetate [MPA] and estradiol [E2]) on tumor growth, differentiation and oncogene expression were evaluated using the estrogen-receptor positive human breast carcinoma cell line MCF-7 transplanted into nude mice. In MCF-7 tumors treated with E2, tumor incidence, mean weight of tumors, 3H-thymidine labelling index, differentiation antigen HMFGM (human milk-fat globule membrane) and ras p21, c-myc, neu oncogene products, the level was significantly increased. On the other hand MPA suppressed all of them. TAM increased the level of c-myc expression and HMFGM antigen, but suppressed the others. This evidence indicates that E2 induces both proliferation and differentiation of MCF-7 tumor cells. MPA suppresses both proliferation and differentiation, and TAM induces differentiation and suppresses proliferation.
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PMID:Effects of tamoxifen, medroxyprogesterone acetate and estradiol on tumor growth and oncogene expression in MCF-7 breast cancer cell line transplanted into nude mice. 183 73


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