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chloroquine resistance

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https://www.readbyqxmd.com/read/28106079/modification-of-tumour-cell-metabolism-modulates-sensitivity-to-chk1-inhibitor-induced-dna-damage
#1
Andrew J Massey
Chk1 kinase inhibitors are currently under clinical investigation as potentiators of cytotoxic chemotherapy and demonstrate potent activity in combination with anti-metabolite drugs that increase replication stress through the inhibition of nucleotide or deoxyribonucleotide biosynthesis. Inhibiting other metabolic pathways critical for the supply of building blocks necessary to support DNA replication may lead to increased DNA damage and synergy with an inhibitor of Chk1. A screen of small molecule metabolism modulators identified combinatorial activity between a Chk1 inhibitor and chloroquine or the LDHA/LDHB inhibitor GSK 2837808A...
January 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28101344/evaluation-of-pharmacological-relaxation-effect-of-the-natural-product-naringin-on-in-vitro-cultured-airway-smooth-muscle-cells-and-in-vivo-ovalbumin-induced-asthma-balb-c-mice
#2
Yue Wang, Yun Lu, Mingzhi Luo, Xiaohao Shi, Yan Pan, Huilong Zeng, Linhong Deng
Asthma has become a common chronic respiratory disease worldwide and its prevalence is predicted to continue increasing in the next decade, particularly in developing countries. A key component in asthma therapy is to alleviate the excessive bronchial airway narrowing ultimately due to airway smooth muscle contraction, which is often facilitated by a smooth muscle relaxant, such as the β2-adrenergic agonists. Recently, bitter taste receptor (TAS2R) agonists, including saccharin and chloroquine, have been found to potently relax the airway smooth muscle cells (ASMCs) via intracellular Ca(2+) signaling...
December 2016: Biomedical Reports
https://www.readbyqxmd.com/read/28094001/autophagy-inhibition-overcomes-multiple-mechanisms-of-resistance-to-braf-inhibition-in-brain-tumors
#3
Jean M Mulcahy Levy, Shadi Zahedi, Andrea M Griesinger, Andrew Morin, Kurtis D Davies, Dara L Aisner, B K Kleinschmidt-DeMasters, Brent E Fitzwalter, Megan L Goodall, Jacqueline Thorburn, Vladimir Amani, Andrew M Donson, Diane K Birks, David M Mirsky, Todd C Hankinson, Michael H Handler, Adam L Green, Rajeev Vibhakar, Nicholas K Foreman, Andrew Thorburn
Kinase inhibitors are effective cancer therapies, but tumors frequently develop resistance. Current strategies to circumvent resistance target the same or parallel pathways. We report here that targeting a completely different process, autophagy, can overcome multiple BRAF inhibitor resistance mechanisms in brain tumors. BRAF(V600E)mutations occur in many pediatric brain tumors. We previously reported that these tumors are autophagy-dependent and a patient was successfully treated with the autophagy inhibitor chloroquine after failure of the BRAF(V600E) inhibitor vemurafenib, suggesting autophagy inhibition overcame the kinase inhibitor resistance...
January 17, 2017: ELife
https://www.readbyqxmd.com/read/28086777/profile-of-molecular-mutations-in-pfdhfr-pfdhps-pfmdr1-and-pfcrt-genes-of-plasmodium-falciparum-related-to-resistance-to-different-anti-malarial-drugs-in-the-bata-district-equatorial-guinea
#4
Pedro Berzosa, Andrés Esteban-Cantos, Luz García, Vicenta González, Marisa Navarro, Taiomara Fernández, María Romay-Barja, Zaida Herrador, José Miguel Rubio, Policarpo Ncogo, María Santana-Morales, Basilio Valladares, Matilde Riloha, Agustín Benito
BACKGROUND: The emergence of drug resistance in Plasmodium falciparum has been a major contributor to the global burden of malaria. Drug resistance complicates treatment, and it is one of the most important problems in malaria control. This study assessed the level of mutations in P. falciparum genes, pfdhfr, pfdhps, pfmdr1, and pfcrt, related to resistance to different anti-malarial drugs, in the Continental Region of Equatorial Guinea, after 8 years of implementing artesunate combination therapies as the first-line treatment...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#5
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Sabroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasites lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites equivalent to the known antimalarials, chloroquine and mefloquine...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28075474/isomahanine-induces-endoplasmic-reticulum-stress-and-simultaneously-triggers-p38%C3%A2-mapk-mediated-apoptosis-and-autophagy-in-multidrug-resistant-human-oral-squamous-cell-carcinoma-cells
#6
Tanyarath Utaipan, Anan Athipornchai, Apichart Suksamrarn, Surasak Chunsrivirot, Warangkana Chunglok
Advanced oral squamous cell carcinoma (OSCC) is typically aggressive and closely correlated with disease recurrence and poor survival. Multidrug resistance (MDR) is the most critical problem leading to therapeutic failure. Investigation of novel anticancer candidates targeting multidrug-resistant OSCC cells may provide a basis for developing effective strategies for OSCC treatment. In the present study, we investigated the cytotoxic mechanism of a carbazole alkaloid, namely isomahanine, in a multidrug‑resistant OSCC cell line CLS-354/DX...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/28068997/absence-of-in-vivo-selection-for-k13-mutations-after-artemether-lumefantrine-treatment-in-uganda
#7
Betty Balikagala, Toshihiro Mita, Mie Ikeda, Miki Sakurai, Shouki Yatsushiro, Nobuyuki Takahashi, Shin-Ichiro Tachibana, Mary Auma, Edward H Ntege, Daisuke Ito, Eizo Takashima, Nirianne Marie Q Palacpac, Thomas G Egwang, Joseph Okello Onen, Masatoshi Kataoka, Eisaku Kimura, Toshihiro Horii, Takafumi Tsuboi
BACKGROUND: Individual drug treatment may select resistant parasites in the human body, a process termed in vivo selection. Some single nucleotide polymorphisms in Plasmodium falciparum chloroquine-resistance transporter (pfcrt) and multidrug resistance gene 1 (pfmdr1) genes have been reportedly selected after artemether-lumefantrine treatment. However, there is a paucity of data regarding in vivo selection of P. falciparum Kelch propeller domain (pfkelch13) polymorphisms, responsible for artemisinin-resistance in Asia, and six putative background mutations for artemisinin resistance; D193Y in ferredoxin, T484I in multiple resistance protein 2, V127M in apicoplast ribosomal protein S10, I356T in pfcrt, V1157L in protein phosphatase and C1484F in phosphoinositide-binding protein...
January 9, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28055207/octaminomycins-a-and-b-cyclic-octadepsipeptides-active-against-plasmodium-falciparum
#8
Jun-Pil Jang, Toshihiko Nogawa, Yushi Futamura, Takeshi Shimizu, Daisuke Hashizume, Shunji Takahashi, Jae-Hyuk Jang, Jong Seog Ahn, Hiroyuki Osada
Two new cyclic octadepsipeptides, octaminomycins A (1) and B (2), were isolated from a microbial metabolite fraction library of Streptomyces sp. RK85-270 based on Natural Products Plot screening. Their structures were elucidated on the basis of HRESIMS, 1D and 2D NMR spectroscopic data, and MS/MS experiments for sequence analysis. The absolute configurations of the constituent amino acid residues were determined by a combination of single-crystal X-ray diffraction and Marfey's methodology. Notably, octaminomycins A (1) and B (2) showed good in vitro antiplasmodial activity against chloroquine-sensitive as well as chloroquine-resistant strains with no cytotoxicity up to 30 μM...
January 5, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28035111/comparison-of-who-mark-iii-and-hrp-ii-elisa-for-in-vitro-sensitivity-of-plasmodium-falciparum
#9
Supriya Sharma, Neelima Mishra, Neena Valecha, Anupkumar R Anvikar
BACKGROUND & OBJECTIVES: Antimalarial drug resistance is a serious challenge to malaria control worldwide. In vitro sensitivity assays provide an early indication of emerging drug resistance. In vitro susceptibility of field and culture adapted Plasmodium falciparum isolates to different antimalarials was compared using two Methods: World Health Organization (WHO) micro-test (MARK III) and histidine rich protein II (HRP II) based enzyme- linked immunosorbent assay (ELISA). METHODS: In total, 50 P...
October 2016: Journal of Vector Borne Diseases
https://www.readbyqxmd.com/read/28031151/new-derivatives-of-7-chloroquinolin-4-amine-with-antiprotozoal-activity
#10
Johanna Faist, Clemens Hinteregger, Werner Seebacher, Robert Saf, Pascal Mäser, Marcel Kaiser, Robert Weis
Novel ω-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitrypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising...
December 18, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28028628/risk-of-drug-resistance-in-plasmodium-falciparum-malaria-therapy-a-systematic-review-and-meta-analysis
#11
Li-Juan Zhou, Jing Xia, Hai-Xia Wei, Xiao-Jun Liu, Hong-Juan Peng
Plasmodium falciparum is responsible for the vast majority of the morbidity and mortality associated with malaria infection globally. Although a number of studies have reported the emergence of drug resistance in different therapies for P. falciparum infection, the degree of the drug resistance in different antimalarials is still unclear. This research investigated the risk of drug resistance in the therapies with different medications based on meta-analyses. Relevant original randomized control trials (RCTs) were searched in all available electronic databases...
December 27, 2016: Parasitology Research
https://www.readbyqxmd.com/read/28025112/digestomics-an-emerging-strategy-for-comprehensive-analysis-of-protein-catabolism
#12
REVIEW
Travis S Bingeman, David H Perlman, Douglas G Storey, Ian A Lewis
When cells mobilize nutrients from protein, they generate a fingerprint of peptide fragments that reflects the net action of proteases and the identities of the affected proteins. Analyzing these mixtures falls into a grey area between proteomics and metabolomics that is poorly served by existing technology. Herein, we describe an emerging digestomics strategy that bridges this gap and allows mixtures of proteolytic fragments to be quantitatively mapped with an amino acid level of resolution. We describe recent successes using this technique, including a case where digestomics provided the link between hemoglobin digestion by the malaria parasite and the world-wide distribution of chloroquine resistance...
December 22, 2016: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/28012840/synthesis-and-biological-characterisation-of-ester-and-amide-derivatives-of-fusidic-acid-as-antiplasmodial-agents
#13
Marlene Espinoza-Moraga, Kawaljit Singh, Mathew Njoroge, Gurminder Kaur, John Okombo, Carmen De Kock, Peter J Smith, Sergio Wittlin, Kelly Chibale
A series of novel fusidic acid (FA) derivatives was synthesized by replacing the carboxylic acid group with various ester and amide groups and evaluated in vitro for their antiplasmodial activity against the chloroquine-sensitive NF54 and multidrug-resistant K1 strains of the malarial parasite Plasmodium falciparum. Most of these derivatives showed a 4-49 and 5-17-fold increase in activity against NF54 and KI strains, respectively, as compared to FA and had a good selectivity index. These derivatives are stable over the incubation period and do not appear to be prodrugs of fusidic acid...
November 25, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27997206/nanomolar-antimalarial-agents-against-chloroquine-resistant-plasmodium-falciparum-from-medicinal-plants-and-their-structure-activity-relationships
#14
Bin Zhou, Yan Wu, Seema Dalal, Emilio F Merino, Qun-Fang Liu, Cheng-Hui Xu, Tao Yuan, Jian Ding, David G I Kingston, Maria B Cassera, Jian-Min Yue
Inspired by the discovery of the antimalarial drug artemisinin from a traditional Chinese medicine (TCM), a natural product library of 44 lindenane-type sesquiterpenoids was assessed for activities against the Dd2 chloroquine-resistant strain of the malaria parasite Plasmodium falciparum. These compounds were mainly isolated from plants of the Chloranthus genus, many species of which are named "Sikuaiwa" in TCM and have long been used to treat malaria. The compounds consisted of 41 sesquiterpenoid dimers and three monomers, including the 12 new dimers 1-12 isolated from Chloranthus fortunei...
December 20, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27988484/fixed-dose-artesunate-amodiaquine-combination-vs-chloroquine-for-treatment-of-uncomplicated-blood-stage-p-vivax-infection-in-the-brazilian-amazon-an-open-label-randomized-controlled-trial
#15
Andre M Siqueira, Aline C Alencar, Gisely C Melo, Belisa L Magalhaes, Kim Machado, Aristóteles C Alencar Filho, Andrea Kuehn, Marly M Marques, Monica Costa Manso, Ingrid Felger, José L F Vieira, Valerie Lameyre, Claudio T Daniel-Ribeiro, Marcus V G Lacerda
BACKGROUND: Despite increasing evidence of the development of Plasmodium vivax chloroquine (CQ) resistance, there have been no trials comparing its efficacy with that of artemisinin-based combination therapies (ACTs) in Latin America. METHODS: This randomized controlled trial compared the antischizontocidal efficacy and safety of a 3-day supervised treatment of the fixed-dose combination artesunate-amodiaquine Winthrop(®) (ASAQ) versus CQ for treatment of uncomplicated P...
January 15, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27956423/synthesis-and-evaluation-of-chirally-defined-side-chain-variants-of-7-chloro-4-aminoquinoline-to-overcome-drug-resistance-in-malaria-chemotherapy
#16
Vasantha Rao Dola, Awakash Soni, Pooja Agarwal, Hafsa Ahmad, Kanumuri Siva Rama Raju, Mamunur Rashid, Muhammad Wahajuddin, Kumkum Srivastava, W Haq, A K Dwivedi, S K Puri, S B Katti
A novel 4-aminoquinoline derivative ((S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate) exhibiting curative activity against chloroquine resistant malaria parasite has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed SAR studies, has good solid state properties, and has promising activity against in vitro and in vivo experimental malaria models. The in vitro ADME parameters have indicated favourable drug like profile...
December 12, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27941537/autophagy-inhibitors-chloroqiune-and-ly294002-enhance-temozolomide-cytotoxicity-on-cutaneous-melanoma-cell-lines-in-vitro
#17
Oxana O Ryabaya, Andrey N Inshakov, Angelina V Egorova, Marina A Emelyanova, Tatiana V Nasedkina, Alexander S Zasedatelev, Dmitry A Khochenkov, Evgenia V Stepanova
Patients with metastatic melanoma are difficult to treat and have a very poor prognosis because of high resistance to therapy. Recent evidence indicates that tumors could overcome death through autophagy, a survival mechanism, which cancer cells use under lack of energy and nutrient deprivation. Melanoma cells have different sensitivity to temozolomide (TMZ) treatment. In this study, we showed that the combination of autophagy inhibitors chloroquine or LY294002 and TMZ induced enhanced cytotoxicity of alkylating agents on human melanoma cell lines...
December 9, 2016: Anti-cancer Drugs
https://www.readbyqxmd.com/read/27934832/in-vitro-sensitivity-pattern-of-chloroquine-and-artemisinin-in-plasmodium-falciparum
#18
Supriya Sharma, Kamlesh Kaitholia, Neelima Mishra, Bina Srivastava, C R Pillai, Neena Valecha, Anupkumar R Anvikar
Artemisinin (ART) and its derivatives form the mainstay of antimalarial therapy. Emergence of resistance to them poses a potential threat to future malaria control and elimination on a global level. It is important to know the mechanism of action of drug and development of drug resistance. We put forwards probable correlation between the mode of action of chloroquine (CQ) and ART. Modified trophozoite maturation inhibition assay, WHO Mark III assay and molecular marker study for CQ resistance at K76T codon in Plasmodium falciparum CQ-resistant transporter gene were carried out on cultured P...
October 2016: Indian Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27919892/significant-divergence-in-sensitivity-to-antimalarial-drugs-between-neighboring-plasmodium-falciparum-populations-along-the-eastern-border-of-myanmar
#19
Weilin Zeng, Yao Bai, Meilian Wang, Zenglei Wang, Shuang Deng, Yonghua Ruan, Shi Feng, Zhaoqing Yang, Liwang Cui
Malaria parasites in different endemic areas display different levels of resistance to antimalarial drugs as the result of varied drug use histories. To provide updated knowledge of drug sensitivities during the malaria elimination phase in Southeast Asia, an epicenter of multidrug resistance, we determined in vitro susceptibilities of culture-adapted Plasmodium falciparum isolates from two eastern border regions (Wa and Kachin) of Myanmar to ten drugs. Despite their close proximity, the Kachin parasites displayed higher IC50 values than the Wa parasites to chloroquine, piperaquine, naphthoquine, mefloquine, quinine, pyrimethamine, pyronaridine, lumefantrine and dihydroartemisinin...
December 5, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27919256/the-return-of-chloroquine-susceptible-plasmodium-falciparum-malaria-in-zambia
#20
Sydney Mwanza, Sudhaunshu Joshi, Michael Nambozi, Justin Chileshe, Phidelis Malunga, Jean-Bertin Bukasa Kabuya, Sebastian Hachizovu, Christine Manyando, Modest Mulenga, Miriam Laufer
BACKGROUND: Plasmodium falciparum resistance to anti-malarial drugs remains a major obstacle to malaria control and elimination. The parasite has developed resistance to every anti-malarial drug introduced for wide-scale treatment. However, the spread of resistance may be reversible. Malawi was the first country to discontinue chloroquine use due to widespread resistance. Within a decade of the removal of drug pressure, the molecular marker of chloroquine-resistant malaria had disappeared and the drug was shown to have excellent clinical efficacy...
December 5, 2016: Malaria Journal
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