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At least 649 records · Page 36Linked to original sources
PubMed1993

Clustering of modified nucleotides at the functional center of bacterial ribosomal RNA.

An aryl trifluoromethyl diazirine photoreactive derivative was attached to the 2-thiocytidine residue at position 32 of tRNA(IArg) and this derivatized tRNA was bound to Escherichia coli 70S ribosomes. After irradiation at 350 nm the site of cross-linking to the 16S RNA was analyzed by our standard procedures and found to lie within the secondary structural element comprising bases 956-983; this region contains two modified nucleotides at positions 966 and 967. Similarly, an aryl azido photoreactive derivative was attached to the phenylalanine residue of Phe-tRNA(Phe), and the derivatized aminoacyl tRNA was bound to the ribosome either at the A- or the P-site. In both cases, after irradiation at 250 nm, the cross-link site was localized to position 2439 of the 23S RNA; in the secondary structure of the latter the neighboring nucleotide 2442 is base-paired to a modified nucleotide at position 2069. Taken together with other cross-linking data, these results now directly implicate a total of 27 out of the 29 modified nucleotides in E. coli 16S and 23S RNA as lying within or close to the functional center of the ribosome.

Azirines↗
PubMed1982

A phase I trial of aziridinylbenzoquinone (NSC 192986) in patients with previously treated acute leukemia.

Twenty-two adult patients with relapsed leukemia were given aziridinylbenzoquinone (AZQ) intravenously in a phase I clinical trial. AZQ was administered as a 30-minute infusion daily for 17 days. Courses were repeated when the bone marrow returned to normal cellularity and full recovery from nonhematologic toxicity had occurred. The initial dose of AZQ was 8 mg/m2/d x 7. The highest dose given was 28 mg/m2/d x 7. A maximum of three patients were treated at each dose level and patients received at least two courses at a given dose level before they were eligible to be escalated to the next higher available AZQ dose level. Nonhematologic side effects were mild and included nausea/vomiting (32%), mucositis (18%), and alopecia (0%). Dose-limiting toxicity was bone marrow aplasia at the 28 mg/m2/d x 7 level. No complete or partial responses were observed in this initial study. For phase II adult leukemia studies using this schedule, it is recommended that the AZQ dose should be 24 mg/m2/d.

Acute Disease↗
PubMed1982

AZQ therapy in patients with disseminated malignant melanoma.

Twenty-eight patients with disseminated malignant melanoma, who had failed prior therapy, were treated with aziridinylbenzoquinone (AZQ) administered on a 5-day I.V. schedule repeated every 4 weeks. The starting doses were 8 or 6 mg/m2/day x 5 days for good-and-poor-risk patients respectively. There were no complete or partial responses among 23 evaluable patients but four patients had stabilization of disease. The dose-limiting toxicity was thrombocytopenia. Other toxicities included weakness, nausea, vomiting, anorexia, dizziness, abdominal pain, and constipation. AZQ, given on a 5-day schedule, is ineffective in the treatment of patients with metastatic malignant melanoma.

Adult↗
PubMed1983

Phase II trial of aziridinylbenzoquinone (AZQ) in patients with refractory small cell carcinoma of the lung.

Sixteen previously treated patients received AZQ in a phase II study to test therapeutic efficacy in refractory small cell lung cancer. The dose and schedule of AZQ was 20 mg/m2 day 1 and 8, with treatments repeated every 28 days. No objective responses were noted among 16 evaluable patients. Myelosuppression was the major toxicity. AZQ does not appear to have antitumor activity in patients with previously treated small cell carcinoma.

Adult↗
PubMed1984

Phase II clinical evaluation of AZQ in adenocarcinoma of the lung.

Twenty patients with advanced measurable adenocarcinoma of the lung were treated with AZQ 20 mg/m2 weekly for 4 weeks, followed by a 2-week rest. No complete or partial responses were observed. Stabilization was observed in seven individuals, lasting 6-32+ weeks, with a median of 6 weeks. Toxicity was limited to reversible myelosuppression. We conclude that AZQ administered at this dose and schedule has no significant activity against advanced adenocarcinoma of the lung.

Adenocarcinoma↗
PubMed1986

Phase I trial of 5-day continuous infusion aziridinylbenzoquinone (AZQ, diazaquone, NSC 182968).

AZQ was given to 14 patients with solid tumors in a phase I trial. Eight males and six females with a median Karnofsky performance status of 70% (range 40-90%) and a median age of 64 years (range 24-72) received 18 evaluable courses. All patients received prior chemotherapy and seven had prior irradiation. A continuous infusion for 5 consecutive days at doses of 4-8 mg/m2 per day was given every 3-4 weeks. Dose-limiting toxicity was myelosuppression, especially thrombocytopenia. No patient developed an infection while on this study. There was no evidence of cumulative toxicity in the three patients receiving two or more courses. Nonhematologic toxicity consisted only of mild nausea and vomiting in three patients and mild diarrhea in two patients. No patient experienced any mucosal, hepatic, renal, cardiac, or central nervous system toxicity. No objective antitumor responses were seen in the three patients with measurable disease who received two or more courses of AZQ. The recommended doses for phase II studies for continuous-infusion AZQ are 6 mg/m2/day X 5 repeated every 4 weeks.

Adult↗
PubMed1986

Phase II clinical evaluation of AZQ in renal cell carcinoma.

Twenty-two patients with advanced measurable renal cell carcinoma were treated with AZQ 20 mg/m2 weekly for 4 weeks, followed by a 2-week rest. No complete or partial responses were observed among 15 fully evaluable patients. Stabilization was observed in eight individuals (range 8-27 weeks with a median of 12.5 weeks). Toxicity was primarily reversible myelosuppression. We conclude that AZQ administered at this dose and schedule has no significant activity against advanced renal cell carcinoma.

Adenocarcinoma↗
PubMed1986

Phase II evaluation of diaziquone in gastric and pancreatic cancers. A Southeastern Cancer Study Group Trial.

Seventeen patients with pancreatic carcinoma and 30 patients with gastric carcinoma were treated with diaziquone on days 1 and 8 of repeated 4-week courses. No objective responses were seen. Toxicity was primarily myelosuppression, nausea, and vomiting. Since only 10 chemotherapy-naive patients were treated in each disease category, we do not regard this as a definitive trial, but our experience suggests that this dose schedule is not likely to be useful in these types of cancer.

Aged↗
PubMed1988

Response rate and toxicity with aziridinylbenzoquinone in patients with recurrent gliomas. A progress report.

Aziridinylbenzoquinone (AZQ), a quinone-containing lipophilic alkylating agent with molecular properties allowing for good penetration through the blood-brain barrier into the central nervous system, was evaluated in a phase II trial for recurrent gliomas patients. Twenty-four patients with computed tomography (CT) scan measurable disease were entered into the trial and received AZQ in doses of a weekly infusion of 15 mg/m2 (group A) and 17.5 mg/m2 (group B). Twenty-two patients were evaluable for both response and toxicity. There were no complete responses in this study. Partial response rates of 23% (3/13) and 11% (1/9) were achieved in group A and group B patients, for a median duration of response of 35 (range 10-106 weeks) and 19 weeks, respectively. The disease was stabilized in five patients from group A and in four patients from group B. Toxicity was mainly hematologic.

Adolescent↗
PubMed1988

A phase II clinical trial of diaziquone in the treatment of patients with recurrent endometrial carcinoma. A Gynecologic Oncology Group study.

Twenty-six patients with measurable endometrial cancer refractory to standard therapy received AZQ [1,4-cyclohexadiene-1,4-dicarbamic acid, 2,5-bis(1-aziridinyl)3,6,dioxo,diethyl ester, NSC 182986] 22.5 mg/m2 diluted in 150 ml normal saline intravenously every three weeks. Thirteen patients experienced no toxicity and the dose in those patients was increased to 30 mg/m2 after the first course. The median number of courses given was 2.5 (range 1-9). The leukocyte count fell below 3000/microliter in 12 patients, and below 1000/microliter in two. The platelet count fell below 100,000/microliter in 12 patients, and below 25,000/microliter in one. Cumulative hematologic toxicity was not seen. One clinical complete response and one partial response were observed. Eight patients had stable disease. Median time to disease progression was 2 months. Median survival was 5.9 months. At this dose and schedule AZQ does not appear to have significant activity in recurrent endometrial cancer.

Aged↗
PubMed1989

Phase II study of diaziquone in untreated advanced gastric carcinoma. A Southwest Oncology Group Study.

Twenty-nine patients with a diagnosis of advanced adenocarcinoma of the stomach with gross unresectable or measurable residual disease and no prior therapy were entered into a study utilizing diaziquone (AZQ) in an intermittent 3-week schedule of 40 mg/m2. Of 28 eligible patients, 1 (4%) experienced a partial response, 7 (25%) had stable disease of no response, and 18 (64%) developed increasing disease. Two (7%) were unevaluable. Median survival was 3.8 months. Major toxicities were myelosuppression and gastrointestinal, 11 of which were considered to be life-threatening. AZQ used as a single intermittent agent appears to have no significant activity to warrant use in untreated advanced gastric carcinoma. However, recognizing the short plasma half-life of AZQ, significant responses by other schedules of administration are not precluded.

Adenocarcinoma↗
PubMed2002

Evaluation of the usefulness of percutaneous transhepatic portal catheterization for preoperatively diagnosing the localization of insulinomas.

INTRODUCTION: The precise intraoperative localization of insulinoma is essential for successful surgical management. AIMS: To assess the usefulness of measuring insulin levels by preoperative percutaneous transhepatic portal catheterization (PTPC) and intraoperative ultrasonography (US). METHODOLOGY: PTPC and other preoperative procedures (enhanced computed tomography [CT], arteriography, and US) were performed in eight patients with insulinoma based on our experience during the past 18 years. Intraoperative US was performed in six of the eight patients. RESULTS: PTPC was undertaken in all eight patients, and increased levels of insulin at the sites corresponding to tumors were observed in all patients. Intraoperative US was performed in six patients, which made it possible to detect insulinomas as hypoechoic masses in all of these patients. All tumors were found to exist as single entities. CONCLUSION: PTPC showed the highest diagnostic accuracy in detecting the number of and accurately localizing the tumors before surgery. Meanwhile, all findings from intraoperative US were identical to those of the resection samples, suggesting that this method is a highly reliable examination technique. We conclude that a combination of PTPC and intraoperative US may be essential for the successful surgical management of insulinomas.

Angiography↗
PubMed1988

A phase II study of diaziquone in childhood leukemia: a report from the Children's Cancer Study Group.

Diaziquone (aziridinylbenzoquinone, AZQ) was given by 30-min infusion at 25 mg/m2/day on a daily x 5 schedule to 16 children with acute lymphoblastic leukemia (ALL) in bone marrow relapse, 16 children with acute nonlymphocytic leukemia (ANLL) in bone marrow relapse, and 1 child with chronic myelocytic leukemia in blast crisis. None of the children achieved bone marrow remission. Five children (four with ALL and one with ANLL) were also evaluable for the response of central nervous system leukemia; all had a significant reduction in the cerebrospinal fluid blast count. Mild transient transaminase elevation was commonly seen. Grade 3 and 4 hyperbilirubinemia was seen in association with sepsis. AZQ was ineffective for induction of bone marrow remission as utilized in this study.

Adolescent↗
PubMed1980

Pulpal response to a temporary crown and bridge material in ferret teeth.

The histological effects of a temporary crown and bridge material (Scutan) on the pulp of canine teeth of ferrets was investigated at time intervals up to 6 months. After 24 h a moderate to severe pulpal response was observed which persisted up to 6 months. A case of contact sensitivity to Scutan is reported.

Animals↗