A folic acid derivative used as a rodenticide that has been shown to be teratogenic.
Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)
An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.
A peptide that is a homopolymer of glutamic acid.
An enzyme of the oxidoreductase class that catalyzes the reaction 7,8-dihyrofolate and NADPH to yield 5,6,7,8-tetrahydrofolate and NADPH+, producing reduced folate for amino acid metabolism, purine ring synthesis, and the formation of deoxythymidine monophosphate. Methotrexate and other folic acid antagonists used as chemotherapeutic drugs act by inhibiting this enzyme. (Dorland, 27th ed) EC 1.5.1.3.
An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.
A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.
An enzyme that catalyzes the conversion of 5-phosphoribosyl-1-pyrophosphate and hypoxanthine, guanine, or 6-mercaptopurine to the corresponding 5'-mononucleotides and pyrophosphate. The enzyme is important in purine biosynthesis as well as central nervous system functions. Complete lack of enzyme activity is associated with the LESCH-NYHAN SYNDROME, while partial deficiency results in overproduction of uric acid. EC 2.4.2.8.
The formaldehyde-inactivated toxin of Corynebacterium diphtheriae. It is generally used in mixtures with TETANUS TOXOID and PERTUSSIS VACCINE; (DTP); or with tetanus toxoid alone (DT for pediatric use and Td, which contains 5- to 10-fold less diphtheria toxoid, for other use). Diphtheria toxoid is used for the prevention of diphtheria; DIPHTHERIA ANTITOXIN is for treatment.
Large natural streams of FRESH WATER formed by converging tributaries and which empty into a body of water (lake or ocean).
A sphingolipidosis subtype that is characterized by the histological appearance of granulomatous deposits in tissues. It results from the accumulation of CERAMIDES in various tissues due to an inherited deficiency of ACID CERAMIDASE.
The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.
Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property.
Unforeseen occurrences, especially injuries in the course of work-related activities.
Databases devoted to knowledge about specific chemicals.
Exclusive legal rights or privileges applied to inventions, plants, etc.
Large collections of small molecules (molecular weight about 600 or less), of similar or diverse nature which are used for high-throughput screening analysis of the gene function, protein interaction, cellular processing, biochemical pathways, or other chemical interactions.
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.
Also known as articulations, these are points of connection between the ends of certain separate bones, or where the borders of other bones are juxtaposed.
A plasma protein that circulates in increased amounts during inflammation and after tissue damage.
Measurement of rate of settling of erythrocytes in anticoagulated blood.
The articulation between the head of one phalanx and the base of the one distal to it, in each finger.
A plant genus of the family ANNONACEAE. It has edible fruit and seeds which contain asitrocin, asitrilobins, and other tetrahydrofuran acetogenins.
A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).
Antineoplastic antibiotic obtained from Streptomyces peucetius. It is a hydroxy derivative of DAUNORUBICIN.
Polyketides of up to a few dozen carbons in length, formed by chain extension of multiple PROPIONATES and oxygenated to form tetrahydrofuran and lactone rings along the length of the chain. They are found in ANNONACEAE and other PLANTS. Related compounds cyclize to MACROLIDES.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA TOPOISOMERASES, TYPE I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.
Messages between computer users via COMPUTER COMMUNICATION NETWORKS. This feature duplicates most of the features of paper mail, such as forwarding, multiple copies, and attachments of images and other file types, but with a speed advantage. The term also refers to an individual message sent in this way.
Gram-negative gas-producing rods found in feces of humans and other animals, sewage, soil, water, and dairy products.
Gram-negative, capsulated, gas-producing rods found widely in nature. Both motile and non-motile strains exist. The species is closely related to KLEBSIELLA PNEUMONIAE and is frequently associated with nosocomial infections
A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.
A class of carbohydrates that contains five carbon atoms.
A characteristic symptom complex.
A member of the vitamin B family that stimulates the hematopoietic system. It is present in the liver and kidney and is found in mushrooms, spinach, yeast, green leaves, and grasses (POACEAE). Folic acid is used in the treatment and prevention of folate deficiencies and megaloblastic anemia.
Compounds based on 5,6,7,8-tetrahydrofolate.
A nutritional condition produced by a deficiency of FOLIC ACID in the diet. Many plant and animal tissues contain folic acid, abundant in green leafy vegetables, yeast, liver, and mushrooms but destroyed by long-term cooking. Alcohol interferes with its intermediate metabolism and absorption. Folic acid deficiency may develop in long-term anticonvulsant therapy or with use of oral contraceptives. This deficiency causes anemia, macrocytic anemia, and megaloblastic anemia. It is indistinguishable from vitamin B 12 deficiency in peripheral blood and bone marrow findings, but the neurologic lesions seen in B 12 deficiency do not occur. (Merck Manual, 16th ed)
A 4-hydroxylated metabolite of AFLATOXIN B1, one of the MYCOTOXINS from ASPERGILLUS tainted food. It is associated with LIVER damage and cancer resulting from its P450 activation to the epoxide which alkylates DNA. Toxicity depends on the balance of liver enzymes that activate it (CYTOCHROME P-450) and others that detoxify it (GLUTATHIONE S TRANSFERASE) (Pharmac Ther 50.443 1991). Primates & rat are sensitive while mouse and hamster are tolerant (Canc Res 29.236 1969).
Nitro-phenanthrenes occurring in ARISTOLOCHIACEAE and other plants. They derive from stephanine (APORPHINES) by oxidative ring cleavage. The nitro group is a reactive alkylator (ALKYLATING AGENTS) that binds to biological macromolecules. Ingestion by humans is associated with nephropathy (NEPHRITIS). There is no relationship to the similar named aristolochene (SESQUITERPENES).
Furano-furano-benzopyrans that are produced by ASPERGILLUS from STERIGMATOCYSTIN. They are structurally related to COUMARINS and easily oxidized to an epoxide form to become ALKYLATING AGENTS. Members of the group include AFLATOXIN B1; aflatoxin B2, aflatoxin G1, aflatoxin G2; AFLATOXIN M1; and aflatoxin M2.
A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.
A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)
Any of the monobasic inorganic or organic acids of sulfur with the general formula RSO(OH). (From McGraw Hill Dictionary of Scientific and Technical Terms, 4th ed)
A group of 3-hydroxy-4-keto-FLAVONOIDS.
Organic compounds which contain platinum as an integral part of the molecule.
The area covering the terminal portion of ESOPHAGUS and the beginning of STOMACH at the cardiac orifice.
The minimum acceptable patient care, based on statutes, court decisions, policies, or professional guidelines.
The use of two or more chemicals simultaneously or sequentially in the drug therapy of neoplasms. The drugs need not be in the same dosage form.
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.

Phase I study of escalating doses of edatrexate in combination with paclitaxel in patients with metastatic breast cancer. (1/155)

Motivated by the observation of preclinical synergy, a Phase I dose escalation study of edatrexate in combination with a 3-h paclitaxel infusion was performed in patients with advanced breast cancer to determine the maximum tolerated dose (MTD) of edatrexate and the toxicities associated with this combination and to report preliminary observations of efficacy with this novel combination. Thirty-six patients were enrolled in this Phase I trial. Thirty-five eligible patients were treated every 21 days in cohorts of at least three patients and were assessable for toxicity. One patient was ineligible due to hyperbilirubinemia. Stepwise dose escalations of edatrexate were administered until grade >3 nonhematological dose-limiting toxicities were reported. The initial dose level of edatrexate was 180 mg/m2; subsequent cohorts were treated with escalating doses of edatrexate (210, 240, 270, 300, 350, and 400 mg/m2). Edatrexate was administered by i.v. infusion over 1 h. Paclitaxel was administered 24 h later at a fixed dose of 175 mg/m2 as a 3-h infusion with standard dexamethasone, diphenhydramine, and cimetidine premedication. The MTD of edatrexate was reached at the 350 mg/m2 level in this study. Grade 3 diarrhea was seen in one patient at the 300 and 400 mg/m2 dose levels, requiring dose reductions. Two patients experienced grade 4 stomatitis at the 400 mg/m2 dose level and also required dose reduction, establishing the MTD as 350 mg/m2. Grade 3 nausea and vomiting were noted in two of three patients at the highest dose level. Of 35 patients, 4 patients reported grade 3 myalgias and 1 patient reported grade 3 neurosensory complaints, which were seen mostly at the 350 and 400 mg/m2 dose levels; however, 1 patient reported grade 3 myalgias at 180 mg/m2. No cumulative neurotoxicity was observed, and no patient experienced an allergic reaction to paclitaxel. In 23 patients with bidimensionally measurable disease, there were four complete (17%) and seven partial responses, with an overall response rate of 48% (95% confidence interval, 27-69%). All of the responses were seen in patients who had not received prior chemotherapy for stage IV disease. The median duration of response was not assessable because many responding patients went on to receive high-dose chemotherapy treatment with stem cell support. The combination of edatrexate and paclitaxel for treatment of metastatic breast cancer is a feasible and safe regimen. The MTD of edatrexate was 350 mg/m2 when combined with a 3-h infusion of paclitaxel (175 mg/m2) given 24 h later. Activity was noted even among patients who had relapsed shortly after receiving methotrexate- and/or doxorubicin-containing adjuvant regimens. Additional studies evaluating the sequences and dosing schema for this combination are warranted to improve the response proportion and define the duration of the response.  (+info)

Folylpolyglutamyl synthetase gene transfer and glioma antifolate sensitivity in culture and in vivo. (2/155)

BACKGROUND: Although antifolates are popular agents for use in chemotherapy, they display minimal toxicity against slow-growing tumors and are toxic to actively replicating cells in normal tissues. These drugs are converted intracellularly into polyglutamate derivatives by the enzyme folylpolyglutamyl synthetase (FPGS). Because tumors with high expression of FPGS often respond to nontoxic antifolate doses, we investigated whether augmenting tumoral FPGS activity by gene delivery would enhance tumoral antifolate sensitivity. METHODS: 9L rat gliosarcoma cells were stably transfected with a human FPGS complementary DNA (cDNA), producing 9L/FPGS cells. The sensitivity of these cells to the antifolates methotrexate and edatrexate was measured in culture and in subcutaneous tumors, as was their ability to increase the chemosensitivity of nearby nontransfected cells, i.e., a bystander effect. The antifolate sensitivity of nonselected cells transduced with a hybrid amplicon vector that expressed FPGS was also ascertained. RESULTS: In comparison with 9L cells, 9L/FPGS cells displayed enhanced sensitivity to 4-hour pulses of antifolate. Subcutaneous 9L/FPGS tumors responded as well to methotrexate given every third day as 9L tumors did to daily treatment. A modest bystander effect was observed with edatrexate treatment in culture and in vivo. The observed bystander effect appeared to result from the release of antifolates by transfected cells after the removal of extracellular drug. In culture, enhanced antifolate sensitivity was also seen in other stably transfected rodent and human glioma cell lines, including one with high pre-existing FPGS activity, and in canine and human glioblastoma cell lines transduced with a vector bearing FPGS cDNA. CONCLUSIONS: FPGS gene delivery enhances the antifolate sensitivity of several glioma cell lines and merits further evaluation as a therapeutic strategy.  (+info)

Phase I study of the sequential administration of edatrexate and paclitaxel in patients with advanced solid tumors. (3/155)

BACKGROUND: The antifolate edatrexate and the microtubule-stabilizing agent paclitaxel have both demonstrated single-agent activity in lung and breast cancer. In vitro, the sequential combination of edatrexate followed by paclitaxel produced synergistic antitumor effects. This trial was designed to find the maximum tolerated doses of edatrexate and paclitaxel when given every two weeks utilizing this sequential schedule. PATIENTS AND METHODS: Thirty-four patients with solid tumors received edatrexate intravenously on days 1 and 15 and paclitaxel intravenously as a three-hour infusion on days 2 and 16 of each 28-day cycle. Edatrexate was escalated from 40 to 120 mg/m2 and the paclitaxel dose fixed at 135 mg/m2. When the maximum-tolerated dose was not reached, edatrexate was fixed at 120 mg/m2 and paclitaxel escalated to 175 and 210 mg/m2. RESULTS: All 34 patients were assessable. The maximum tolerated doses were 120 mg/m2 of edatrexate and 210 mg/m2 of paclitaxel. Grade 3 myalgia, peripheral neuropathy, leukopenia, and an infusion-related reaction occurred. Eight patients with non-small-cell lung cancer and one with bladder cancer achieved major objective responses. CONCLUSIONS: The recommended phase II doses are 120 mg/m2 of edatrexate days 1 and 15 and 175 mg/m2 of paclitaxel as a three-hour infusion days 2 and 16 of a 28 day cycle. These results warrant phase II trials of the combination leading to phase III studies comparing the two drugs to a single agent to confirm the preclinical evidence of synergy.  (+info)

Dihydrofolate reductase from Kaposi's sarcoma-associated herpesvirus. (4/155)

Kaposi's sarcoma-associated herpesvirus (KSHV) is the first human virus known to encode dihydrofolate reductase (DHFR), an enzyme required for nucleotide and methionine biosynthesis. We have studied the purified KSHV-DHFR enzyme in vitro and analyzed its expression in cultured B-cell lines derived from primary effusion lymphoma (PEL), an AIDS-associated malignancy. The amino acid sequence of KSHV-DHFR is most similar to human DHFR (hDHFR), but the viral enzyme contains an additional 23 amino acids at the carboxyl-terminus. The viral DHFR, overexpressed and purified from E. coli, was catalytically active in vitro. The K(m) of KSHV-DHFR for dihydrofolate (FH(2)) was 2.4 microM, which is significantly higher than the K(m) of recombinant hDHFR (rhDHFR) for FH(2) (390 nM). K(m) values for NADPH were similar for the two enzymes, about 1 microM. KSHV-DHFR was inhibited by folate antagonists such as methotrexate (K(i): 200 pM), aminopterin (K(i): 610 pM), pyrimethamine (K(i): 29 nM), trimethoprim (K(i): 2.3 microM), and piritrexim (K(i): 3.9 nM). In all cases, K(i) values for these folate antagonists were higher for KSHV-DHFR than for rhDHFR. The viral enzyme was expressed at levels two- to tenfold higher than hDHFR in PEL cell lines as an early lytic cycle gene. KSHV-DHFR mRNA and protein appeared from 6 to 24 h after chemical induction of the KSHV lytic cycle. Epitope-tagged KSHV-DHFR and rhDHFR both localized to the nucleus of transfected cells, while other KSHV nucleotide metabolism genes localized to the cytoplasm. DHFR activity was not essential for viral replication in cultured PEL cells. Since hDHFR was not detectable in peripheral blood mononuclear cells (PBMCs), KSHV-DHFR may function to provide increased DHFR activity in vivo in infected cells that have little or none of their own enzyme.  (+info)

A spontaneous murine melanoma lung metastasis comprised of host x tumor hybrids. (5/155)

Cells from a lung metastasis, arising from Cloudman S91 melanoma cells implanted s.c. in the tail of a BALB/c nu/nu mouse, were comprised chiefly of host x tumor hybrids. These lung metastasis cells showed: (a) 30-40% increased DNA content; (b) resistance to 10(-4) M hypoxanthine, 4 x 10(-7) M aminopterin, and 1.6 x 10(-5) M thymidine (HAT) + G418; and (c) the presence in genomic DNA of genes for both wt and albino tyrosinase, reflecting the DBA/2J (Cloudman S91) and BALB/c mouse genotypes, respectively. Individual clones of lung metastasis cells expressed enhanced pigmentation, motility, and responsiveness to MSH/IBMX, a behavior similar to that recently reported for artificially generated melanoma x macrophage fusion hybrids. These similarities suggested that the host fusion partner generating the lung metastasis hybrids might have been a macrophage, although formal proof for this was not possible. The results provide the first direct evidence that host x tumor hybridization could serve as an initiating mechanism for melanoma metastasis.  (+info)

Trans-stimulation effects of folic acid derivatives on methotrexate transport by rat renal organic anion transporter, OAT-K1. (6/155)

We examined the pharmacological role of the renal organic anion transporter OAT-K1, which localizes predominantly in the brush-border membranes of proximal straight tubules, in the urinary excretion of methotrexate and the possibility of its contribution to "folinic acid rescue." With Madin-Darby canine kidney (MDCK) cells stably transfected with OAT-K1 cDNA, OAT-K1-mediated methotrexate accumulation was inhibited in the presence of various folic acid derivatives. These derivatives included aminopterin, 5-methyltetrahydrofolic acid, unlabeled methotrexate, folinic acid (citrovorum factor, leucovorin), and folic acid with apparent inhibition constant values of 0.5, 1.2, 1.8, 8.2, and 14.1 microM, respectively. In contrast, 10 microM taurocholic acid and sulfobromophthalein did not inhibit OAT-K1-mediated methotrexate accumulation. In addition, methotrexate efflux was stimulated in the presence of inwardly directed gradients of aminopterin, 5-methyltetrahydrofolic acid, unlabeled methotrexate, folinic acid, and folic acid, but not of uric acid, taurocholic acid, and glutathione, indicating that OAT-K1-mediated methotrexate efflux is stimulated by a folic acid derivatives exchange. In conclusion, OAT-K1 was suggested to enhance the apical efflux of highly accumulated methotrexate in tubular epithelial cells and contribute at least in part to folinic acid rescue by exchanging intracellular methotrexate for extracellular folinic acid.  (+info)

Phase I and pharmacokinetic study of 10-propargyl-10-deazaaminopterin, a new antifolate. (7/155)

The 10-deazaaminopterins are a new class of rationally designed antifolates demonstrating greater antitumor effects than methotrexate in murine tumor models and human tumor xenografts. Their design was aimed at improving membrane transport and polyglutamylation in tumor cells, resulting in increased intracellular accumulation and enhanced cytotoxicity. Compared with other 4-aminofolate analogues, 10-propargyl-10-deazaaminopterin (PDX) is the most efficient permeant for the RFC-1-mediated internalization and substrate for folylpolyglutamate synthetase. PDX demonstrates greater in vitro and in vivo antitumor efficacy than methotrexate or edatrexate. We undertook a Phase I study with PDX to identify the potential toxicities and define an optimal dose and schedule. Thirty-three patients were enrolled, all of whom had non-small cell lung cancer (NSCLC) and were treated previously with a median of two prior chemotherapy regimens. Initially, PDX was administered weekly for 3 weeks in a 4-week cycle. Mucositis requiring dose reduction and/or delay in the first cycle occurred in four of six patients treated at the initial dose level (30 mg/m2), making this the maximal tolerated dose for PDX given on this schedule. The treatment schedule was then modified to every 2 weeks. Twenty-seven patients were treated twice weekly with a total of 102 four-week cycles (median, 2 cycles/patient). Mucositis was the dose-limiting toxicity, with grade 3 and 4 mucositis occurring in the first two patients treated at the 170 mg/m2 dose level. Other toxicities were mild and reversible. No neutropenia was observed. The recommended Phase II dose is 150 mg/m2 biweekly. At that dose level, the mean area under the curve was 20.6 micromol x h, and the mean terminal half-life was 8 h. Two patients with stage IV NSCLC had major objective responses, and five patients had stable disease for 7 (two patients), 9 (one patient), 10 (one patient), and 13 months (one patient). PDX is a new antifolate with manageable toxicity and evidence of antitumor activity in NSCLC. A Phase II trial in NSCLC and a Phase I trial with paclitaxel are under way. These studies will also quantitate the expression of genes controlling internalization (RFC-1) and polyglutamylation of PDX in tumor cells as correlates of response.  (+info)

Co-administration of probenecid, an inhibitor of a cMOAT/MRP-like plasma membrane ATPase, greatly enhanced the efficacy of a new 10-deazaaminopterin against human solid tumors in vivo. (8/155)

Earlier studies from this laboratory have shown that the uricosuric agent probenecid (PBCD) will inhibit the extrusion of folate analogues from tumor cells mediated by a plasma membrane ATPase resembling the canicular multispecific organic anion transporter/multidrug resistance-related protein (MRP) family of ATP binding cassette transporters. This inhibition of this outwardly directed membrane ATPase has been shown to have a favorable impact upon the cellular pharmacokinetics, cytotoxicity, and efficacy of methotrexate in vivo. In an extension of these earlier studies, which had focused only on murine ascites tumors, we now report that parental co-administration of PBCD will also enhance net intracellular accumulation in vitro and intracellular persistence in vivo of a new folate analogue, 10-propargyl-10-deazaaminopterin (PDX) in tumor cells. This resulted in marked enhancement of the efficacy of PDX against murine and human lung neoplasms and human prostate and mammary neoplasms growing as solid tumors in mice. As possible ATPases targeted by PBCD, all of these tumors expressed MRP-1, -4, and -7 genes, with expression of MRP-4 being greatest in each case. Four other MRP genes were expressed to a variable extent in some tumors but not others. The therapeutic enhancement of PDX by PBCD was manifested as tumor regression, where PDX alone was only growth inhibitory (A549 NSCL tumor), or as a substantial increase (3-4-fold) in overall regression and/or number of complete regressions (Lewis and LX-1 lung, PC-3 and TSU-PR1 prostate, and MX-1 mammary tumors) compared to PDX alone. Also, only in the case of PDX with PBCD, a significant number of mice transplanted with LX-1 or MX-1 tumors that experienced complete regression did not have regrowth of their tumor. In view of these results, clinical trials of this therapeutic modality appear to be warranted, especially in the case of new more efficacious folate analogues that are also permeants for this canicular multispecific organic anion transporter/MRP-like plasma membrane ATPase.  (+info)

Fetal aminopterin syndrome is a condition affecting babies whose mothers were exposed to the chemical aminopterin or methotraxate during pregnancy. Only about 50 cases have been reported. Babies exposed to aminopterin or methotraxate during development can be born with developmental delays such as inability to properly grow, abnormal arms or legs, and changes to the face or skull. Symptoms of fetal aminopterin syndrome depend on how early in pregnancy the woman is exposed to aminopterin or methotraxate and the dosage of the medication being used. There is no cure for fetal aminopterin syndrome, though symptoms can be managed. Aminopterin is no longer used, but methotraxate may still be used to treat some conditions such as cancer. Pregnant women should consult a physician before taking medications with either chemical ...
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia. - Mechanism of Action & Protocol.
Aminopterin (4-aminopterojska kislina) je 4-amino derivat folne kisline, ki izkazuje imunosupresivno in citostatično delovanje. Aminopterin je sintezni derivat pterina. Deluje kot encimski zaviralec, ker se veže na vezišča encima dihidrofolat reduktaze (namesto fiziološkega substrata - folne kisline) in s tem zavre sintezo tetrahidrofolata. Posledično pride do motenj nastajanja nukleotidov in s tem do zaviranja sinteze DNK, RNK in beljakovin. Aminopterin se je nekoč uporabljal za zdravljenje raka, dandanes pa ga je povsem nadomestil metotreksat, ki je spojina s podobno strukturo. Ponekod se še vedno uporablja kot rodenticid. Leta 2007 se je v ZDA pojavil škandal z aminopterinom, ko so v okoli 100 vrst hrane za pse in mačke dokazali znatne količine spojine (nad 40 ppm). Hrano so umaknili iz prodaje. Aminopteridina pri živih živalih ni mogoče dokazati. Obstajajo sumi na nefrotoksično delovanje (strupen učinek na ledvice), vendar nedvomnih dokazov o njegovem delovanju na zdravje ...
Ovaj lek je otkrio Dr. Yellapragada Subbarao, a prvi je koristio njegovu antifolatnu aktivnost Sidni Farber 1947. da indukuje remisiju kod dece sa leukemijom.[3][4] Aminopterin je kasnije prodavala kompanija Lederle Laboratories (Pearl River, Njujork) u SAD od 1953 do 1964 za pedijatrijsku leukemiju. Ta kompanije je u toku istog perioda prodavala blisko srodni antifolat metotreksat. Lederle Laboratories je zatim obustavila prodaju aminopterina u korist metotreksata zbog proizvodnih razloga. Aminopterin je u toku svog tržišnog veka korišćen i za tretman psorijaze u SAD. Ovaj lek je doveo do dramatičnog čišćenja lezija.[5]. Upotreba aminopterina u tretmanu raka je zamenjena 1950-tih godina metotreksatom zbog boljeg terapeutskog indeksa metotreksata.[6] Nedavno je došlo do obnavljanja interesa u aminopterin, tako da su u toku klinička ispitivanja sa ciljom suzbijanja leukemije.[7]. Ovo jedinjenje je bilo istraženo kao abortifacijent 1960-tih i ranije, ali je bilo asocirano sa ...
Four folate analogues, methotrexate, aminopterin, 10-deazaaminopterin, and 10-ethyl-10-deazaaminopterin were assessed for their ability to be metabolized to poly-γ-glutamyl derivatives in three tumor lines which vary in their sensitivity to these agents. Cytotoxicity of the four analogues against the murine L1210 leukemia and the human Manca B cell leukemia, as determined by a 3-h clonogenic assay, showed aminopterin and the two 10-deazaaminopterin compounds to be approximately equivalent for each cell type and were 3- to 10- (L1210) and 7- to 14-fold (Manca) more potent than methotrexate. In murine Sarcoma 180 cells, 10-ethyl-10-deazaaminopterin and aminopterin were similarly potent but were 5- to 10-fold more potent than 10-deazaaminopterin and 40- to 80-fold more potent than methotrexate. These results could be explained in part by the differences in transport properties and substrate activities for polyglutamylation for each analogue in these cell types.. Initial rates of polyglutamate ...
Pralatrexate is given as an infusion into your vein over 3 to 5 minutes under the supervision of your doctor or nurse. Pralatrexate is usually given once a week for 6 weeks, with no treatment on the 7th week to complete the 7-week cycle. Several treatment cycles of pralatrexate may be given depending on your response to treatment. Prior to being given pralatrexate, your doctor will advise you to take certain medicines or vitamin supplements before starting and while being on treatment to help minimise side effects.. Pralatrexate is approved by the TGA for the following indication:. The treatment of adult patients with peripheral T-cell lymphoma (nodal, extranodal, and leukaemic/disseminated) who have progressed after at least one prior therapy.. Pralatrexate is listed on the PBS from April 1st, 2018. Breaking News. Pralatrexate may have the following side effects:. ...
Takeda Remains Committed to Continuing the Ongoing Alisertib Clinical Development Program Cambridge, MA, May 12, 2015 and Osaka, Japan, May 13, 2015 - Takeda Pharmaceutical Company Limited...
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies. ...
PRIMARY OBJECTIVES:. I. To determine the overall response rate in patients with advanced esophago-gastric cancer (EGC) to combination pralatrexate and oxaliplatin.. SECONDARY OBJECTIVES:. I. To examine the toxicity and tolerability of this regimen. II. To determine the time-to-progression and overall survival using this regimen.. III. To examine whether functionally relevant polymorphisms of genes of the folate metabolism pathway correlate with efficacy and toxicity of pralatrexate.. IV. To examine whether response to pralatrexate can be predicted by micro-ribonucleic acid (microRNA) expression profiling of the epithelial component of the tumor.. OUTLINE:. Patients receive pralatrexate intravenously (IV) over 3-5 minutes and oxaliplatin IV over 2 hours on day 1. Courses repeat every 2 weeks in the absence of disease progression or unacceptable toxicity. Oxaliplatin will be discontinued after 12 courses.. After completion of study treatment, patients are followed up for 30 days and then ...
...NCCN has added pralatrexate (Folotyn(TM) Allos Therapeutics Inc.) to...FORT WASHINGTON Pa. Oct. 15 -- Upon the rece...The updated NCCN Guidelines have added pralatrexate as a second-line t...Peripheral T-cell lymphoma is a rare form of non-Hodgkins lymphoma th...,NCCN,Updates,NHL,Guidelines,Following,FDA,Approval,of,Pralatrexate,medicine,advanced medical technology,medical laboratory technology,medical device technology,latest medical technology,Health
In the current study we addressed the question as to whether membrane translocation in the overall process of FGF-2 externalization requires protein unfolding. For this purpose we combined a FACS-based in vivo system reconstituting FGF-2 export (Engling et al., 2002) with a modified FGF-2-GFP reporter molecule that contains the DHFR domain at its C-terminus. The membrane-permeable folate analogue aminopterin (Eilers and Schatz, 1986; Wienhues et al., 1991) was used to stabilize the DHFR domain in vivo, which allows us to analyse a potential need for protein unfolding during FGF-2 export. The principal finding of this study is that membrane translocation of FGF-2 by living cells apparently occurs in a folded conformation as an FGF-2-GFP-DHFR fusion protein is efficiently exported in the presence of aminopterin. Importantly, on the basis of antibodies directed against the N-terminal part (anti-GFP) of the reporter, as well as antibodies directed against the extreme C-terminus (anti-His), we showed ...
In June 3, 1948, The New England Journal of Medicine published a study by Sidney Farber, MD, showing that a synthetic compound, 4-aminopteroylglutamic acid (aminopterin), could induce remissions in seriously ill children with acute leukemia.1 Although the study was small-just 16 children-10 showed clinical, hematologic, and pathologic evidence of improvement. Even though the childrens remissions were short-lived, Dr. Farbers findings were so groundbreaking-until then, no drug had proved effective against non-solid tumor cancers-they ushered in the era of chemotherapeutics, chemical agents that could stop cancer cells from growing and replicating, in effect killing them.. Aminopterin was later replaced by methotrexate, a similar but more effective folic acid antagonist with fewer side effects, which is still used today in the treatment of leukemia and other blood and solid tumor cancers. Nevertheless, the results of Dr. Farbers study earned him the title, the Father of Modern ...
days in Clicks medium with 0.5% NMS and then placed in IL-2 for 3 days to expand. T cell clones and lines can be successfully fused following an analogous schedule, in this case the clone or line is set up in a standard re-stimulation flask with 5.0 X 105 T cells, 2.0 X 107 irradiated NOD spleen cells in 20 ml DMEM/10% FBS with 50U/ml IL-2. The cultures are incubated for four days at which point they are subjected to Lympholyte M separation and culture for 3 days in 50 U/ml IL-2, the cells are then counted and washed as below.. Hybrid cells are selected by culturing the fused cells in hypoxanthine/aminopterin/thymidine (HAT). The aminopterin component of HAT inhibits a key enzyme in purine and ...
Within the last decade, weve witnessed the emergence from the oral non-vitamin K oral anticoagulants (NOACs), that have numerous advantages weighed against the vitamin K antagonists, particularly their insufficient dependence on monitoring; because of this their use is definitely increasing. checks, thromboelastometry guidelines buy Aminopterin and thrombin-generation indices induced by rivaroxaban and apixaban.34 Antifibrinolytic Providers. Tranexamic acidity inhibits fibrinolysis therefore stabilisng fibrin clots. Nevertheless, its prothrombic potential in NOAC-associated blood loss is unfamiliar. buy Aminopterin Haemodialysis. Dabigatran could be taken off the blood flow by haemodialysis in individuals with major blood loss or surgical treatments. This approach requires 4C6 hours, and it is more appealing in individuals with end-stage renal disease and overdosing.46 Expert Opinion: What Should We Make use of?23,34 Its important to check out the exact period of last NOAC intake. Predicated ...
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Term] id: EDAM:0002078 name: Sequence range format namespace: format def: Format used to specify range(s) of sequence positions. subset: format is_a: EDAM:0002350 ! Format (typed) relationship: is_format_of EDAM:0001017 ! Sequence range [Term] id: EDAM:0002571 name: Raw sequence format namespace: format def: Format of a raw molecular sequence (i.e. the alphabet used). subset: format is_a: EDAM:0002350 ! Format (typed) relationship: is_format_of EDAM:0000848 ! Raw sequence [Term] id: EDAM:0001921 name: Alignment format namespace: format def: Data format for molecular sequence alignment information. subset: format is_a: EDAM:0002350 ! Format (typed) relationship: is_format_of EDAM:0000863 ! Sequence alignment [Term] id: EDAM:0001919 name: Sequence record format namespace: format def: Data format for a molecular sequence record. subset: format is_a: EDAM:0002350 ! Format (typed) relationship: is_format_of EDAM:0000849 ! Sequence record [Term] id: EDAM:0002057 name: Sequence trace format namespace: ...
This phase II trial evaluated the efficacy of pralatrexate plus oxaliplatin in the treatment of patients with unresectable or metastatic oesophageal, stomach,
FOLOTYN (Pralatrexate) drug information & product resources from MPR including dosage information, educational materials, & patient assistance.
On Friday, the U.S. Food and Drug Administration said recalled pet foods contained melamine, a chemical used to make plastics, but that its tests failed to confirm the presence of a rat poison, aminopterin, reported by the New York State Food Laboratory. The FDA said it also found melamine in wheat gluten used as an ingredient in the wet-style products. Still, it was not immediately clear whether the melamine was the culprit in the deaths.. ...
In March 2007, the most lethal pet food in history was the subject of the largest recall ever. Menu Foods recalled more than 100 brands including Iams, Eukanuba, Hills Science Diet, Purina Mighty Dog, and many store brands including Wal-Marts. Thousands of pets were sickened (the FDA received more than 17,000 reports) and an estimated 20% died from acute renal failure caused by the food. Cats were more frequently and more severely affected than dogs. The toxin was initially believed to be a pesticide, the rat poison aminopterin in one of the ingredients. In April, scientists discovered high levels of melamine, a chemical used in plastics and fertilizers, in wheat gluten and rice protein concentrate imported from China. The melamine had been purposefully added to the ingredients to falsely boost their protein content. Subsequent tests revealed that the melamine-tainted ingredients had also been used in feed for cows, pigs, and chickens and thousands of animals were quarantined and destroyed. ...
Term] id: EDAM:0000850 name: Sequence set namespace: data def: A collection of multiple molecular sequences and associated metadata that do not (typically) correspond to molecular sequence database records or entries and which (typically) are derived from some analytical method. [EDAM:EBI EMBRACE definition] comment: This term may be used for arbitrary sequence sets and associated data arising from processing. subset: data is_a: EDAM:0002955 ! Sequence report [Term] id: EDAM:0001234 name: Sequence set (nucleic acid) namespace: data def: Any collection of multiple nucleotide sequences and associated metadata that do not (typically) correspond to common sequence database records or database entries. [EDAM:EBI EMBRACE definition] subset: data is_a: EDAM:0000850 ! Sequence set is_a: EDAM:0002977 ! Nucleic acid sequence [Term] id: EDAM:0001240 name: PCR primers namespace: data def: Oligonucleotide primer(s) for PCR and DNA amplification, for example a minimal primer set. [EDAM:EBI EMBRACE ...
The goal of this clinical research study is to learn if it is safe to give pembrolizumab in combination with romidepsin to patients with peripheral T-cell
Term] id: EDAM:0000850 name: Sequence set namespace: data def: A collection of multiple molecular sequences and associated metadata that do not (typically) correspond to molecular sequence database records or entries and which (typically) are derived from some analytical method. comment: This term may be used for arbitrary sequence sets and associated data arising from processing. subset: data is_a: EDAM:0002955 ! Sequence report [Term] id: EDAM:0001234 name: Sequence set (nucleic acid) namespace: data def: Any collection of multiple nucleotide sequences and associated metadata that do not (typically) correspond to common sequence database records or database entries. subset: data is_a: EDAM:0000850 ! Sequence set is_a: EDAM:0002977 ! Nucleic acid sequence [Term] id: EDAM:0001240 name: PCR primers namespace: data def: Oligonucleotide primer(s) for PCR and DNA amplification, for example a minimal primer set. subset: data is_a: EDAM:0001234 ! Sequence set (nucleic acid) [Term] id: EDAM:0001246 ...
Several HDAC inhibitors have been studied in clinical trials for non-Hodgkin lymphoma. However, only three HDAC inhibitors (romidepsin, vorinostat and belinostat) have received approval. Vorinostat was granted regular approval for third-line cutaneous T-cell lymphoma based on two open-label trials (one was a single-arm trial and the other assessed several dosing regimens) achieving ORRs of 30% (median DoR was not reached but estimated to exceed 6 months) and 24% (median DoR of 106 days).. The accelerated approval of belinostat was based on efficacy and safety data from a single-arm phase II trial. With the approval of belinostat, three drugs are now approved for the treatment of relapsed or refractory PTCL under the accelerated approval regulations: pralatrexate in 2009, romidepsin in 2011, and belinostat in 2014. Although cross-study comparisons must be interpreted with caution, the ORRs were similar for the three drugs: belinostat (ORR: 26%, CR: 11%, DoR: 8.4 months), pralatrexate [ORR: 27%, ...
Online lymphoma resource for healthcare professionals, providing information, news & support relating to lymphoma, Hodgkin & non Hodgkin disease
This drug may make you feel generally unwell. This is not uncommon, as chemotherapy can affect healthy cells as well as cancer cells. Report any side effects. Continue your course of treatment even though you feel ill unless your doctor tells you to stop.. Call your doctor or health care professional for advice if you get a fever, chills or sore throat, or other symptoms of a cold or flu. Do not treat yourself. This drug decreases your bodys ability to fight infections. Try to avoid being around people who are sick.. This medicine may increase your risk to bruise or bleed. Call your doctor or health care professional if you notice any unusual bleeding.. Do not become pregnant while taking this medicine or for 6 months after the last dose. Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Men should not father a child while taking this medicine or for 3 months after the last dose. ...
Well, you didnt, did you? Nalgol bit out, thoroughly disgusted. First the strike team, now Oissan. Get back to work. We still have an hour or two before the battle out there winds down to where well be entering it. VOTF p.651. In other words, Han Solo figured that a single Star Destroyer could finish off the warring fleets by itself and then burn off Bothawui, all with no survivors, no witnesses, and Nalgol confirmed this plan. The three ISDs were just insurance; it is quite obvious from Solos interpretation of the plan that its common knowledge in the New Republic that a single Star Destroyer is capable of doing this on its own. Enough of your lies and evasions, Edam. Stand up and debate like a man.. Or it is common misinformation. Everytime we see ISDs and similar ships try to do this they take hours to do it - the whole operation with 10x the capacity for damage is expected to take hours. 100 VSDs attacking Khomm did very little damage in half an hour. When Boosters ISD slagged the ...
Learn about the potential side effects of Folotyn (pralatrexate). Includes common and rare side effects information for consumers and healthcare professionals.
Looking for online definition of pralatrexate in the Medical Dictionary? pralatrexate explanation free. What is pralatrexate? Meaning of pralatrexate medical term. What does pralatrexate mean?
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RATIONALE: Pralatrexate may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Drugs used in chemotherapy, such as f
Chemotherapeutic agents: Chemotherapy, Pawpaw, Biosynthesis of doxorubicin, Camptothecin, Epothilone, Aminopterin, ABVD, Cyclophosphamide von Source: Wikipedia bei AbeBooks.de - ISBN 10: 1157367399 - ISBN 13: 9781157367390 - Books LLC, Wiki Series - 2011 - Softcover
During the early phases (phases 1 and 2), researchers assess safety, side effects, optimal dosages and risks/benefits. In the later phase (phase 3), researchers study whether the treatment works better than the current standard therapy. They also compare the safety of the new treatment with that of current treatments. Phase 3 trials include large numbers of people to make sure that the result is valid. There are also less common very early (phase 0) and later (phase 4) phases. Phase 0 trials are small trials that help researchers decide if a new agent should be tested in a phase 1 trial. Phase 4 trials look at long-term safety and effectiveness, after a new treatment has been approved and is on the market. ...
A Dutch import made with part-skim cows milk for a rich, buttery flavor with a hint of sweetness, this cheese has a smooth, firm texture. Boars Head® Edam Cheese is inspired by cheese-making traditions that originated in Holland more than eight centuries ago.
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The Department comprises a number of disciplines from the study of the earliest civilizations to the philosophy of the mind, from world literature to the study of comparative mythology and great religions of the world, from the beginning of theatre in ancient Greece to the latest Broadway plays and Hollywood movies, from music through the ages to the appreciation of art ...
Purpose: Pralatrexate is a folic acid analogue metabolic inhibitor similar to methotrexate, which has shown tolerability and efficacy with an overall response rate of 45% in a phase I dose deescalation study of patients with relapsed/refractory cutaneous T-cell lymphoma (CTCL).. Experimental Design: The object of this phase I/II open-label, multicenter clinical trial was to determine the MTD and recommended dose of pralatrexate plus oral bexarotene in 34 patients with relapsed/refractory CTCL who had failed prior systemic therapies. Pralatrexate was administered by intravenous push at 15 mg/m2 given weekly 3 weeks out of 4 weeks with daily oral bexarotene (150 or 300 mg/m2), levothyroxine, atorvastatin, folate, and with B12 every 2 months.. Results: At the MTD of 15 mg/m2 bexarotene and 15 mg/m2 pralatrexate, the response rate was 60% [4 complete responses (CR), 14 partial responses (PR)], the maximum observed response duration was 28.9+ months, and duration of response for 4 CRs ranged from 9.0 ...
Purpose The positron-emitting tomography (PET) tracer, 124I-cG250, directed against carbonic anhydrase IX (CAIX) shows promise for pre-surgical analysis of very clear renal cell carcinoma (cRCC) [1, 2]. two tracers endocytosis, 124I-iodotyrosine is expelled through the cell after lysosomal degradation [7] rapidly. Conversely, residualizing radiometals such as for example 111In and 177Lu are maintained from the cell by means of low-molecular pounds catabolites [8]. This trend has been proven to possess clinical outcomes for cG250/CAIX imaging; for instance, Brouwers, performed a primary intra-patient assessment of single-photon Pralatrexate emission computed tomography imaging of 131I-cG250 and 111In-cG250 in RCC metastases and discovered that the total amount of lesions exposed was greater using the 111In-labeled tracer, because of the higher activity in the lesions and the bigger tumor-to-blood ratios [9] general. The longer-lived radiometal 89Zr offers emerged as a good option to 124I, due to ...
Pralatrexate (PDX, 10-propargyl 10-deazaaminopterin) is a novel anti-folate agent that is approved for use in relapsed peripheral T cell lymphoma (PTCL). It is distinguished from the parent drug methotrexate (MTX) by having significantly greater affinity for the reduced folate carrier (RFC)-1, the principle transporter that internalize anti-folates, as well as broader efficacy, which strongly suggests that PDX has mechanisms of action beyond inhibition of nucleotide synthesis. Given the activity of PDX in aggressive lymphoid malignancies such as PTCL, we examined the activity of this agent in preclinical models of multiple myeloma (MM), a plasma cell malignancy that is currently incurable. We examined the cytotoxic activity of anti-folates in vitro against a panel of human multiple myeloma cell lines (HMCL) and showed that PDX induced dose-dependent apoptotic cell death in a subset of these. In sensitive cell lines (MM.1s and ARH-77) PDX demonstrated significantly greater potency at 48 hours ...
Sterigmatocystin (STG), a biosynthesis precursor of aflatoxin B1, is well known for its toxic and carcinogenic effects in humans and animals. STG derivatives and protein conjugates are needed for generation of monoclonal antibodies (mAbs). This work describes a reliable and fast synthesis of novel STG derivatives, based on which novel STG bovine serum albumin conjugates were prepared. With the novel STG bovine serum albumin conjugates, three sensitive and specific mAbs against STG, named VerA 3, VerA 4, and VerA 6, were prepared by semi-solid hypoxanthine/aminopterin/thymidine (HAT) medium using a modified two-step screening procedure. They exhibited high affinity for STG and no cross-reactivity (CR) with aflatoxins B1, B2, G1, G2, and M1. Based on the most sensitive antibody VerA 3, an ultra-sensitive competitive enzyme-linked immunosorbent assay (ELISA) was developed for STG in wheat, maize, and peanuts. Assays were performed in the STG-GA-BSA-coated (0.5 g mL(-1)) ELISA format, in which the ...
Find public databases by data type Version: EMBOSS:6.5.0.0 Standard (Mandatory) qualifiers: [-query] string List of EDAM data keywords (Any string) [-outfile] outresource [*.drfinddata] Output data resource file name Additional (Optional) qualifiers: (none) Advanced (Unprompted) qualifiers: -sensitive boolean [N] By default, the query keywords are matched against the EDAM term names (and synonyms) only. This option also matches the keywords against the EDAM term definitions and will therefore (typically) report more matches. -[no]subclasses boolean [Y] Extend the query matches to include all terms which are specialisations (EDAM sub-classes) of the matched type. Associated qualifiers: -outfile associated qualifiers -odirectory2 string Output directory -oformat2 string Data resource output format General qualifiers: -auto boolean Turn off prompts -stdout boolean Write first file to standard output -filter boolean Read first file from standard input, write first file to standard output -options ...
DBL Calcium Folinate is a medicine available in a number of countries worldwide. A list of US medications equivalent to DBL Calcium Folinate is available on the Drugs.com website.
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The folic acid antagonists, aminopterin and then methotrexate, have been the primary systemically administered drugs for the treatment of severe psoriasis for 25 years. Methotrexate was finally approved by the FDA 5 years ago and was recently estimated to be used for approximately 25 000 psoriatic patients annually. With the small but chronic doses used for psoriasis, methotrexate has been relatively safe, except for a limited occurrence of significant hepatotoxicity. The good to excellent results obtained in most patients must, therefore, be weighed against the small risk of liver damage. Methotrexate has also been used with some effectiveness in several other dermatologic conditions, including mycosis fungoides, dermatomyositis, pityriasis rubra pilaris, and others, although they are not yet FDA-approved indications. The recent successful introduction of photochemotherapy (psoralen and ultraviolet light) for moderate and severely affected psoriatics will probably lead to a substantial decrease ...
Learn more about Methotrexate at Doctors Hospital of Augusta Alternate Names : Amethopterin MTX Trade Names : Immunex Folex PFS Rheumatrex ...
Learn more about Methotrexate at Doctors Hospital of Augusta Alternate Names : Amethopterin MTX Trade Names : Immunex Folex PFS Rheumatrex ...
در این پژوهش، امکان به کارگیری پایه های زئولیتی و تاثیر نوع های گوناگون آن بر روی ویژگی های کاتالیستی و عملکرد راکتوری نانوکاتالیست کروم اکسید برای استفاده در فرایند هیدروژن گیری اکسایشی اتان به کمک کربن دی اکسید مورد ارزیابی قرار گرفت. در این راستا، شماری از کاتالیست های کروم اکسید دارای 4/3 % وزنی کروم با تلقیح پایه های زئولیتی انتخاب شده کلینوپتیلولیت، SAPO-34 و HZSM-5 تهیه شدند. بدین منظور، کلینوپتیلولیت خریداری شد و پایه های SAPO-34 و HZSM-5 به روش هیدروترمال تهیه شدند که آنالیزهای XRD، FESEM، BET و EDX تهیه موفقیت آمیز آن ها را تایید کردند. تصویرهای FESEM تشکیل کلوخه های ...
Background: Amethopterin is a folic acid antagonist which used as a chemotherapeutic agent and its anti-oxidant activity is used to treat many cancer types. This study aimed to determine the possible protective effects of L-carnitine against Amethopterin induced large intestine toxicity. Methodology: A total 60 male albino rats were equally divided into six groups; the first and second groups were the control and L-carnitine groups respectively while the 3rd group was Amethopterin rat group; the 4th and 5th groups were co- and post- treated Amethopterin rat with L-carnitine respectively and the 6th group was self treated Amethopterin rat group. Results: Glutathione, catalase and total protein levels in Amethopterin and self-treated groups showed a significant decrease when compared with control group, while MDA levels in Amethopterin and self-treated groups showed a significant increase when compared with control group. Many of abnormalities as colonic epithelial cell damage in the form of epithelial
Synonyms for antifolate in Free Thesaurus. Antonyms for antifolate. 6 synonyms for folic acid: folacin, folate, pteroylglutamic acid, pteroylmonoglutamic acid, vitamin Bc, vitamin M. What are synonyms for antifolate?
Robbie was really happy to be diagnosed with pulmonary tuberculosis. Before he arrived he was convinced he had lung cancer. Robbie is in his late 50s, he was born in Glasgow and left school at fifteen with no qualifications. His father was a shipbuilder on the Clyde. Robbie thought he would do the same, but…
Emazian B12 Injections information about active ingredients, pharmaceutical forms and doses by Pfizer, Emazian B12 Injections indications, usages and related health products lists
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Learn more about Methotrexate at LewisGale Regional Health System Alternate Names : Amethopterin MTX Trade Names : Immunex Folex PFS Rheumatrex ...
Lichter, sneller en betere rijeigenschappen - de Epic Hardtail Comp Carbon zet de wereld van XC hardtails op zijn kop. Met een gewicht van 1175 gram is dit een van de lichtste frames die we ooit hebben gemaakt. Om dit lage gewicht te bereiken, hebben we gebruikt gemaakt van onze ongeëvenaarde FACT 10m carbon vezels. Daarnaast hebben we elementen van het Rider-First Engineered™ concept op het nieuwe frame toegepast, net als bij enkele van onze racefietsen wordt elke framemaat individueel ontworpen. Hierdoor kunnen we voor elke maat de perfecte balans tussen gewicht, stijfheid en rijeigenschappen bereiken. We hebben op de geometrie gefinetuned om voor nog meer snelheid en stabiliteit te zorgen. Een minder steile balhoofdbuis, een langere bovenbuis en gecorrigeerde hoek van de zadelbuis zorgen voor een geometrie die nog meer vertrouwen geeft. Daarnaast hebben de we inbouwbreedte vergroot naar 12x148mm en hebben we het frame voorzien van interne split-housing kabelvoering. Voor de afmontage hebben we
... hypoxanthine-aminopterin-thymidine medium) for roughly 10 to 14 days. Aminopterin blocks the pathway that allows for nucleotide ...
Exposing cells to aminopterin (a folic acid analogue, which inhibits dihydrofolate reductase, DHFR), makes them unable to use ... The selective culture medium is called HAT medium because it contains hypoxanthine, aminopterin and thymidine. This medium is ...
Effect of folic acid, aminopterin and vitamin K on growth of roots in Allium cepa. Proc. Soc. Exp. Biol. Med. 74:310-12 The ...
Realizing this, he attempted to use a folate antagonist, aminopterin, to block the function of folic acid in patients with ... In 1947, Farber conducted a clinical trial on aminopterin on 16 children, 10 of which eventually achieved temporary remission. ... aminopterin)". New England Journal of Medicine. 238 (23): 787-793. doi:10.1056/nejm194806032382301. PMID 18860765.CS1 maint: ... he carried out both the preclinical and clinical evaluation of aminopterin (synthesized by Yellapragada Subbarow). He showed ...
His team gave 16 infants and children with acute lymphoblastic leukemia a folic acid inhibitor, aminopterin-10 showed ... Aminopterin)". New England Journal of Medicine. 238 (23): 787-93. doi:10.1056/NEJM194806032382301. PMID 18860765. Zoll, PM ( ...
Farber was able to use a drug of this type, aminopterin, to achieve a temporary remission in childhood leukemia. In the early ...
By 1947 Boston pathologist Sidney Farber believed from past experiments that aminopterin, a folic acid mimic, could potentially ...
Yellapragada Subbarow (of Lederle lab and his friend and colleague at Harvard Medical School) to supply Aminopterin and later ... Sidney Farber received the Lasker in 1966 for his 1947 discovery that a combination of aminopterin and methotrexate, both folic ...
... known for the synthesis of the first ever chemotherapeutic drug aminopterin, and subsequently methotrexate. He is also known ...
... aminopterin, melamine (a plastic precursor that may also be used as a fertiliser), and cyanuric acid (which is commonly used to ...
... aminopterin - AML - amonafide - amoxicillin - amphotericin B - ampulla - ampulla of Vater - amputation - amsacrine - amylase - ...
6-Mercaptopurine 6-Thioguanine Aminopterin Arsenic trioxide Asparaginase Cladribine Clofarabine Cyclophosphamide Cytosine ...
... cerebro vascular Fetal acitretin syndrome Fetal akinesia syndrome X linked Fetal alcohol syndrome Fetal aminopterin syndrome ...
It is not to be confused with Aminopterin.. Methotrexate (MTX), formerly known as amethopterin, is a chemotherapy agent and ... In 1947, a team of researchers led by Sidney Farber showed aminopterin, a chemical analogue of folic acid developed by ... Animal studies published in 1956 showed the therapeutic index of methotrexate was better than that of aminopterin, and clinical ... use of aminopterin was thus abandoned in favor of methotrexate. In 1951, Jane C. Wright demonstrated the use of methotrexate in ...
Aminopterin, a cytostatic drug with anti-folate effect, was used during the 1950s and 1960s to induce therapeutic abortions. In ... some cases the abortion didn´t happen, but the newborns suffered a fetal aminopterin syndrome consisting of growth retardation ...
... using aminopterin. This, and another antifolate drug, methotrexate used by Dr. Farber, were discovered and supplied by Dr. ...
Aminopterin, a cytostatic drug with antifolate effect, was used during the 1950s and 1960s to induce therapeutic abortions. In ... some cases, the abortion did not happen, but the newborns suffered a fetal aminopterin syndrome consisting of growth ...
Zlite celice gojimo nato v gojišču HAT (H = hipoksantin, A = aminopterin, T = timidin), v katerem preživijo samo hibridne ... Pot de novo, po kateri se formilne ali metilne skupine prenesejo iz aktivirane oblike tetrahidrofolata, blokira aminopterin, ...
... aga leiti folaadi antagonistid aminopterin ja amethopterin, rajas tee maailma esimese vähiravimi aminopterin'i avastamisele ( ...
Aminopterin je sintetički derivat pterina. Aminopterin dejstvuje kao inhibitor enzima dihidrofolat reduktaze. Njegov afinitet ... Aminopterin je u toku svog tržišnog veka korišćen i za tretman psorijaze u SAD. Ovaj lek je doveo do dramatičnog čišćenja ... No Aminopterin in Tissues of Animals Killed by Recalled Pet Food". PRNewsWire. 30. 3. 2007. Приступљено 14. 04. 2007.. ... Aminopterin i metotreksat su široko korišćeni u selekciji medija (kao što je HAT medijum) za ćelijske kulture. ...
Analogi folne kisline (aminopterin, metotreksat, pemetreksed, raltitreksed) Purinski analogi (kladribin, klofarabin, fludarabin ... Aminopterin se je nekoč uporabljal za zdravljenje raka, dandanes pa ga je povsem nadomestil metotreksat, ki je spojina s ... Aminopterin je sintezni derivat pterina. Deluje kot encimski zaviralec, ker se veže na vezišča encima dihidrofolat reduktaze ( ... Aminopterin (4-aminopterojska kislina) je 4-amino derivat folne kisline, ki izkazuje imunosupresivno in citostatično delovanje ...
... R-250 was first used to visualise proteins in 1964 by Fazekas de St. Groth and colleagues. Protein samples were separated electrophoretically on a cellulose acetate sheet. The sheet was then soaked in sulfosalicylic acid to fix the protein bands and then transferred to a solution of the dye.[10] Two years later in 1965 Meyer and Lambert used Coomassie Brilliant Blue R-250 to stain protein samples after electrophoretic separation in a polyacrylamide gel. They soaked the gel in a dye solution containing methanol, acetic acid and water. As the dye stained the polyacrylamide gel as well as the protein, in order to visualise the protein bands they needed to destain the gel which they did electrophoretically.[11] Subsequent publications reported that polyacrylamide gels could be successfully destained using an acetic acid solution. The first report of the use of the "G" form of the dye to visualise protein bands in polyacrylamide gels came in 1967, where the dye was dissolved ...
InChI=1S/C48H74O14.C47H72O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38;1-24(2)41-27(5)16-17-46(61-41)22-33-19-32(60-46)15-14-26(4)42(25(3)12-11-13-31-23-54-44-39(48)28(6)18-34(45(50)57-33)47(31,44)51)58-38-21-36(53-10)43(30(8)56-38)59-37-20-35(52-9)40(49)29(7)55-37/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3;11-14,18,24-25,27,29-30,32-44,48-49,51H,15-17,19-23H2,1-10H3/b13-12+,27-15+,32-14+;12-11+,26-14+,31-13+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+;25-,27-,29-,30-,32+,33-,34-,35-,36-,37-,38-,39+,40-,41+,42-,43-,44+,46+,47+/m00/s1 ...
... is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine can be phosphorylated to become guanosine monophosphate (GMP), cyclic guanosine monophosphate (cGMP), guanosine diphosphate (GDP), and guanosine triphosphate (GTP). These forms play important roles in various biochemical processes such as synthesis of nucleic acids and proteins, photosynthesis, muscle contraction, and intracellular signal transduction (cGMP). When guanine is attached by its N9 nitrogen to the C1 carbon of a deoxyribose ring it is known as deoxyguanosine. The antiviral drug acyclovir, often used in herpes treatment, and the anti-HIV drug abacavir, are structurally similar to guanosine. Guanosine is required for an RNA splicing reaction in mRNA, when a "self-splicing" intron removes itself from the mRNA message by cutting at both ends, re-ligating, and leaving just the exons on either side to be translated into protein.[1] ...
... is not produced by plants[citation needed] and is only observed in nature as a metabolite of caffeine in animals. Paraxanthine is also a natural metabolite of caffeine in some species of bacteria.[1] After intake, roughly 84% of caffeine is demethylated at the 3-position to yield paraxanthine, making it the chief metabolite of caffeine in the body.[2] Paraxanthine is also a major metabolite of caffeine in humans and other animals, such as mice.[3] Shortly after ingestion, caffeine is metabolized into paraxanthine by hepatic cytochrome P450,[4] which removes a methyl group from the N3 position of caffeine.[5] After formation, paraxanthine can be broken down to 7-methylxanthine by demethylation of the N1 position,[6] which is subsequently demethylated into xanthine or oxidized by CYP2A6 and CYP1A2 into 1,7-dimethylaric acid.[5] In another pathway, paraxanthine is broken down into 5-acetylamino-6-formylamino-3-methyluracil through N-acetyl-transferase 2, which is then broken down into ...
... has been shown to inhibit TGF-beta-mediated conversion of pulmonary fibroblasts into myofibroblasts in COPD and asthma via cAMP-PKA pathway and suppresses COL1 mRNA, which codes for the protein collagen.[24] It has been shown that theophylline may reverse the clinical observations of steroid insensitivity in patients with COPD and asthmatics who are active smokers (a condition resulting in oxidative stress) via a distinctly separate mechanism. Theophylline in vitro can restore the reduced HDAC (histone deacetylase) activity that is induced by oxidative stress (i.e., in smokers), returning steroid responsiveness toward normal.[25] Furthermore, theophylline has been shown to directly activate HDAC2.[25] (Corticosteroids switch off the inflammatory response by blocking the expression of inflammatory mediators through deacetylation of histones, an effect mediated via histone deacetylase-2 (HDAC2). Once deacetylated, DNA is repackaged so that the promoter regions of inflammatory genes ...
Lunell E, Svedmyr N, Andersson KE, Persson CG (1982). "Effects of enprofylline, a xanthine lacking adenosine receptor antagonism, in patients with chronic obstructive lung disease". European Journal of Clinical Pharmacology. 22 (5): 395-402. doi:10.1007/bf00542541. PMID 6288396 ...
ADP cycling supplies the energy needed to do work in a biological system, the thermodynamic process of transferring energy from one source to another. There are two types of energy: potential energy and kinetic energy. Potential energy can be thought of as stored energy, or usable energy that is available to do work. Kinetic energy is the energy of an object as a result of its motion. The significance of ATP is in its ability to store potential energy within the phosphate bonds. The energy stored between these bonds can then be transferred to do work. For example, the transfer of energy from ATP to the protein myosin causes a conformational change when connecting to actin during muscle contraction. It takes multiple reactions between myosin and actin to effectively produce one muscle contraction, and, therefore, the availability of large amounts of ATP is required to produce each muscle contraction. For this reason, biological processes have evolved to produce efficient ways to replenishment the ...
Animals that metabolize theobromine (found in chocolate) more slowly, such as dogs,[26] can succumb to theobromine poisoning from as little as 50 grams (1.8 oz) of milk chocolate for a smaller dog and 400 grams (14 oz), or around nine 44-gram (1.55 oz) small milk chocolate bars, for an average-sized dog. The concentration of theobromine in dark chocolates (approximately 10 g/kg (0.16 oz/lb)) is up to 10 times that of milk chocolate (1 to 5 g/kg (0.016 to 0.080 oz/lb)) - meaning dark chocolate is far more toxic to dogs per unit weight or volume than milk chocolate. The same risk is reported for cats as well,[27] although cats are less likely to ingest sweet food, with most cats having no sweet taste receptors.[28] Complications include digestive issues, dehydration, excitability, and a slow heart rate. Later stages of theobromine poisoning include epileptic-like seizures and death. If caught early on, theobromine poisoning is treatable.[29] Although not common, the effects of theobromine ...
Aminopterin je sintetički derivat pterina. Aminopterin dejstvuje kao inhibitor enzima dihidrofolat reduktaze. Njegov afinitet ... Aminopterin je u toku svog tržišnog veka korišćen i za tretman psorijaze u SAD. Ovaj lek je doveo do dramatičnog čišćenja ... No Aminopterin in Tissues of Animals Killed by Recalled Pet Food". PRNewsWire. 30. 3. 2007. Приступљено 14. 04. 2007.. ... Aminopterin i metotreksat su široko korišćeni u selekciji medija (kao što je HAT medijum) za ćelijske kulture. ...
Analogi folne kisline (aminopterin, metotreksat, pemetreksed, raltitreksed) Purinski analogi (kladribin, klofarabin, fludarabin ... Aminopterin se je nekoč uporabljal za zdravljenje raka, dandanes pa ga je povsem nadomestil metotreksat, ki je spojina s ... Aminopterin je sintezni derivat pterina. Deluje kot encimski zaviralec, ker se veže na vezišča encima dihidrofolat reduktaze ( ... Aminopterin (4-aminopterojska kislina) je 4-amino derivat folne kisline, ki izkazuje imunosupresivno in citostatično delovanje ...
Tetrazole-aminopterin , C19H20N12O3 , CID 124422 - structure, chemical names, physical and chemical properties, classification ...
1 mg of LD-aminopterin, or 3 mg of LD-aminopterin in a 1:1:1 ratio. The study hypothesis is that the 3 mg LD-aminopterin per ... Aminopterin Dose Finding Treatment for Methotrexate-Naïve Rheumatoid Arthritis. The safety and scientific validity of this ... Intestinal transport of aminopterin enantiomers in dogs and humans with psoriasis is stereoselective: evidence for a mechanism ... Aminopterin. Abortifacient Agents, Nonsteroidal. Abortifacient Agents. Reproductive Control Agents. Physiological Effects of ...
Aminopterin had a similar effect on deoxyuridine reversal of tritiated dThd incorporation into DNA. Aminopterin had no effect ... aminopterin was safe and efficacious in canine AD. Twice-weekly dosing negated efficacy despite having the same daily and ... aminopterin was safe and efficacious in canine AD. Twice-weekly dosing negated efficacy despite having the same daily and ... LD-aminopterin in the canine homologue of human atopic dermatitis: a randomized, controlled trial reveals dosing factors ...
There is now a well-defined syndrome of congenital anomalies associated with the use of aminopterin. The aminopterin syndrome ... The use of aminopterin has now fallen out of favor. Methotrexate is a folate antagonist that is now used more frequently. A ... Newborns who survived after aminopterin exposure were noted for years to have defects of the neural tube, skull, or limbs. ... We report two patients who presented with classic features of aminopterin syndrome combined with significant congenital cardiac ...
Aminopterin, ABVD, Cyclophosphamide von Source: Wikipedia bei AbeBooks.de - ISBN 10: 1157367399 - ISBN 13: 9781157367390 - ... Chemotherapeutic agents: Chemotherapy, Pawpaw, Biosynthesis of doxorubicin, Camptothecin, Epothilone, Aminopterin, ABVD, ... Chemotherapeutic agents: Chemotherapy, Pawpaw, Biosynthesis of doxorubicin, Camptothecin, Epothilone, Aminopterin, ABVD, ... Chapters: Chemotherapy, Pawpaw, Biosynthesis of doxorubicin, Camptothecin, Epothilone, Aminopterin, ABVD, Cyclophosphamide, ...
Aminopterin inhibition in Aerobacter aerogenes: alanine and valine accumulation during the inhibition and their utilization on ... Aminopterin inhibition in Aerobacter aerogenes: alanine and valine accumulation during the inhibition and their utilization on ... Aminopterin inhibition in Aerobacter aerogenes: alanine and valine accumulation during the inhibition and their utilization on ... Aminopterin inhibition in Aerobacter aerogenes: alanine and valine accumulation during the inhibition and their utilization on ...
Fetal aminopterin syndrome is a condition affecting babies whose mothers were exposed to the chemical aminopterin or ... Symptoms of fetal aminopterin syndrome depend on how early in pregnancy the woman is exposed to aminopterin or methotraxate and ... There is no cure for fetal aminopterin syndrome, though symptoms can be managed. Aminopterin is no longer used, but ... Babies exposed to aminopterin or methotraxate during development can be born with developmental delays such as inability to ...
Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia. - Mechanism ... Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase ( ... Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. ... Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the ...
Aminopterin is a synthetic derivative of pterin. Aminopterin works as an enzyme inhibitor by competing for the folate binding ... the enzyme inhibited by aminopterin. Leucovorin has been used in rats, dogs and humans to rescue aminopterin toxicity.[19][20][ ... and 0.097 mg/kg aminopterin each day for 7 to 12 days. Folic acid was given in a weight ratio to aminopterin of 200:1 to 800:1 ... optimal of 1 hour prior to aminopterin) of administration in relation to aminopterin.[24][25] The temporal relationship between ...
... exporter of AMINOPTERIN including all laboratory Chemicals, and offered to our clients at the best industry prices, Inquire us ...
... hypoxanthine-aminopterin-thymidine medium) for roughly 10 to 14 days. Aminopterin blocks the pathway that allows for nucleotide ...
... cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin- ... cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin- ...
... information resources and questions answered by our Genetic and Rare Diseases Information Specialists for Fetal aminopterin ... Fetal aminopterin syndrome Title Other Names:. Aminopterin embryopathy syndrome; Aminopterin fetopathy syndrome; Aminopterin ... syndrome; Aminopterin embryopathy syndrome; Aminopterin fetopathy syndrome; Aminopterin syndrome; Fetal methotrexate syndrome ...
Aminopterin LKT Labs. Aminopterin is a folic acid analog and derivative of pterin; it is very similar to methotrexate in ... Aminopterin exhibits anticancer chemotherapeutic and immunosuppressive activities. Like other folic acid analogs, aminopterin ...
Aminopterin. 500. 500/10,000 55-91-4. Isofluorphate. b. 100. 100 56-25-7. Cantharidin. 100. 100/10,000 ...
Folic acid is a type of B vitamin. This article discusses the test to measure the amount of folic acid in the blood.
Poisoned Pet Food, Aminopterin. 3/23/2007. The New York State Food Laboratory has identified the presence of aminopterin in all ...
A useful article about Treating a Case of Suspected Feline Aminopterin Poisoning.Full details about... ...
Aminopterin. Antineoplastic Agents. Folic Acid Antagonists. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. ...
... aminopterin; xeloda; ibandronate; CPT-11; topoisomerase inhibitor RFS 2000; difluoromethylornithine (DMFO); retinoic acid; ...
... aminopterin; xeloda; ibandronate; CPT-11; topoisomerase inhibitor RFS 2000; difluoromethylomithine (DMFO); retinoic acid; ...
Craniosynostosis is the early fusion of two or more bones of the skull. Synostosis can interfere with normal growth of the brain and skull..
Read chapter Case Study 53: Reproductive and Developmental Hazards: People are increasingly concerned about potential environmental health hazards and oft...
Hypoxanthine - Aminopterin - Thymidine (H.A.T.) 500x concentrate (ATCC® 69-X™) ATCC® Number: 69-X™ Quantity: 5 x 2 ml vials, ...
Realizing this, he attempted to use a folate antagonist, aminopterin, to block the function of folic acid in patients with ... In 1947, Farber conducted a clinical trial on aminopterin on 16 children, 10 of which eventually achieved temporary remission. ... aminopterin)". New England Journal of Medicine. 238 (23): 787-793. doi:10.1056/nejm194806032382301. PMID 18860765.CS1 maint: ... he carried out both the preclinical and clinical evaluation of aminopterin (synthesized by Yellapragada Subbarow). He showed ...
Copyright:www.vvchem.com 2010-2020 source chemicals on the most professional electronic B2B platform ICP NO.:浙ICP备09052245号-11 ...
ATTEMPTED ABORTION WITH AMINOPTERIN (4-AMINO-PTEROYLGLUTAMIC ACID): MALFORMATIONS OF THE CHILD. WARKANY, JOSEF; BEAUDRY, PIERRE ...
  • This is a double-blind, randomized, placebo-controlled, dose ranging study that will evaluate the safety, efficacy, and pharmacokinetic properties (the absorption, distribution and excretion) of aminopterin following oral administration by subjects with active rheumatoid arthritis (≥ 6 tender and ≥ 6 swollen joints) who have not been treated with methotrexate (MTX). (clinicaltrials.gov)
  • A series of novel hydrogen peroxide sensitive prodrugs of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in mice with collagen induced arthritis (CIA) as a model of chronic rheumatoid arthritis (RA). (worldwidescience.org)
  • Congenital Cardiac Defects: A Possible Association of Aminopterin Syndrome and In Utero Methotrexate Exposure? (biomedsearch.com)
  • We report two patients who presented with classic features of aminopterin syndrome combined with significant congenital cardiac malformations after first-trimester in utero methotrexate exposure. (biomedsearch.com)
  • Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. (medchemexpress.com)
  • Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. (wikidoc.org)
  • The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. (wikidoc.org)
  • [4] Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro , aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate. (wikidoc.org)
  • [6] Similar congenital abnormalities have been documented with methotrexate, and collectively their teratogenic effects have become known as the fetal aminopterin syndrome . (wikidoc.org)
  • Aminopterin and methotrexate are widely used in selection media (such as HAT medium ) for cell culture . (wikidoc.org)
  • Four folate analogues, methotrexate, aminopterin, 10-deazaaminopterin, and 10-ethyl-10-deazaaminopterin were assessed for their ability to be metabolized to poly-γ-glutamyl derivatives in three tumor lines which vary in their sensitivity to these agents. (aacrjournals.org)
  • Cytotoxicity of the four analogues against the murine L1210 leukemia and the human Manca B cell leukemia, as determined by a 3-h clonogenic assay, showed aminopterin and the two 10-deazaaminopterin compounds to be approximately equivalent for each cell type and were 3- to 10- (L1210) and 7- to 14-fold (Manca) more potent than methotrexate. (aacrjournals.org)
  • In murine Sarcoma 180 cells, 10-ethyl-10-deazaaminopterin and aminopterin were similarly potent but were 5- to 10-fold more potent than 10-deazaaminopterin and 40- to 80-fold more potent than methotrexate. (aacrjournals.org)
  • In L1210 cells incubated for 3 h with drug, efflux of methotrexate and aminopterin polyglutamates was found to be slower than the parent drug and decreased with the addition of polyglutamyl residues. (aacrjournals.org)
  • In contrast, the efflux of methotrexate and aminopterin diglutamates from cells preloaded with these derivatives and the parent compounds was the same, and efflux overall was markedly more rapid. (aacrjournals.org)
  • Fused cells are incubated in HAT medium (hypoxanthine-aminopterin-thymidine medium) for roughly 10 to 14 days. (wikipedia.org)
  • The selective culture medium is called HAT medium because it contains hypoxanthine, aminopterin and thymidine. (wikipedia.org)
  • 2.Cell fusion to produce hybridomas: Myeloma cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin-thymidine (HAT) choice medium utilized after cell combination. (maryelizabethbodycare.com)
  • Peripheral blood lymphocytes from "old" male individuals and "young" controls were fused with a Chinese hamster cell line (CHO-YH21), yielding 10 HAT-resistant rodent-human clones from the old propositi and 22 from the young controls (HAT = hypoxanthine/aminopterin/thymidine). (nih.gov)
  • The New York State Food Laboratory has identified the presence of aminopterin in all of the samples of cat and. (jonbarron.org)
  • Fetal aminopterin syndrome is a condition affecting babies whose mothers were exposed to the chemical aminopterin or methotraxate during pregnancy. (diseaseinfosearch.org)
  • Symptoms of fetal aminopterin syndrome depend on how early in pregnancy the woman is exposed to aminopterin or methotraxate and the dosage of the medication being used. (diseaseinfosearch.org)
  • There is no cure for fetal aminopterin syndrome , though symptoms can be managed. (diseaseinfosearch.org)
  • Following organizations serve the condition "Fetal Aminopterin Syndrome" for support, advocacy or research. (diseaseinfosearch.org)
  • Finding the right clinical trial for Fetal Aminopterin Syndrome can be challenging. (diseaseinfosearch.org)
  • The terms "Fetal Aminopterin Syndrome" returned 0 free, full-text research articles on human participants. (diseaseinfosearch.org)
  • According to ClinicalTrials.gov there are currently 0 additional "open" studies for "Fetal Aminopterin Syndrome" (open studies are recruiting volunteers) and 0 "Fetal Aminopterin Syndrome" studies with "all" status. (diseaseinfosearch.org)
  • The purpose of this study is to determine whether aminopterin is effective in the treatment of rheumatoid arthritis (RA). (clinicaltrials.gov)
  • The study hypothesis is that the 3 mg LD-aminopterin per week is effective at treating rheumatoid arthritis compared to placebo. (clinicaltrials.gov)
  • Effect of aminopterin in rheumatoid arthritis and psoriasis. (springer.com)
  • There is now a well-defined syndrome of congenital anomalies associated with the use of aminopterin. (biomedsearch.com)
  • When a similar cluster of abnormalies appears in the absence of exposure to antifolates it is referred to as aminopterin-like syndrome without aminopterin. (wikidoc.org)
  • Aminopterin works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase . (wikidoc.org)
  • While working at Harvard Medical School on a research project funded by a grant from the American Cancer Society, he carried out both the preclinical and clinical evaluation of aminopterin (synthesized by Yellapragada Subbarow), a folate antagonist in childhood acute lymphoblastic leukemia. (wikipedia.org)
  • He then helped develop the drug aminopterin that targets folate metabolism. (theconversation.com)
  • The antifolate activity of aminopterin was first used by Sidney Farber in 1947 to induce remissions among children with leukemia . (wikidoc.org)
  • Aminopterin (4-aminopteroic acid), a 4-amino analog of folic acid , is an antineoplastic drug with immunosuppressive properties used in chemotherapy . (wikidoc.org)
  • In the early 1940s, the first chemotherapy trial in children used a drug called aminopterin , which suppresses the immune system. (theconversation.com)
  • [3] [4] Aminopterin je kasnije prodavala kompanija Lederle Laboratories (Pearl River, Njujork ) u SAD od 1953 do 1964 za pedijatrijsku leukemiju . (wikipedia.org)
  • [1] [2] Aminopterin was later marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. (wikidoc.org)
  • The apparently mistaken association of aminopterin with its use as a rodenticide likely dates back to a 1951 patent issued to the American Cyanamid Company (then the holding company of Lederle Laboratories) that is commonly cited by a variety of reference textbooks. (wikidoc.org)
  • Aminopterin i metotreksat su široko korišćeni u selekciji medija (kao što je HAT medijum ) za ćelijske kulture . (wikipedia.org)
  • Aminopterin se je nekoč uporabljal za zdravljenje raka , dandanes pa ga je povsem nadomestil metotreksat , ki je spojina s podobno strukturo. (wikipedia.org)
  • Aminopterin je sintetički derivat pterina . (wikipedia.org)
  • Aminopterin (4-aminopterojska kislina) je 4- amino derivat folne kisline , ki izkazuje imunosupresivno in citostatično delovanje. (wikipedia.org)
  • Separately, New York state officials, who said they discovered aminopterin -- a substance used in rat poison -- in tainted pet food last week, said they have no doubt that melamine is present in the recalled food. (reuters.com)
  • Since neither aminopterin nor melamine are compounds that should be found in pet food, it is important for full public disclosure," said New York State Department of Agriculture and Markets Commissioner Patrick Hooker. (reuters.com)
  • Acute Renal Failure (ARF) from the ingestion of aminopterin and/or melamine (most likely the latter). (itchmo.com)
  • However, in Sarcoma 180 cells, only aminopterin polyglutamates reached a similar maximum percentage of accumulation, while lower relative polyglutamate levels were achieved with the other analogues. (aacrjournals.org)
  • Accumulation of individual polyglutamates in each cell line was similar for all analogues except aminopterin. (aacrjournals.org)
  • Aminopterin dejstvuje kao inhibitor enzima dihidrofolat reduktaze . (wikipedia.org)
  • His team gave 16 infants and children with acute lymphoblastic leukemia a folic acid inhibitor, aminopterin -10 showed improvement by clinical and hematologic parameters after three months. (wikipedia.org)
  • The first suggestions that folic acid antagonists were teratogenic in humans were based on reports of failed terminations in mothers given aminopterin in the first trimester. (biomedsearch.com)
  • Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a K i of 3.7 pM. (medchemexpress.com)
  • The IC 50 value of Aminopterin (4-Aminofolic acid) against CCRF-CEM cells during 72 h of exposure is 4.4 nM [2] . (medchemexpress.com)
  • Aminopterin (4-Aminofolic acid) produces a marked inhibition of mitosis in low concentrations in human leukemic leukocytes [4] . (medchemexpress.com)
  • Exposing cells to aminopterin (a folic acid analogue, which inhibits dihydrofolate reductase, DHFR), makes them unable to use the de novo pathway and become fully auxotrophic for nucleic acids, thus requiring supplementation to survive. (wikipedia.org)
  • Aminopterin , 4-amino analog folne kiseline , je antineoplastični lek sa imunosupresivnim osobinama koji se koristi u hemoterapiji . (wikipedia.org)
  • Aminopterin is a synthetic derivative of pterin . (wikidoc.org)
  • Aminopterin has a potent effect on leukaemia cells growing in a test tube. (theconversation.com)
  • The influence of aminopterin on limb regeneration in Ambystoma mexicanum. (medchemexpress.com)
  • Their findings contradict the New York State Food Laboratory's tests, which pointed to aminopterin - a rat poison - as the likely culprit. (redorbit.com)
  • Aminopterin for psoriasis: A decade's observation. (wikipedia.org)
  • During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. (wikidoc.org)
  • Newborns who survived after aminopterin exposure were noted for years to have defects of the neural tube, skull, or limbs. (biomedsearch.com)
  • Aminopterin blocks the pathway that allows for nucleotide synthesis. (wikipedia.org)
  • Although the use of aminopterin as a rodenticide is widely asserted on the web and elsewhere, there is no evidence that it has ever been used for that purpose either in the United States or elsewhere in the world. (wikidoc.org)
  • Using step-wise selection, lines of mouse L-cells were obtained (clones B-82, TK-), resistance to aminopterin (AP) of which exceeds resistance of parental cells by 10 3 -5 x 10 4 times. (worldwidescience.org)
  • Aminopterin was accumulated mainly as the diglutamate, particularly in Manca cells where 70% of total drug was in the diglutamate form within the first 3 h and remained the predominant form for 24 h. (aacrjournals.org)
  • The FDA, however, has still not confirmed the presence of aminopterin in the recalled pet food. (reuters.com)
  • On March 23 2007 , ABC News reported [11] that aminopterin was the chemical linked to the 2007 Menu Foods pet food contamination incident . (wikidoc.org)
  • Tests at the University of Guelph in Ontario , Canada detected aminopterin in some pet food samples, but only in concentrations of parts per billion or parts per trillon, amounts too low to cause the symptoms seen. (wikidoc.org)
  • Nor was it clear why earlier tests identified the foreign agent as aminopterin, a finding U.S. Food and Drug Administration officials said they were unable to confirm. (redorbit.com)
  • He tested aminopterin in 16 children with leukaemia and obtained temporary remission in ten of them. (theconversation.com)
  • Aminopterin is no longer used, but methotraxate may still be used to treat some conditions such as cancer. (diseaseinfosearch.org)
  • A structurally similar antifolate, aminopterin, also reduced the arthritis. (nih.gov)
  • Journal Article] Adenosine blocks aminopterin-induced suppression of osteoclast differentiation. (nii.ac.jp)
  • To address this issue and understand how dosing affects antifolate efficacy in AD, we examined the efficacy and safety of different oral doses and schedules of LD- aminopterin in the canine model of AD. (worldwidescience.org)
  • These same reports stated that the FDA had failed to find evidence of aminopterin in the wheat gluten. (wikidoc.org)