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https://www.readbyqxmd.com/read/29787565/expression-purification-and-inhibition-profile-of-dihydrofolate-reductase-from-the-filarial-nematode-wuchereria-bancrofti
#1
Andrew M Tobias, Dea Toska, Keith Lange, Tyler Eck, Rohit Bhat, Cheryl A Janson, David P Rotella, Ueli Gubler, Nina M Goodey
Filariasis is a tropical disease caused by the parasitic nematodes Wuchereria bancrofti and Brugia malayi. Known inhibitors of dihydrofolate reductase (DHFR) have been previously shown to kill Brugia malayi nematodes and to inhibit Brugia malayi DHFR (BmDHFR) at nanomolar concentrations. These data suggest that BmDHFR is a potential target for the treatment of filariasis. Here, protocols for cloning, expression and purification of Wuchereria bancrofti DHFR (WbDHFR) were developed. The Uniprot entry J9F199-1 predicts a 172 amino acid protein for WbDHFR but alignment of this sequence to the previously described BmDHFR shows that this WbDHFR sequence lacks a crucial, conserved 13 amino acid loop...
2018: PloS One
https://www.readbyqxmd.com/read/29550996/molecular-docking-to-toxoplasma-gondii-thymidylate-synthase-dihydrofolate-reductase-and-efficacy-of-raltitrexed-in-infected-mice
#2
Michelle de Paula Reis, Daniely Alves de Lima, Karoline Bach Pauli, Carlos Eduardo Linhares Andreotti, André Luiz Soares de Moraes, Daniela Dib Gonçalves, Italmar Teodorico Navarro, Paulo Sérgio Alves Bueno, Flavio Augusto Vicente Seixas, Arquimedes Gasparotto Junior, Emerson Luiz Botelho Lourenço
Toxoplasmosis is a zoonosis of worldwide distribution. Currently, two drugs, pyrimethamine and sulfadiazine, are used as a reference in the treatment of toxoplasmosis, but the resistance of Toxoplasma gondii appears as a relevant public health problem. In order to identify new drugs to toxoplasmosis treatment, we performed a molecular docking of raltitrexed to T. gondii thymidylate synthase-dihydrofolate reductase (TS-DHFR) and also evaluated its efficacy in infected mice. Initially, raltitrexed was docked on the crystallographic structures of TS-DHFR from T...
May 2018: Parasitology Research
https://www.readbyqxmd.com/read/29548480/fluoropyrimidine-induced-cardiotoxicity
#3
REVIEW
Ilaria Depetris, Donatella Marino, Alessandro Bonzano, Celeste Cagnazzo, Roberto Filippi, Massimo Aglietta, Francesco Leone
Fluoropyrimidines (5-fluorouracil and capecitabine) are antimetabolite drugs, widely used for the treatment of a variety of cancers, both in adjuvant and in metastatic setting. Although the most common toxicities of these drugs have been extensively studied, robust data and comprehensive characterization still lack concerning fluoropyrimidine-induced cardiotoxicity (FIC), an infrequent but potentially life-threatening toxicity. This review summarizes the current state of knowledge of FIC with special regard to proposed pathogenetic models (coronary vasospasm, endothelium and cardiomyocytes damage, toxic metabolites, dihydropyrimidine dehydrogenase deficiency); risk and predictive factors; efficacy and usefulness in detection of laboratory markers, electrocardiographic changes and cardiac imaging; and specific treatment, including a novel agent, uridine triacetate...
April 2018: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/29538414/biomolecular-study-of-human-thymidylate-synthase-conformer-selective-inhibitors-new-chemotherapeutic-approach
#4
Hala O El-Mesallamy, Hekmat M El Magdoub, James M Chapman, Nadia M Hamdy, Mona F Schaalan, Lamiaa N Hammad, Sondra H Berger
Thymidylate synthase (TS) is a well-validated target for the therapy of adult cancers. Propane-1,3-diphosphonic acid (PDPA) has significant inhibitory properties against human thymidylate synthase (hTS) relative to mouse TS which is not predicted to adopt an inactive conformer. The current research aims to identify novel, lead inhibitors of hTS and examine the prediction that they bind selectively to hTS enzymes existing in different conformational equilibria. Conformer-selectivity was evaluated through performing activity inhibition studies, as well as intrinsic fluorescence (IF) studies in comparison to the known orthosteric inhibitor raltitrexed (RTX)...
2018: PloS One
https://www.readbyqxmd.com/read/29507800/chemotherapy-treatment-in-malignant-pleural-mesothelioma-a-difficult-history
#5
REVIEW
Marika Cinausero, Karim Rihawi, Francesca Sperandi, Barbara Melotti, Andrea Ardizzoni
Malignant pleural mesothelioma (MPM) is a rare neoplasm that typically arises from mesothelial surfaces of the pleural cavity. Despite treatment improvements, it carries a dismal prognosis. The majority of patients either have unresectable disease or are not candidates for surgery due to medical comorbidities or old age. For such patients, chemotherapy (CT) represents the gold-standard treatment. To date, combination CT with cisplatin plus pemetrexed represents the most widely used regimen in first-line setting for patients with unresectable MPM...
January 2018: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/29246011/network-meta-analysis-of-the-efficacy-of-first-line-chemotherapy-regimens-in-patients-with-advanced-colorectal-cancer
#6
Dong-Mei Wu, Yong-Jian Wang, Shao-Hua Fan, Juan Zhuang, Zi-Feng Zhang, Qun Shan, Xin-Rui Han, Xin Wen, Meng-Qiu Li, Bin Hu, Chun-Hui Sun, Ya-Xing Bao, Hai-Juan Xiao, Lin Yang, Jun Lu, Yuan-Lin Zheng
This network meta-analysis compared the short-term and long-term efficacies of first-line chemotherapy regimens in patients with advanced colorectal cancer (CRC). The 10 regimens included folinic acid + 5-fluorouracil + oxaliplatin (FOLFOX), folinic acid + 5-fluorouracil + irinotecan (FOLFIRI), folinic acid + 5-fluorouracil + gemcitabine (FFG), folinic acid + 5-fluorouracil + trimetrexate (FFT), folinic acid + 5-fluorouracil (FF), irinotecan + oxaliplatin (IROX), raltitrexed + oxaliplatin (TOMOX), folinic acid + tegafur-uracil (FTU), raltitrexed, and capecitabine...
November 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/29108296/comparison-of-two-transarterial-chemoembolization-regimens-in-patients-with-unresectable-hepatocellular-carcinoma-raltitrexed-plus-oxaliplatin-versus-5-fluorouracil-plus-oxaliplatin
#7
Wei Cui, Wenzhe Fan, Qun Zhang, Jia Wen, Yonghui Huang, Jianyong Yang, Jiaping Li, Yu Wang
Aims: To compare the safety and efficacy of TACE using raltitrexed, oxaliplatin and epirubicin with 5-fluorouracil, oxaliplatin and epirubicin for patients with unresectable hepatocelluar carcinoma. Results: Median overall survival (OS) was 7.4 months in the raltitrexed group [95% confidence interval (CI): 5.4, 9.4) and 5.8 months in the control group (95% CI: 5.2, 6.4; P = 0.177). The median progression-free survival (PFS) time was significantly higher in the raltitrexed group (3...
October 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/28927061/5fu-resistance-caused-by-reduced-fluoro-deoxyuridine-monophosphate-and-its-reversal-using-deoxyuridine
#8
Ryutaro Mori, Manabu Futamura, Toshiyuki Tanahashi, Yoshihiro Tanaka, Nobuhisha Matsuhashi, Kazuya Yamaguchi, Kazuhiro Yoshida
The mechanism of 5-fluorouracil (5FU) resistance was investigated, focusing on the level of thymidylate synthase (TS) ternary complex formed with fluoro-deoxyuridine monophosphate (FdUMP). MKN45 and 5FU-resistant MKN45/F2R cells were treated with 5FU and fluoro-deoxyuridine (FdU) in combination with deoxyuridine (dU) and thymidine (dT). Subsequently, the levels of ternary complex were determined by western blotting and the cell viability was calculated using an MTT assay. MKN45/F2R cells exhibited 5FU resistance (56...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28697647/antimetabolites-in-the-treatment-of-advanced-pleural-mesothelioma-a-network-meta-analysis-of-randomized-clinical-trials
#9
Davide Tassinari, Chiara Cherubini, Emiliano Tamburini, Fabrizio Drudi, Maximilian Papi, Manuela Fantini, Luigi Lazzari-Agli, Sergio Sartori
An indirect comparison of cisplatin-pemetrexed (CP) and cisplatin-raltitrexed (CR) was performed. The Odds Ratios of 10, 15 and 20 month survival rate and response rate were assumed as indexes of efficacy; the Odds Ratio of grade III-IV side effects, and the absolute risk of overall, hematologic and non-hematologic toxicity, were assumed as indexes of safety. The outcomes of 352 patients were analysed. The Odds Ratios and 95% Confidence Interval (95% CI) of 10, 15 and 20 months survival rate and response rate were 1...
December 2017: Journal of Chemotherapy
https://www.readbyqxmd.com/read/28634233/structural-analyses-of-human-thymidylate-synthase-reveal-a-site-that-may-control-conformational-switching-between-active-and-inactive-states
#10
COMPARATIVE STUDY
Dan Chen, Anna Jansson, Daniel Sim, Andreas Larsson, Pär Nordlund
Thymidylate synthase (TS) is the sole enzyme responsible for de novo biosynthesis of thymidylate (TMP) and is essential for cell proliferation and survival. Inhibition of human TS (hTS) has been extensively investigated for cancer chemotherapy, but several aspects of its activity and regulation are still uncertain. In this study, we performed comprehensive structural and biophysical studies of hTS using crystallography and thermal shift assay and provided the first detailed structural information on the conformational changes induced by ligand binding to the hTS active site...
August 11, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28628839/a-simple-and-fast-lc-ms-ms-method-with-a-very-high-sensitivity-for-the-measurement-of-raltitrexed-in-human-plasma
#11
Stefano Kim, Amaëlle Bisch, Damien Montange, Marie-Justine Paillard, Thierry Nguyen, Marine Jary, Marion Jacquin, Betsy Winkfield, Christophe Borg, Bernard Royer
Raltitrexed is a thymidylate synthase inhibitor that can be administered safely to patients with cardiovascular disease or dihydropyrimidine dehydrogenase deficiency, as opposed to 5FU. The recommended dose of 3mg/m(2) every 3 weeks often leads to toxicity. Interestingly, the 2mg/m(2) every 2 weeks dose appears to be less toxic. A pharmacokinetic trial was then performed by our team to investigate such phenomenon. However, there are currently, two main methods for RTX measurement described in the literature: a radioimmunoassay (RIA) and chromatographic-based methods with either UV or mass spectrometry detections...
August 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28535418/a-study-of-peritoneal-metastatic-xenograft-model-of-colorectal-cancer-in-the-treatment-of-hyperthermic-intraperitoneal-chemotherapy-with-raltitrexed
#12
COMPARATIVE STUDY
Cen Qiu, Yueqi Li, Xin Liang, Yingxue Qi, Yiyang Chen, Xianke Meng, Hongtu Zheng, Ye Xu, Sanjun Cai, Guoxiang Cai, Jianwen Liu
Peritoneal metastasis of colorectal cancer is one of the most incident and fateful diseases among relapse cases. It shows a certain resistance to systemic chemotherapy. The perfusion system in clinic is complex and hard to be used in fundamental researches. This study aims at evaluating the effect of an improved hyperthermic intraperitoneal chemotherapy with Raltitrexed used in tumor-bearing mice with peritoneal metastatic colorectal carcinoma. The results showed that no severe adverse effect was observed. All control animals developed extensive peritoneal and mesenteric metastatic nodes...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28456721/investigation-of-the-importance-of-multidrug-resistance-associated-protein-4-mrp4-abcc4-in-the-active-efflux-of-anionic-drugs-across-the-blood-brain-barrier
#13
Kayoko Kanamitsu, Hiroyuki Kusuhara, John D Schuetz, Kenji Takeuchi, Yuichi Sugiyama
The importance of multidrug resistance-associated protein 4 (Mrp4/Abcc4) in limiting the penetration of Mrp4 substrate compounds into the central nervous system across the blood-brain barrier was investigated using Mrp4(-/-) mice. Significant adenosine triphosphate-dependent uptake by MRP4 was observed for ochratoxin A, pitavastatin, raltitrexed (Km = 43.7 μM), pravastatin, cyclic guanosine monophosphate, 2,4-dichlorophenoxyacetate, and urate. The defect in the Mrp4 gene did not affect the brain-to-plasma ratio (Kp,brain) of quinidine and dantrolene...
April 27, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28415810/comparison-of-two-transarterial-chemoembolization-regimens-in-patients-with-unresectable-hepatocellular-carcinoma-raltitrexed-plus-oxaliplatin-versus-5-fluorouracil-plus-oxaliplatin
#14
Wei Cui, Wenzhe Fan, Qun Zhang, Jia Wen, Yonghui Huang, Jianyong Yang, Jiaping Li, Yu Wang
AIMS: To compare the safety and efficacy of TACE using raltitrexed, oxaliplatin and epirubicin with 5-fluorouracil, oxaliplatin and epirubicin for patients with unresectable hepatocelluar carcinoma. RESULTS: Median overall survival (OS) was 7.4 months in the raltitrexed group [95% confidence interval (CI): 5.4, 9.4) and 5.8 months in the control group (95% CI: 5.2, 6.4; P = 0.177). The median progression-free survival (PFS) time was significantly higher in the raltitrexed group (3...
March 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28293087/hepatic-artery-infusion-with-raltitrexed-or-5-fluorouracil-for-colorectal-cancer-liver-metastasis
#15
Jian-Hai Guo, Hang-Yu Zhang, Song Gao, Peng-Jun Zhang, Xiao-Ting Li, Hui Chen, Xiao-Dong Wang, Xu Zhu
AIM: To evaluate the efficiency and safety of hepatic artery infusion chemotherapy (HAIC) using raltitrexed or 5-fluorouracil for colorectal cancer (CRC) liver metastasis (CRCLM). METHODS: A retrospective analysis of patients with unresectable CRCLM who failed systemic chemotherapy and were subsequently treated with HAIC at our institute from May 2013 to April 2015 was performed. A total of 24 patients were treated with 5-fluorouracil, and 18 patients were treated with raltitrexed...
February 28, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28197626/kdm6a-and-kdm6b-altered-expression-in-malignant-pleural-mesothelioma
#16
Sian Cregan, Maeve Breslin, Gerard Roche, Sigrid Wennstedt, Lauren MacDonagh, Cinaria Albadri, Yun Gao, Kenneth J O'Byrne, Sinead Cuffe, Stephen P Finn, Steven G Gray
Malignant pleural mesothelioma (MPM) is a rare aggressive cancer of the pleura primarily associated with prior exposure to asbestos. The current standard of care for patients suffering from MPM is a combination of cisplatin and pemetrexed (or alternatively cisplatin and raltitrexed). Most patients, however, die within 24 months of diagnosis. New therapies are therefore urgently required for this disease. Inflammation is thought to be a key element in the pathogenesis of MPM, and recently Kdm6 family members (Kdm6a and Kdm6b) have been identified as playing important roles in inflammatory processes...
March 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28121946/pancreatic-carcinosarcoma-with-rare-long-term-survival-case-report-and-review-of-the-literature
#17
REVIEW
Zhe Jia, Ke Zhang, RongHai Huang, XinGang Zhou, Li Jiang
PATIENT CONCERNS: We report a rare case of pancreatic carcinosarcoma involving a 44-year-old woman. The patient complained of discomfort associated with the upper abdomen and jaundice of skin and sclera for 1 week. DIAGNOSES: After hospitalization, relevant examinations were completed. The disease was diagnosed as carcinoma of the pancreatic head. INTERVENTIONS: Whipple procedure was conducted in May 2013. Intraoperative exploration indicated 2 components of the tumor: a fish-shaped gray matter and a hard structure similar to cancellous bone...
January 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28032528/chemotherapy-rechallenge-after-regorafenib-treatment-in-metastatic-colorectal-cancer-still-hope-after-the-last-hope
#18
Paola Bertocchi, Francesca Aroldi, Tiziana Prochilo, Fausto Meriggi, Giordano Domenico Beretta, Alberto Zaniboni
INTRODUCTION: The introduction of biological agents in cancer therapy is changing the progression of metastatic colorectal cancer. Currently, resistance to biological agents is an emerging problem; the progression of the disease is caused by the development of resistant clones. According to some authors, these clones can be re-sensitized to traditional and previously utilized chemotherapy agents. The results of the CORRECT study demonstrated the efficacy of regorafenib monotherapy in both KRAS wild type and mutant pretreated patients (pts)...
April 2017: Journal of Chemotherapy
https://www.readbyqxmd.com/read/27936107/structural-analysis-of-thymidylate-synthase-from-kaposi-s-sarcoma-associated-herpesvirus-with-the-anticancer-drug-raltitrexed
#19
Yong Mi Choi, Hyun Ku Yeo, Young Woo Park, Jae Young Lee
Kaposi's sarcoma-associated herpesvirus (KSHV) is a highly infectious human herpesvirus that causes Kaposi's sarcoma. KSHV encodes functional thymidylate synthase, which is a target for anticancer drugs such as raltitrexed or 5-fluorouracil. Thymidylate synthase catalyzes the conversion of 2'-deoxyuridine-5'-monophosphate (dUMP) to thymidine-5'-monophosphate (dTMP) using 5,10-methylenetetrahydrofolate (mTHF) as a co-substrate. The crystal structures of thymidylate synthase from KSHV (apo), complexes with dUMP (binary), and complexes with both dUMP and raltitrexed (ternary) were determined at 1...
2016: PloS One
https://www.readbyqxmd.com/read/27703008/the-role-of-folate-transport-in-antifolate-drug-action-in-trypanosoma-brucei
#20
Simon Dewar, Natasha Sienkiewicz, Han B Ong, Richard J Wall, David Horn, Alan H Fairlamb
The aim of this study was to identify and characterize mechanisms of resistance to antifolate drugs in African trypanosomes. Genome-wide RNAi library screens were undertaken in bloodstream form Trypanosoma brucei exposed to the antifolates methotrexate and raltitrexed. In conjunction with drug susceptibility and folate transport studies, RNAi knockdown was used to validate the functions of the putative folate transporters. The transport kinetics of folate and methotrexate were further characterized in whole cells...
November 18, 2016: Journal of Biological Chemistry
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