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A Review on L-Asparaginase
Published in Se-Kwon Kim, Marine Biochemistry, 2023
The natural lactone that is isolated from the marine Bryozoan is bryostatin-1, which has both antitumor activity and immunomodulatory effects (Wall et al., 1999). It has in vitro cytotoxicity effect over various leukemia and tumor cell lines. Bryostatin-1 proved antitumor activity against leukemia, melanoma, ovarian cancer and lymphoma. It also has an stimulatory effect on several anticancer agents such as cisplatin, cytosine arabinoside, vincristine, paclitaxel, melphalan and others (Wall et al., 1999).
Nucleic Acids as Therapeutic Targets and Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
This agent is approved in the UK for the treatment (by mouth) of acute nonlymphocytic leukemia, and in combination therapy for advanced breast cancer after failure of first-line chemotherapy (not including anthracyclines). It is also combined with cytosine arabinoside as a first-line treatment for acute myeloid leukemia.
Fetal and neonatal medicine
Published in Jagdish M. Gupta, John Beveridge, MCQs in Paediatrics, 2020
Jagdish M. Gupta, John Beveridge
The type II virus accounts for about 75% of herpes simplex infections which are acquired during delivery (following rupture of membranes). Diagnosis in the mother is difficult and may not be obvious. Intravenous cytosine arabinoside has not been shown to be effective, though treatment with acyclovir is more encouraging. Jaundice is an early and prominent symptom.
Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Joanna Stefaniak, Michał G. Nowak, Marek Wojciechowski, Sławomir Milewski, Andrzej S. Skwarecki
Le Camus and co-workers found arabinose-5-phosphate oxime 43 (APO) to be a potent inhibitor of GlcN-6-P synthase65. The authors obtained the aforementioned compound by converting the commercially available arabinose-5-phosphate to its oxime with hydroxylamine (Scheme 10A). Due to the low hydrolytic stability of phosphate moiety in 43, the authors decided to obtain its homolog 44. This compound was obtained using d-arabinose-derived aldehyde 45, which was converted into vinylphosphonate 46 using the Horner-Emmons reaction. A Series of selective deprotection reactions, followed by a reaction with hydroxylamine, led to the final formation of oxime 44 (Scheme 10B). Both compounds, 43 and 44, can be considered as structural analogues of open ring fructosamine-6-P, formed at the ISOM active site from Fru-6-P after its amination with glutamine-derived ammonia. The enzyme inhibitory potential of 43 was quite high (Ki = 14.3 µM), while that of 44 was much lower (Ki = 0.36 mM)65.
Overexpression of cancerous inhibitor ofPP2A (CIP2A) in acute myeloid leukemia
Published in Expert Review of Hematology, 2022
Reem Hasanin, Ghada Mossallam, Sally Elfishawi, Ahmed Rabea, Nayera Hamdy
The immunophenotyping was performed on BM blast cells using a comprehensive panel including CD45, CD13, CD33, MHC CLASSII, CD34, CD11C, CD64, CD36, CD14, CD4, CD8, CD7, CD2, CD1, CD56, CD3, CytCD3, CD5, CD19, CD10, CD22, CD20, Cytμ, Cyt CD79α, CD34, CD117 (Bechman Coulter, Miami, FL). Mutation analysis was routinely performed for all newly diagnosed patients with AML for FLT3/ITD using polymerase chain reaction and fragment analysis, FLT3-TKD using PCR- restriction fragment length polymorphism (PCR-RFLP) and for NPM1 using the ipsogen NPM1 MutaScreen kit (Qiagen). The treatment protocol for AML included high-intensity induction with 7 + 3 regimen (cytosine arabinoside 100 mg/m2 continuous infusion days 1 to 7 and doxorubicin 45 mg/m2 days 1 to 3). Patients older than 60 years and those with poor performance status received less-intensive therapy of low-dose cytosine arabinoside (LDAC), 20 mg/12 hr subcutaneously for 10 days, or hydroxyurea (if the patient will not tolerate chemotherapy due to comorbidities). After attaining complete remission (CR), consolidation chemotherapy was carried out by four cycles of a high-dose cytosine arabinoside regimen consisting of 2 g/m2 on days 1, 3, and 5 by infusion over 3 hours. Patients who had HLA matched donors were referred to stem cell transplantation.
Spectroscopic observations of β-eudesmol binding to human cytochrome P450 isoforms 3A4 and 1A2, but not to isoforms 2C9, 2C19, and 2D6
Published in Xenobiotica, 2022
Dawid Krenc, Kesara Na-Bangchang
A single transformant E. coli colony was grown overnight in 2.0 mL LB medium containing 10 mM glucose, 0.1 mg/mL ampicillin sodium, and 20 μg/mL chloramphenicol. The culture was split into three aliquots of 0.55 mL and each was added to 60 mL growth medium in a 500-mL Erlenmeyer flask. The medium consisted of Terrific Broth (12.0 g/L tryptone, 1.0 g/L peptone, 24.0 g/L yeast extract, and 0.2% v/v glycerol), with supplements of 100 mM potassium phosphate buffer (pH 7.4), 1.0 mM thiamine hydrochloride (Sigma-Aldrich, St. Louis, MO), 0.1 mg/mL ampicillin sodium, 20 μg/mL chloramphenicol, and trace elements (250 μM FeCl3, 2.4 μM ZnCl2, 2.1 μM CoCl2, 2.1 μM Na2MoO4, 1.9 μM CuCl2, 2.0 μM H3BO3, added as a combined 4000x stock solution in 10% HCl). The three culture flasks were mounted on a non-temperature-controlled shaker (Orbital Shaker PSU-10i, Biosan, Latvia) and incubated at room temperature (23.5–25 °C) with shaking (180 rpm) for 5 h. To each culture was then added a second set of supplements to final concentrations of 4.0 mg/mL L-arabinose (Sigma-Aldrich), 0.5 mM δ-aminolevulinic acid (Sigma-Aldrich), and 1.0 mM isopropyl-β-D-thiogalactopyranoside (TCI, Tokyo, Japan), with further incubation for 43–46 h. A temperature of ≤32 °C served to facilitate protein folding (Yun et al. 2006).