Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027651 (tumor)
 685,946 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We have studied the effects of a novel derivative of apovincaminic acid ester, VA-033, on the resistance of tumors to chemotherapeutic agents. VA-033 increased the sensitivity of drug-resistant cell lines (P388/VCR, P388/ADM, AD10, and K562/ADM) to adriamycin or vincristine. The potency of VA-033 was stronger than verapamil. The drug lengthened the survival time of the P388/VCR-implanted mice treated with vincristine. VA-033 increased the intracellular accumulation of vincristine in the tumor cells, and the photolabeling of P-glycoprotein by [3H]azidopine was inhibited by VA-033. VA-033 showed a slight inhibitory effect on the L-type Ca2+ current in the ventricular myocytes, and had less effect on the cardiovascular parameters such as blood pressure, contractile force and atrio-ventricular conduction time than verapamil when administered systemically in the dog. These results suggest that VA-033 may become a beneficial compound as a modifier to the neoplastic cell resistant to multidrugs.
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PMID:Overcoming of multidrug resistance by VA-033, a novel derivative of apovincaminic acid ester. 920 May 66

E7010 (N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonami de), an orally active sulfonamide antitumor agent that is currently in a Phase I clinical trial, showed rather consistent growth-inhibitory activities against a panel of 26 human tumor cell lines (IC50 = 0.06-0.8 microg/ml), in contrast to vincristine (VCR; IC50 = 0.0002-0.04 microg/ml), 5-fluorouracil (IC50 = 0.2-30 microg/ml), Adriamycin (IC50 = 0.002-0.7 microg/ml), mitomycin C (IC50 = 0.007-3 microg/ml), 1-beta-D-arabinofuranoxylcytosine (IC50 = 0.005 to >30 microg/ml), camptothecin (IC50 = 0.002-0.4 microg/ml), and cisplatin (IC50 = 0.5-20 microg/ml). It caused a dose-dependent increase in the percentage of mitotic cells in parallel with a decrease in cell proliferation, like VCR. It also showed a dose-dependent inhibition of tubulin polymerization, which correlated well with the cell growth-inhibitory activity. 14C-labeled E7010 bound to purified tubulin, and this binding was inhibited by colchicine but not by VCR. However, its binding properties were different from those of colchicine, as well as those of VCR. E7010 was active against two kinds of VCR-resistant P388 cell lines, one of which showed multidrug resistance due to the overexpression of P-glycoprotein (resistant to Taxol), and the other did not show multidrug resistance (sensitive to Taxol). Furthermore, four E7010-resistant P388 cell lines showed no cross-resistance to VCR, a different pattern of resistance to podophyllotoxin, and collateral sensitivity to Taxol. Therefore, E7010 is a novel tubulin-binding agent that has a wider antitumor spectrum than VCR and has different properties from those of VCR or Taxol.
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PMID:Mechanism of action of E7010, an orally active sulfonamide antitumor agent: inhibition of mitosis by binding to the colchicine site of tubulin. 924 51

The biological characteristics of a new monoclonal antibody (TO73) reacting with a vincristine-resistant human leukemic cell line (KY-VCR) were evaluated. Immunological and electron-immunological studies showed that TO73 reacted with the surface glycoprotein of KY-VCR. TO73 was found to have no effect on cell growth and intracellular uptake of vincristine. In human neoplastic cell lines, TO73 was found to react with 11 of 27 (41%) cell lines. With regard to de novo primary tumor with one exception, TO73 did not react with any of the examined primary tumor cells. The patient with TO73-positive leukemia died of induction failure due to drug resistance. Complete remission was achieved in the other leukemic patients. These results indicate that TO73 antigen may be associated with immortalization of tumor cells and poor prognosis in some cases.
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PMID:High reactivity of monoclonal antibody (TO73) with human malignant tumor cell line. 931 Oct 11

A 32-year-old man presented with a swelling of the left testis, for which he underwent high inguinal orchiectomy. Histopathological examination of the specimen revealed teratocarcinoma. Further evaluation revealed no metastasis (stage I), and he was followed-up by monthly examination without prophylactic chemotherapy (surveillance). Thirteen months after orchiectomy, AFP and hCG-beta were elevated at 133.8 ng/ml and 0.8 ng/ml respectively. Abdominal CT scan revealed para-aortic masses of recurrent tumor. Although the AFP and hCG-beta levels markedly declined after five courses of COMPE (CDDP, VCR, MTX, PEP, Etoposide) chemotherapy, the retroperitoneal masses had further enlarged and had undergone cystic change. Excision of the residual tumors was performed, and microscopic examination of specimens revealed mature teratoma without malignant components. The diagnosis of the growing teratoma syndrome was therefore made. The growing teratoma syndrome occurs in nonseminomatous testicular germ cell tumors following chemotherapy and is characterized by enlargement of metastatic lesions with normal tumor marker levels. Total surgical resection of the mass yields good results, and tumor is unresponsive to chemotherapy. Early recognition of this syndrome is important for successful treatment.
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PMID:[The growing teratoma syndrome: report of a case]. 978 Jun 59

A chemotherapeutic protocol for advanced thymic carcinoma has not been established as yet. We described a case of advanced and relapsed thymic carcinoma that responded remarkably to subsequent chemotherapy with CPT-11. A 61-year-old man was admitted to our hospital because of facial edema and general fatigue. Chest X-ray and CT scan showed anterior mediastinal tumor which involved large vessels and pericardium. CT guided needle biopsy yielded a diagnosis of squamous cell type of thymic carcinoma. The patient was initially treated with ADOC (ADM, CDDP, VCR, CPA) chemotherapy and had successfully controlled for six months. However, the mediastinal tumor recurred and radiotherapy and nedaplatin plus ETP therapy were not effective. Then, CPT-11 chemotherapy (80 mg/m2, 2 weeks) was performed. The patient showed a partial response after two courses of CPT-11 chemotherapy. This case suggests that CPT-11 is a useful chemotherapeutic agent for advanced thymic carcinoma.
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PMID:[A case of relapsed thymic carcinoma that responded remarkably to chemotherapy with CPT-11]. 983 15

PSC 833, a nonimmunosuppressive cyclosporin, is able to inhibit the efflux of antitumor drugs mediated by P-glycoprotein (P-gp). The purpose of the present study is to compare the effect of PSC 833 on the tumor disposition of [3H]vincristine ([3H]VCR) and [3H]vinblastine ([3H]VBL) in in vitro and in vivo experiments from a pharmacokinetic point of view. In in vitro experiments, the effect of PSC 833 was investigated on the cellular uptake of [3H]VCR and [3H]VBL by HCT-15 and COLO 205, human colorectal tumor cell lines with extensive and minimal expression of P-gp, respectively. PSC 833 (2 microM) increased the cellular uptake of [3H]VCR and [3H]VBL by HCT-15 cells, but not that by COLO 205 cells, 8- and 6-fold, respectively, without affecting the initial influx rates. In addition, 2 microM PSC 833 reduced the efflux of [3H]VCR from HCT-15 cells to a level comparable with that from COLO 205 cells. Furthermore, the effect of PSC 833 on the tumor disposition of intravenously administered [3H]VCR and [3H]VBL was studied in tumor inoculated mice. Infusion of PSC 833 (10 microg/hr/mouse) increased the HCT-15 tumor disposition of [3H]VBL and [3H]VCR in vivo to a level comparable with that observed in vitro. These findings demonstrate that PSC 833 enhances the tumor disposition of vinca alkaloids by inhibition of P-gp-mediated efflux not only in vitro but also in vivo in a solid tumor model.
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PMID:Modulation of the tumor disposition of vinca alkaloids by PSC 833 in vitro and in vivo. 986 80

The curability of pediatric cancer has been improved to nearly seventy percent. This change has been achieved by refinements in treatment strategy and supportive care. More than seventy percent of patients with ALL can be cured by modern chemo-radiotherapy with reduced late effects. The stratification of the patients by risk factor, introduction of CNS prophylaxis, shortening of the duration of chemotherapy and intensification of the chemotherapy with agents such as HD-MTX have contributed to this remarkable success. Burkitt's lymphoma is a tumor for which the curability has improved from almost zero to ninety percent. With Wilms' tumor, clinical trials have been used to optimally refine the treatment strategy. The NWTS first compared the efficacy of combined VCR and Act-D with the single use of each drug. The difference was significant. The results of the systematic trials were then used to improve the survival rate of patients with Wilms' tumor from twenty to ninety percent and shorten the duration of chemotherapy to six months. On the other hand, tumors remain with which less than half of patients can survive for long. Advanced neuroblastoma and AML are typical such tumors. With these diseases, refinements in the treatment based on evidence derived from clinical trials have been insufficient. Further intensification of the treatment or novel approaches to control tumor growth are warranted for these diseases. In this article, I would like to describe the "standard" therapy for each tumor and the evidence on which improvements in those strategies have been based.
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PMID:[Evidence based chemotherapy for pediatric cancers]. 1070 Aug 90

TZT-1027 was evaluated for its antitumor effects in sixteen human tumors xenografted in nude mice from gastric (H-81, H-106, H-30, H-154), breast (H-31, H-62), colon (H-110, H-143), lung (LC-376, H-74, Mqnu-1, LC-351), liver (H-181), renal cell (H-12) and ovarian (H-OC-3, SOC-4) cancer lines. In the latter three and lung (Mqnu-1, LC-351) cancers the results were compared with those obtained with CPT-11, VCR, CDDP, ADM. TZT-1027 showed effective antitumor activity (IR > or = 58%) against fifteen of the tumor lines, all but LC-351, and showed markedly effective activity (IR > or = 80%) against twelve tumor lines, including drug-resistant colon (H-110), lung (H-74) and ovarian (SOC-4) cancer lines. The complete regression was shown in five H-OC-3 tumor-bearing mice out of seven. Moreover, TZT-1027 was shown to be more potent in three cancer models (Mqnu-1, H-81, SOC-4) than CPT-11, and to have markedly effective antitumor activity in two cancers (H-12, H-OC-3) in which VCR was ineffective and in ovarian cancer (SOC-4) in which CPT-11, CDDP and ADM were ineffective. The administration of TZT-1027 induced fewer side effects; transient reduction of body weight was observed in four lines out of sixteen tested. These results suggest that TZT-1027 is an excellent candidate for clinical trials for the treatment of cancer.
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PMID:[Antitumor effects of TZT-1027, a novel dolastatin 10 derivative, on human tumor xenografts in nude mice]. 1074 Jun 40

A 67-year-old man was admitted with left pleural effusion on chest X-ray film. Chest CT scans showed an anterior mediastinal tumor, left pleural dissemination and pleural effusion. Percutaneous needle biopsy yielded a diagnosis of epitherial carcinoma. The patient underwent 3 courses of systemic chemotherapy (CDDP + ADM + VCR + CPA). At achievement of partial response, the tumor was completely resected. Examination of the resected tumor revealed partial response to chemotherapy. A 49-year-old woman was admitted our hospital with supraclavicular lymph nodes swelling. Chest CT scans showed an large mediastinal tumor. Percutaneous needle biopsy yielded a diagnosis of squamous cell carcinoma of thymus. The patient underwent 3 courses of systemic chemotherapy. At achievement of partial response, the tumor was completely resected. Examination of the resected tumor revealed partial response to chemotherapy. These cases indicate the usefulness of preoperative chemotherapy for advanced thymic carcinoma to reduce tumor size and to control local invasion, distant metastasis before operation.
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PMID:[Two cases of thymic carcinoma effectively treated by preoperative chemotherapy]. 1080 95

We have reported that three reversal agents were sifted out from 32 Chinese galenicals through a series of cell culture tests. Among them, Fw13-te41 has the best effect of reversal cancer multidrug resistance (MDR) in vitro. In this study, the reversal action of Fw13-te41 in vivo was studied on the animal model of nude mice with human leukemia k562/ADR. Twenty SPF BALB/c-nu/nu nude mice with xenograft tumor were randomly divided into the control group (n = 6), VCR group [intraperitoneal (i.p.) VCR 250 micrograms/week, n = 5], VCR + Fw13-te41 group (i.p VCR 250 micrograms/week + Fw13-te41 0.2 ml/day, equivalent to crude drug 10 g/kg, n = 5), and Fw13-te41 group (i.p Fw13-te41 0.2 ml/day, equivalent to crude drug 10 g/kg, n = 4). After 18 days, the rate of tumor inhibition (RTI) of VCR group was 19.79%, but the RTI of VCR + Fw13-te41 group was as high as 86.95% (P < 0.05). There results demonstrate that the Chinese medicine Fw13-te41 has an evident reversal action of malignancy MDR in vitro and in vivo.
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PMID:[Study on the reversal of cancer multidrug resistance by Chinese medicine Fw13-te41 in nude mice]. 1138 39


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