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1

Ghanim, Viviane, Harald Herrmann, Gerwin Heller, et al. "5-azacytidine and decitabine exert proapoptotic effects on neoplastic mast cells: role of FAS-demethylation and FAS re-expression, and synergism with FAS-ligand." Blood 119, no. 18 (2012): 4242–52. http://dx.doi.org/10.1182/blood-2011-09-382770.

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Abstract Aggressive systemic mastocytosis (ASM) and mast cell leukemia (MCL) are advanced hematopoietic neoplasms with poor prognosis. In these patients, neoplastic mast cells (MCs) are resistant against various drugs. We examined the effects of 2 demethylating agents, 5-azacytidine and decitabine on growth and survival of neoplastic MCs and the MC line HMC-1. Two HMC-1 subclones were used, HMC-1.1 lacking KIT D816V and HMC-1.2 exhibiting KIT D816V. Both agents induced apoptosis in HMC-1.1 and HMC-1.2 cells. Decitabine, but not 5-azacytidine, also produced a G2/M cell-cycle arrest in HMC-1 cel
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2

Schneeweiss-Gleixner, Mathias, Yüksel Filik, Gabriele Stefanzl, et al. "CDK4/CDK6 Inhibitors Synergize with Midostaurin, Avapritinib, and Nintedanib in Inducing Growth Inhibition in KIT D816V+ Neoplastic Mast Cells." Cancers 14, no. 13 (2022): 3070. http://dx.doi.org/10.3390/cancers14133070.

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In most patients with advanced systemic mastocytosis (AdvSM), neoplastic mast cells (MC) express KIT D816V. However, despite their disease-modifying potential, KIT D816V-targeting drugs, including midostaurin and avapritinib, may not produce long-term remissions in all patients. Cyclin-dependent kinase (CDK) 4 and CDK6 are promising targets in oncology. We found that shRNA-mediated knockdown of CDK4 and CDK6 results in growth arrest in the KIT D816V+ MC line HMC-1.2. The CDK4/CDK6 inhibitors palbociclib, ribociclib, and abemaciclib suppressed the proliferation in primary neoplastic MC as well
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3

Ghanim, Viviane, Harald Herrmann, Emir Hadzijusufovic, et al. "5-Azacytidine and Decitabine Induce FAS Re-Expression, Exert Major Proapoptotic Effects, and Cooperate with the FAS Ligand in Producing Apoptosis in Neoplastic Human Mast Cells,." Blood 118, no. 21 (2011): 3457. http://dx.doi.org/10.1182/blood.v118.21.3457.3457.

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Abstract Abstract 3457 Aggressive systemic mastocytosis (ASM) and mast cell leukemia (MCL) are advanced myeloid neoplasms with a poor prognosis. In these patients, neoplastic mast cells (MC) are resistant against most conventional drugs. Demethylating agents reportedly exert beneficial effects in several advanced myelogenous neoplasms, including myelodysplastic syndromes. We examined the effects of two demethylating agents, 5-Azacytidine and 5-Aza-2`Deoxycytidine (Decitabine) on growth and survival (apoptosis) of neoplastic MC and the human MC line HMC-1. Two HMC-1 subclones were used, HMC-1.1
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4

Ubertini, Valentina, Frida Ponthan, Aude-Marine Bonavita, and James Wilson. "Abstract 2754: Transwell-grown monolayers derived from small intestinal organoids to study the effects of tight junction modulators that may improve the absorption of orally-administered, anti-neoplastic drugs." Cancer Research 83, no. 7_Supplement (2023): 2754. http://dx.doi.org/10.1158/1538-7445.am2023-2754.

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Abstract Although oral dosing is the most convenient route of drug administration, most anti-neoplastic drugs are administered intravenously due to poor bioavailability because of the epithelial barriers. A major organ involved in oral drug absorption is the small intestine where enterocytes are linked together by tight junctions (TJs). TJs regulate paracellular transport by creating a selectively permeable barrier to small molecules, ions, and water, thereby restricting the uptake of drugs. Transient modulation of the TJs is considered a potential strategy to improve drug delivery. Human smal
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5

Tomas Koltai. "Fundamentals for the repurposing of hydralazine as an anti-neoplastic drug." World Journal of Advanced Pharmaceutical and Life Sciences 5, no. 1 (2023): 012–23. http://dx.doi.org/10.53346/wjapls.2023.5.1.0075.

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Hydralazine (HDZ) is a drug patented in 1949 that has been used for the treatment of arterial hypertension since 1953. New and better anti-hypertensive drugs have almost moved HDZ into oblivion. Interestingly, anti-cancer effects were found and this drug is seriously being considered for repurposing it for cancer treatment. The main mechanism of action against tumors seems to be its ability to act as a demethylator agent. By demethylating the promoter region of tumor suppressor genes HDZ seems to restore the effects of these genes, which are frequently inhibited in cancer through epigenetic me
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6

Schneeweiss, Mathias A., Gabriele Stefanzl, Daniela Berger, et al. "The CDK4/6 Inhibitor Palbociclib Exerts Growth-Inhibitory Effects on Neoplastic Mast Cells and Synergizes with Midostaurin in Producing Growth Arrest." Blood 132, Supplement 1 (2018): 1363. http://dx.doi.org/10.1182/blood-2018-99-116525.

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Abstract Aggressive systemic mastocytosis (ASM) and mast cell leukemia (MCL) are rare, malignant diseases with an unfavorable prognosis. In a majority of patients, the transforming KIT mutation D816V is detectable. Currently, several drugs are available for the treatment of ASM/MCL, including midostaurin, a KIT D816V-targeting drug that has recently been approved for the treatment of advanced SM in the US and in Europe. However, when applied as single drug, midostaurin usually fails to induce durable remissions in patients with ASM/MCL, and the same holds true for all other drugs tested in the
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7

Gleixner, K. V., M. Mayerhofer, A. Vales, et al. "The Hsp32/HO-1-targeted drug SMA-ZnPP counteracts the proliferation and viability of neoplastic cells in solid tumors and hematologic neoplasms." Journal of Clinical Oncology 25, no. 18_suppl (2007): 14122. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.14122.

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14122 Background: Heat shock protein 32 (Hsp32) is a stress-related survival factor that is overexpressed in various neoplastic cells. Recently, specific Hsp32- targeting drugs such as styrene maleic acid encapsulated zinc protoporphyrin (SMA-ZnPP) have been developed. Methods: We examined the effects of SMA-ZnPP on proliferation and survival of various tumor cell-lines, including U97MG (glioblastoma), A549 (lung cancer), MDA-MB-231 (breast cancer), BxPC-3 (pancreatic), HepG2 (hepatocellular), Colo201, Colo320DM, DLD-1 (colon), OvCar3 (ovarian carcinoma), KG1, U937, HL60, K562 (myeloid leukemi
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8

Ubertini, Valentina, Stephanie French, James Wilson, and Frida Ponthan. "Abstract 374: Small intestinal organoids to study the effects of tight junction modulators that may improve the absorption of orally-administered, anti-neoplastic drugs." Cancer Research 82, no. 12_Supplement (2022): 374. http://dx.doi.org/10.1158/1538-7445.am2022-374.

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Abstract Although oral dosing is the most convenient route of drug administration, most anti-neoplastic drugs are administered intravenously due to poor bioavailability because of the epithelial barriers. A major organ involved in oral drug absorption is the small intestine where enterocytes are linked together by tight junctions (TJs). TJs regulate paracellular transport by creating a selectively-permeable barrier to small molecules, ions and water, thereby restricting the uptake of drugs. Transient modulation of the TJs is considered a potential strategy to improve drug delivery. Human small
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9

Hari, Dr Anupama, Dr Bushra Shereen, and Dr J. Sreeja Shraddha. "Anti-Neoplastic Drug Exposure in Pregnancy and Fetal Haemorrhage: A Rare Teratogenicity." Scholars International Journal of Obstetrics and Gynecology 5, no. 3 (2022): 130–32. http://dx.doi.org/10.36348/sijog.2022.v05i03.011.

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Anti-neoplastic drugs are known to have teratogenic effects on the fetus. In this case report we are presenting a case of a patient who got operated for breast carcinoma, conceived while on chemotherapy and underwent termination of pregnancy in the second trimester. Fetal haemorrhage and ecchymosis lead to further evaluation of the case, which revealed fetal thrombocytopenia, a rare teratogenic effect of the anti-neoplastic drugs.
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10

Wedeh, Ghaith, Emir Hadzijusufovic, Sabine Cerny-Reiterer, et al. "Bromodomain-Containing Protein 4 (BRD4): A Novel Marker and Drug Target Expressed In Neoplastic Cells In Advanced Mast Cell Neoplasms." Blood 122, no. 21 (2013): 3747. http://dx.doi.org/10.1182/blood.v122.21.3747.3747.

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Abstract Advanced mast cell (MC) neoplasms are characterized by uncontrolled growth and rapid expansion of neoplastic MC in various organ systems and a poor prognosis. In human patients, advanced systemic mastocytosis (SM) is rare and usually presents as aggressive SM (ASM) or mast cell leukemia (MCL). In canines, advanced MC tumors (MCT) are considered one of the most frequent skin tumors. Hence, so far, no effective treatment concept has been established for advanced MC neoplasms in humans or canines. This is due to the fact that neoplastic MC in advanced SM usually are resistant against var
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11

Gleixner, Karoline V., Matthias Mayerhofer, Sabine Cerny-Reiterer, et al. "KIT-D816V–independent oncogenic signaling in neoplastic cells in systemic mastocytosis: role of Lyn and Btk activation and disruption by dasatinib and bosutinib." Blood 118, no. 7 (2011): 1885–98. http://dx.doi.org/10.1182/blood-2010-06-289959.

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Abstract Systemic mastocytosis (SM) either presents as a malignant neoplasm with short survival or as an indolent disease with normal life expectancy. In both instances, neoplastic mast cells (MCs) harbor D816V-mutated KIT, suggesting that additional oncogenic mechanisms are involved in malignant transformation. We here describe that Lyn and Btk are phosphorylated in a KIT-independent manner in neoplastic MCs in advanced SM and in the MC leukemia cell line HMC-1. Lyn and Btk activation was not only detected in KIT D816V-positive HMC-1.2 cells, but also in the KIT D816V-negative HMC-1.1 subclon
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12

Gleixner, Karoline V., Katharina Blatt, Barbara Peter, Emir Hadzijusufovic, and Peter Valent. "Ponatinib Exerts Growth-Inhibitory Effects on Neoplastic Mast Cells and Synergizes with Midostaurin in Producing Growth Arrest and Apoptosis,." Blood 118, no. 21 (2011): 3497. http://dx.doi.org/10.1182/blood.v118.21.3497.3497.

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Abstract Abstract 3497 Aggressive systemic mastocytosis (ASM) and mast cell leukemia (MCL) have a poor prognosis. In these patients, neoplastic mast cells (MC) usually harbor the D816V-mutated variant of KIT and are resistant to conventional cytoreductive drugs and to several tyrosine kinase inhibitors (TKI) such as imatinib. More recently, various KIT kinase blockers including midostaurin (PKC412), have been described to overcome KIT D816V-mediated resistance in neoplastic MC. However, despite encouraging first results observed in clinical trials, these novel kinase blockers are unable to ind
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13

K, . Gnanankitha, . Lahari A, Poojitha V., Bhanuji Rao Paila., and Phani Satyavathi Nimmala. "Platinum –Based Anti Neoplastic Drugs and Hematotoxicity: Challenges in Cancer Treatmemt." International Journal of Innovative Science and Research Technology (IJISRT) 10, no. 2 (2025): 1154–58. https://doi.org/10.5281/zenodo.14959376.

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Platinum-based chemotherapy agents, such as cisplatin, carboplatin, and oxaliplatin, are essential in cancer treatment due to their ability to disrupt DNA replication and induce the death of tumor cells. However, their use is often linked with significant hematologic toxicities, particularly myelosuppression, which can lead to conditions like anemia, neutropenia, and thrombocytopenia. These side effects may require dose adjustments, treatment delays, and increase the likelihood of infections and bleeding complications. This article delves into the mechanisms of hematotoxicity linked to platinu
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14

Davis, Megan, and Kiko Bracker. "Retrospective Study of 122 Dogs That Were Treated with the Antifibrinolytic Drug Aminocaproic Acid: 2010–2012." Journal of the American Animal Hospital Association 52, no. 3 (2016): 144–48. http://dx.doi.org/10.5326/jaaha-ms-6298.

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ABSTRACT Antifibrinolytic drugs are used to promote hemostasis and decrease the need for red blood cell transfusion. Medical records of 122 dogs that were prescribed either oral or intravenous aminocaproic acid between 2010 and 2012 were evaluated retrospectively. Of the 122 dogs, three experienced possible drug-related adverse effects. No significant differences were identified between dogs that experienced adverse effects and those that did not and the possible adverse effects noted were all minor. All dogs that received packed red blood cell transfusions were evaluated for correlations betw
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15

Aichberger, Karl J., Karoline V. Gleixner, Irina Mirkina, et al. "Identification of proapoptotic Bim as a tumor suppressor in neoplastic mast cells: role of KIT D816V and effects of various targeted drugs." Blood 114, no. 26 (2009): 5342–51. http://dx.doi.org/10.1182/blood-2008-08-175190.

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Abstract Systemic mastocytosis (SM) is a myeloid neoplasm involving mast cells (MCs) and their progenitors. In most cases, neoplastic cells display the D816V-mutated variant of KIT. KIT D816V exhibits constitutive tyrosine kinase (TK) activity and has been implicated in increased survival and growth of neoplastic MCs. Recent data suggest that the proapoptotic BH3-only death regulator Bim plays a role as a tumor suppressor in various myeloid neoplasms. We found that KIT D816V suppresses expression of Bim in Ba/F3 cells. The KIT D816–induced down-regulation of Bim was rescued by the KIT-targetin
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16

Zhang, Yanyan, Ghaith Wedeh, Liang He, et al. "In vitro and in vivo efficacy of an anti-CD203c conjugated antibody (AGS-16C3F) in mouse models of advanced systemic mastocytosis." Blood Advances 3, no. 4 (2019): 633–43. http://dx.doi.org/10.1182/bloodadvances.2018026179.

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Abstract Antibody-drug conjugates (ADCs) are a new class of therapeutics that use antibodies to deliver potent cytotoxic drugs selectively to cancer cells. CD203c, an ecto-nucleotide pyrophosphatase-phosphodiesterase 3, is overexpressed on neoplastic mast cells (MCs) in systemic mastocytosis (SM), thus representing a promising target for antibody-mediated therapy. In this study, we have found that human neoplastic MC lines (ROSAKIT D816V and ROSAKIT D816V-Gluc), which express high levels of CD203c, are highly and specifically sensitive to the antiproliferative effects of an ADC against CD203c
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17

Sundel, Margaret H., Natalia Sampaio Moura, Kunrong Cheng, et al. "Selective Activation of M1 Muscarinic Receptors Attenuates Human Colon Cancer Cell Proliferation." Cancers 15, no. 19 (2023): 4766. http://dx.doi.org/10.3390/cancers15194766.

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M3 muscarinic receptor (M3R) activation stimulates colon cancer cell proliferation, migration, and invasion; M3R expression is augmented in colon cancer and ablating M3R expression in mice attenuates colon neoplasia. Several lines of investigation suggest that in contrast to these pro-neoplastic effects of M3R, M1R plays an opposite role, protecting colon epithelial cells against neoplastic transformation. To pursue these intriguing findings, we examined the relative expression of M1R versus M3R in progressive stages of colon neoplasia and the effect of treating colon cancer cells with selecti
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18

Kondo, Rudin, Karoline V. Gleixner, Matthias Mayerhofer, et al. "Identification of heat shock protein 32 (Hsp32) as a novel survival factor and therapeutic target in neoplastic mast cells." Blood 110, no. 2 (2007): 661–69. http://dx.doi.org/10.1182/blood-2006-10-054411.

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AbstractSystemic mastocytosis (SM) is a myeloid neoplasm characterized by increased survival and accumulation of neoplastic mast cells (MCs). In most patients, the D816V-mutated variant of KIT is detectable. We report here that heat shock protein 32 (Hsp32), also known as heme oxygenase-1 (HO-1), is a novel KIT-inducible survival factor in neoplastic MCs. As assessed by reverse transcription-polymerase chain reaction (RT-PCR), immunocytochemistry, and Western blotting, the KIT D816V+ MC line HMC-1.2 as well as highly enriched primary neoplastic MCs were found to express Hsp32 mRNA and the Hsp3
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19

Petrella, Francesco, Isabella Rimoldi, Stefania Rizzo, and Lorenzo Spaggiari. "Mesenchymal Stromal Cells for Antineoplastic Drug Loading and Delivery." Medicines 4, no. 4 (2017): 87. http://dx.doi.org/10.3390/medicines4040087.

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Mesenchymal stromal cells are a population of undifferentiated multipotent adult cells possessing extensive self-renewal properties and the potential to differentiate into a variety of mesenchymal lineage cells. They express broad anti-inflammatory and immunomodulatory activity on the immune system and after transplantation can interact with the surrounding microenvironment, promoting tissue healing and regeneration. For this reason, mesenchymal stromal cells have been widely used in regenerative medicine, both in preclinical and clinical settings. Another clinical application of mesenchymal s
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20

Gleixner, Karoline V., Matthias Mayerhofer, Karl J. Aichberger, et al. "PKC412 Inhibits In Vitro Growth of Neoplastic Mast Cells Expressing the D816V-Mutated Variant of KIT: Comparison with AMN107 and Imatinib, and Evaluation of Drug-Interactions." Blood 106, no. 11 (2005): 3523. http://dx.doi.org/10.1182/blood.v106.11.3523.3523.

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Abstract In most patients with systemic mastocytosis (SM) including aggressive SM and mast cell leukemia (MCL), neoplastic cells express the oncogenic c-KIT mutation D816V. KIT-D816V is associated with constitutive tyrosine kinase (TK) activity and thus represents an attractive target of drug therapy. However, most available TK inhibitors including STI571=imatinib, fail to block TK-activity of KIT D816V at pharmacologic concentrations. We provide evidence that the novel TK-targeting drugs PKC412 and AMN107 decrease TK-activity of D816V-mutated KIT and counteract growth of Ba/F3 cells with doxy
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21

Serini, Simona, Roberta Cassano, Federica Curcio, Sonia Trombino, and Gabriella Calviello. "Nutraceutical-Based Nanoformulations for Breast and Ovarian Cancer Treatment." International Journal of Molecular Sciences 23, no. 19 (2022): 12032. http://dx.doi.org/10.3390/ijms231912032.

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Different strategies have been investigated for a more satisfactory treatment of advanced breast cancer, including the adjuvant use of omega-3 polyunsaturated fatty acids (PUFAs). These nutritional compounds have been shown to possess potent anti-inflammatory and antiangiogenic activities, the capacity to affect transduction pathways/receptors involved in cell growth and to reprogram tumor microenvironment. Omega-3 PUFA-containing nanoformulations designed for drug delivery in breast cancer were shown to potentiate the effects of enclosed drugs, enhance drug delivery to target sites, and minim
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22

Khosravi, Mohammad Reza, Elham Raeisi, Saeid Heidari-Soureshjani, and Catherine MT Sherwin. "The survey of antitumor effects of bromelain on neoplastic breast cells: A systematic review." Journal of Herbmed Pharmacology 13, no. 1 (2024): 10–18. http://dx.doi.org/10.34172/jhp.2024.48078.

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Background: Breast cancer is one of the most prevalent cancers in women worldwide. Considering the side effects of chemotherapy treatments, we investigated the anticancer effects and mechanisms of bromelain (Br) on breast cancer cells in this systematic review. Methods: The PRISMA recommendations were followed to design this systematic review. Web of Science, PubMed, Cochrane Library, and Scopus were high-coverage databases used for searching. After considering the inclusion and exclusion criteria for the study, 18 articles were included. The desired information was gathered, entered into an E
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23

Gleixner, Karoline V., Matthias Mayerhofer, Karoline Sonneck, et al. "Synergistic Growth-Inhibitory Effects of Two Tyrosine Kinase Inhibitors, Dasatinib and PKC412, on Neoplastic Mast Cells Expressing the D816V-Mutated Oncogenic Variant of KIT." Blood 108, no. 11 (2006): 526. http://dx.doi.org/10.1182/blood.v108.11.526.526.

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Abstract In a majority of all patients with systemic mastocytosis (SM) including aggressive SM and mast cell leukemia (MCL), neoplastic cells display the D816V-mutated variant of KIT. The respective oncoprotein, KIT-D816V, exhibits constitutive tyrosine kinase (TK) activity and has been implicated in malignant cell growth. Therefore, several attempts have been made to identify KIT-D816V-targeting drugs. We found that the TK-inhibitor dasatinib (BMS-354825) inhibits TK activity of wild type (wt) KIT and KIT-D816V in Ba/F3 cells with doxycycline-inducible KIT-expression. In addition, dasatinib w
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24

Hmed, BenNasr, Hammami Turky Serria, and Zeghal Khaled Mounir. "Scorpion Peptides: Potential Use for New Drug Development." Journal of Toxicology 2013 (2013): 1–15. http://dx.doi.org/10.1155/2013/958797.

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Several peptides contained in scorpion fluids showed diverse array of biological activities with high specificities to their targeted sites. Many investigations outlined their potent effects against microbes and showed their potential to modulate various biological mechanisms that are involved in immune, nervous, cardiovascular, and neoplastic diseases. Because of their important structural and functional diversity, it is projected that scorpion-derived peptides could be used to develop new specific drugs. This review summarizes relevant findings improving their use as valuable tools for new d
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25

Gleixner, Karoline Veronika, Matthias Mayerhofer, Gregor Hörmann, et al. "Bosutinib Blocks Lyn and Btk Activation and Synergizes with the KIT D816V-Targeting Drug Midostaurin in Inducing Apoptosis in Neoplastic Human Mast Cells." Blood 114, no. 22 (2009): 1717. http://dx.doi.org/10.1182/blood.v114.22.1717.1717.

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Abstract Abstract 1717 Poster Board I-743 Advanced systemic mastocytosis (SM) is a malignant hematopoietic neoplasm characterized by destructive growth of neoplastic mast cells (MC) in various organ systems. In these patients, the response to conventional cytoreductive therapy is poor and the prognosis is grave. The D816V-mutated variant of c-KIT is found in most patients and is considered to be a major transforming oncoprotein in SM that leads to abnormal survival and growth of neoplastic MC. Therefore, agents interfering with the kinase activity of KIT D816V have been developed. One promisin
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26

Peter, Barbara, Karl J. Aichberger, Karoline V. Gleixner, et al. "Effects of the Mcl-1/Bcl-2 Inhibitor GX015-070 (Obatoclax®) on Growth and Viability of Canine and Human Neoplastic Mast Cells." Blood 112, no. 11 (2008): 861. http://dx.doi.org/10.1182/blood.v112.11.861.861.

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Abstract Mcl-1 is a Bcl-2 family-member that has been described to act anti-apoptotic in various myeloid neoplasms. We and others have recently shown that neoplastic mast cells (MC) in patients with systemic mastocytosis (SM) display Mcl-1, Bcl-2, and Bcl-xL. In the present study, we examined the effects of the Mcl-1/Bcl-2-targeting drug GX015-070 (obatoclax®; GeminX, Montréal, Quebéc, Canada) on growth and viability of primary neoplastic MC obtained from patients with SM (n=3), the human MC leukemia cell line HMC-1, and the canine mastocytoma cell line C2. Two HMC-1 subclones, one lacking K
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27

Andreidesz, Kitti, Aliz Szabo, Dominika Kovacs, et al. "Cytostatic Effect of a Novel Mitochondria-Targeted Pyrroline Nitroxide in Human Breast Cancer Lines." International Journal of Molecular Sciences 22, no. 16 (2021): 9016. http://dx.doi.org/10.3390/ijms22169016.

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Mitochondria have emerged as a prospective target to overcome drug resistance that limits triple-negative breast cancer therapy. A novel mitochondria-targeted compound, HO-5114, demonstrated higher cytotoxicity against human breast cancer lines than its component-derivative, Mito-CP. In this study, we examined HO-5114′s anti-neoplastic properties and its effects on mitochondrial functions in MCF7 and MDA-MB-231 human breast cancer cell lines. At a 10 µM concentration and within 24 h, the drug markedly reduced viability and elevated apoptosis in both cell lines. After seven days of exposure, ev
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28

Laurenzana, Ilaria, Daniela Lamorte, Stefania Trino, et al. "Extracellular Vesicles: A New Prospective in Crosstalk between Microenvironment and Stem Cells in Hematological Malignancies." Stem Cells International 2018 (May 27, 2018): 1–11. http://dx.doi.org/10.1155/2018/9863194.

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The bone marrow (BM) microenvironment in hematological malignancies (HMs) comprises heterogeneous populations of neoplastic and nonneoplastic cells. Cancer stem cells (CSCs), neoplastic cells, hematopoietic stem cells (HSCs), and mesenchymal stromal/stem cells (MSCs) are all components of this microenvironment. CSCs are the HM initiators and are associated with neoplastic growth and drug resistance, while HSCs are able to reconstitute the entire hematopoietic system; finally, MSCs actively support hematopoiesis. In some HMs, CSCs and neoplastic cells compromise the normal development of HSCs a
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29

Hadzijusufovic, Emir, Barbara Peter, Harald Herrmann, et al. "Establishment of a Novel Canine Mastocytoma Cell Line, NI-1: a Model for Studying Resistance Against KIT Tyrosine Kinase Inhibitors In Canine Neoplastic Mast Cells." Blood 116, no. 21 (2010): 4936. http://dx.doi.org/10.1182/blood.v116.21.4936.4936.

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Abstract Abstract 4936 Advanced mast cell (MC) disorders are characterized by uncontrolled growth of neoplastic MC in various organ systems, resistance to conventional cytoreductive drugs, and a poor prognosis. In most patients, transforming mutations in the KIT proto-oncogene are detectable and are considered to contribute to resistance. MC lines are an important model for analyzing drug resistance in neoplastic MC. We have established a novel canine mastocytoma cell line, NI-1 from a canine patient suffering from mast cell leukemia. NI-1 cells were found to harbour several homozygous KIT mut
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30

Ziegler, DK. "Opiate and Opioid Use in Patients With Refractory Headache." Cephalalgia 14, no. 1 (1994): 5–10. http://dx.doi.org/10.1046/j.1468-2982.1994.1401005.x.

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Opiate and opioid analgesics are commonly used for pain in general and presumably for headache. Codeine, oxycodone and propoxyphene, among the most commonly prescribed, do carry some risk of abuse, and their efficacy in headache patients has not been well studied. In many patients with other kinds of pain, however, both of neoplastic and non-neoplastic origin, chronic opiate use has been demonstrated to be of benefit without adverse side effects. The type of headache patient with intractable pain who needs frequent opiate analgesic and who does not develop addiction or drug abuse is an importa
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31

Mathai, Bincy Mariyam, Manu M. Joseph, Santhi Maniganda, et al. "Guanidinium rich dendron-appended hydnocarpin exhibits superior anti-neoplastic effects through caspase mediated apoptosis." RSC Advances 6, no. 58 (2016): 52772–80. http://dx.doi.org/10.1039/c6ra08724h.

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Medicinal plants have truly demonstrated their potential as a repository of active biomolecules with promising therapeutic potential and represent an important source for the identification of novel drug leads.
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32

Blatt, Katharina, Sabine Cerny-Reiterer, Karl Sotlar, et al. "Identification Of The Ki-1 Antigen (CD30) As a Novel Marker and Potential Therapeutic Target In Neoplastic Mast Cells In Advanced Systemic Mastocytosis." Blood 122, no. 21 (2013): 3773. http://dx.doi.org/10.1182/blood.v122.21.3773.3773.

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Abstract Systemic mastocytosis (SM) is a hematologic neoplasm characterized by abnormal expansion and accumulation of neoplastic mast cells (MC) in various organs, including the bone marrow, skin, liver, spleen and gastrointestinal tract. In a majority of all patients, the transforming KIT mutation D816V is detectable. The clinical picture and prognosis in SM vary, depending on the variant of SM and the presence of an associated hematologic non-MC-lineage disease (AHNMD). The WHO classification discriminates between indolent SM (ISM), SM-AHNMD, aggressive SM (ASM) and MC leukemia (MCL). Recent
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33

Efentakis, Panagiotis, Ioanna Andreadou, Konstantinos E. Iliodromitis, et al. "Myocardial Protection and Current Cancer Therapy: Two Opposite Targets with Inevitable Cost." International Journal of Molecular Sciences 23, no. 22 (2022): 14121. http://dx.doi.org/10.3390/ijms232214121.

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Myocardial protection against ischemia/reperfusion injury (IRI) is mediated by various ligands, activating different cellular signaling cascades. These include classical cytosolic mediators such as cyclic-GMP (c-GMP), various kinases such as Phosphatydilinositol-3- (PI3K), Protein Kinase B (Akt), Mitogen-Activated-Protein- (MAPK) and AMP-activated (AMPK) kinases, transcription factors such as signal transducer and activator of transcription 3 (STAT3) and bioactive molecules such as vascular endothelial growth factor (VEGF). Most of the aforementioned signaling molecules constitute targets of a
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34

Karlic, Heidrun, Rene Reitermaier, Viviane Ghanim, et al. "5-Azacytidine and Decitabine Induce Demethylation and Re-Expression of FAS (CD95) and Promote Apoptosis in Neoplastic Cells in Acute Myeloid Leukemia (AML),." Blood 118, no. 21 (2011): 3463. http://dx.doi.org/10.1182/blood.v118.21.3463.3463.

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Abstract Abstract 3463 Epigenetic and apoptosis-regulating mechanisms have been implicated as critical factors contributing to the progression from myelodysplastic syndromes (MDS) to secondary acute myeloid leukemia (AML). However, the exact molecular mechanisms and genes involved in disease evolution have not been identified yet. We screened for epigenetically regulated pro-apoptotic effector molecules in neoplastic cells in patients with MDS (n=50) and AML (n=30). Among a series of potential regulators, we identified FAS (CD95) as an epigenetically regulated critical death regulator in neopl
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35

Gleixner, Karoline V., Matthias Mayerhofer, Uwe Rix, et al. "Delineation of a KIT-Independent Oncogenic Pathway in Neoplastic Mast Cells That Involves Lyn and Btk, and Can Be Disrupted by the KIT/Lyn/Btk-Targeting Drug Dasatinib." Blood 110, no. 11 (2007): 1541. http://dx.doi.org/10.1182/blood.v110.11.1541.1541.

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Abstract Systemic mastocytosis (SM) is a myeloid neoplasm characterized by increased growth and survival of neoplastic mast cells (MC). Aggressive SM (ASM) and MC leukemia (MCL) are advanced disease variants that usually are drug-resistant and have an unfavorable prognosis. In most patients, the D816V-mutated ′oncogenic′ variant of KIT is detectable. However, the mutant is also detectable in patients with indolent SM exhibiting a normal life-expectancy, and therefore is not considered to represent a fully transforming oncoprotein. This assumption is also supported by studies in Ba/F3 cells, an
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36

Ferenc, Veronika, Karoline V. Gleixner, Alexander Gruze, et al. "The Plk-1 Inhibitor BI 2536 Counteracts the Growth of Neoplastic Mast Cells and Synergizes with the KIT D816V-Targeting Drug Midostaurin (PKC412) in Producing Growth-Inhibition." Blood 110, no. 11 (2007): 3554. http://dx.doi.org/10.1182/blood.v110.11.3554.3554.

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Abstract Systemic mastocytosis (SM) is a myeloid neoplasm characterized by abnormal growth and accumulation of mast cells (MC) in various internal organs. In most patients, the D816V-mutated variant of c-KIT, which mediates resistance against several tyrosine kinase (TK) inhibitors like imatinib, is found. In advanced SM, the response of neoplastic MC to conventional drugs is poor and the prognosis is grave. Therefore current research is attempting to identify novel targets in neoplastic MC. Polo-like kinase 1 (Plk-1) is a serine/threonine kinase that plays an essential role in mitosis and has
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37

Sharma, Kopal, Sandeep Jasuja, Monica Jain, and Yatendra Singh. "Assessment of adverse drug reactions in oral cancer patients receiving chemotherapy treatment at tertiary care centres in North-Western India." Scripta Medica 54, no. 1 (2023): 45–51. http://dx.doi.org/10.5937/scriptamed54-42967.

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Background/Aim: Pharmacovigilance in oncology is imperative as antineoplastic drugs are two-edged swords whose irrational use can pose a major health problem and a needless financial burden on the patient. The aim of this study was to study the comprehensive safety profile of anti-neoplastic drugs used for treating oral cancers. Methods: This hospital-based prospective observational study was conducted at two premiers (a government and a private) tertiary care centres in North-Western India among newly diagnosed cases of oral cancers of both sexes between the ages of 20-70 years and requiring
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38

Dyrka, Kamil, Agata Czarnywojtek, Magdalena Borowska, et al. "Temozolomide: a cytostatic drug that is still important today." Acta Poloniae Pharmaceutica - Drug Research 79, no. 6 (2023): 763–75. http://dx.doi.org/10.32383/appdr/159449.

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TMZ has an advantage over other traditional alkylating agents (carmustine, lomustine, procarbazine), which are highly toxic and have poor patient survival. TMZ circumvents these problems because cytochrome P450 enzymes and the kidneys are not involved in its metabolism, it has predictable side effects (nausea, vomiting, thrombocytopenia, neutropenia), which are usually reversible and only mild to moderate, have been widely described. About half of patients treated with TMZ have high drug resistance induced by activity of O6-methylguanine methyltransferase. Cancer stem cells (CSCs), which are f
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39

Cassidy, Róisín M., Sharon L. McKenna, and Órla P. Barry. "Evaluation of Cytotoxic Activity of Epigenetic Drugs in Oesophageal Squamous Cell Carcinoma." European Journal of Medical and Health Sciences 5, no. 2 (2023): 25–36. http://dx.doi.org/10.24018/ejmed.2023.5.2.1618.

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Oesophageal squamous cell carcinoma (OESCC) is a poor prognosis cancer with current treatments demonstrating limited efficacy. Recently, the field of epigenetics has gained equal importance to that of genetics in cancer, including in oesophageal cancer. The increasing number of epigenetic drugs is driving the need to identify the most efficacious and potent of these drugs in various cancers. This study investigated both the metabolic activity and importantly, the long-term cytotoxic effects of different families of epigenetic drugs including DNA methyltransferase inhibitors (DNMTi: azacitidine
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40

Peter, Barbara, Katharina Blatt, Gabriele Stefanzl, et al. "The Midostaurin (PKC412) Metabolite CGP52421 Shows Little Growth-Inhibitory Activity Against Against Neoplastic Mast Cells but Retains Inhibitory Effects on IgE-Dependent Activation and Histamine Release." Blood 118, no. 21 (2011): 1417. http://dx.doi.org/10.1182/blood.v118.21.1417.1417.

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Abstract Abstract 1417 The multikinase inhibitor midostaurin (PKC412) is currently tested in clinical trials in patients with advanced systemic mastocytosis (SM). Although clinical symptoms improve in many patients and sometimes the proliferation of neoplastic mast cells (MC) can be kept under control for some time, most patients progress after a variable latency period, even if their mediator-related symptoms are still completely suppressed. In vivo, midostaurin is metabolized to two major and active metabolites, namely CGP62221 and CGP52421. Whereas the in vitro effects of midostaurin on gro
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41

Singhal, Mitali, Jacobo Elies Gomez, Sanjit Nayak, Kirsten Riches Suman, and Amalia Ruiz Estrada. "Abstract 4386: Comparison of cytotoxicity of anthracycline based antineoplastic drugs in breast cancer." Cancer Research 83, no. 7_Supplement (2023): 4386. http://dx.doi.org/10.1158/1538-7445.am2023-4386.

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Abstract Mitoxantrone (MTX) is used for the chemotherapeutic treatment of breast cancer, but it has a dose-limiting cardiotoxicity. One of the mechanisms of MTX cytotoxicity is by inhibiting the topoisomerase II enzyme, which is crucial for maintaining cellular processes like replication. The aim of the study is to investigate if an alternative analog of MTX, named KP71 would be a suitable antineoplastic drug with reduced cardiovascular side effects. Cytotoxicity of both drugs in breast cancer cell lines MDA-MB-468, MDA-MB-231, MCF7, the non-neoplastic breast cell line MCF10, cardiac human fib
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42

Gleixner, Karoline V., Matthias Mayerhofer, Karl J. Aichberger, et al. "PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects." Blood 107, no. 2 (2006): 752–59. http://dx.doi.org/10.1182/blood-2005-07-3022.

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AbstractIn most patients with systemic mastocytosis (SM), including aggressive SM and mast cell leukemia (MCL), neoplastic cells express the oncogenic KIT mutation D816V. KIT D816V is associated with constitutive tyrosine kinase (TK) activity and thus represents an attractive drug target. However, imatinib and most other TK inhibitors fail to block the TK activity of KIT D816V. We show that the novel TK-targeting drugs PKC412 and AMN107 counteract TK activity of D816V KIT and inhibit the growth of Ba/F3 cells with doxycycline-inducible expression of KIT D816V as well as the growth of primary n
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43

Peter, Barbara, Harald Herrmann, Karoline V. Gleixner, et al. "The Aurora-Kinase Inhibitor R763/AS703569 Exerts Major Growth-Inhibitory and Apoptosis-Inducing Effects on Neoplastic Mast Cells." Blood 116, no. 21 (2010): 3972. http://dx.doi.org/10.1182/blood.v116.21.3972.3972.

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Abstract Abstract 3972 Systemic mastocytosis (SM) is a myeloid neoplasm defined by abnormal growth and accumulation of neoplastic mast cells (MC) in one or more internal organs. In most patients, the D816V-mutated variant of KIT is detectable. This mutant supposedly confers resistance against several tyrosine kinase inhibitors including imatinib and masitinib. In aggressive SM (ASM) or mast cell leukemia (MCL) the response to conventional drugs is poor and the prognosis is grave. In these patients, additional KIT-independent signalling pathways and molecules, such as BTK and LYN may play an im
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44

Tomescu, Aneta, Rodica Sîrbu, Stelian Paris, Emin Cadar, Cristina Luiza Erimia, and Cezar Laurentiu Tomescu. "Methotrexate Therapy in Obstetricaĺ Diseases." European Journal of Interdisciplinary Studies 2, no. 1 (2016): 9. http://dx.doi.org/10.26417/ejis.v2i1.p9-16.

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Our study is a rewiew of Methotrexate therapy in obstetrica? diseases such us: hydatidiform mole, and medical abortion. In the medical world, methotrexate is a citostatic drug used in neoplastic diseases. The clinical pharmacology data regarding methotrexate is presented, alongside route of administration and therapeutic effects in malignant disease, hydatiform mole, and medical abortion. The use of methotrexate in medical abortion and ectopic pregnancy is a great accomplishment, as it replaces a surgical intervention marred by characteristic side effects, with similar results.
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45

Tomescu, Aneta, Rodica Sîrbu, Stelian Paris, Emin Cadar, Cristina Luiza Erimia, and Cezar Laurentiu Tomescu. "Methotrexate Therapy in Obstetricaĺ Diseases." European Journal of Interdisciplinary Studies 4, no. 1 (2016): 9. http://dx.doi.org/10.26417/ejis.v4i1.p9-16.

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Our study is a rewiew of Methotrexate therapy in obstetrica? diseases such us: hydatidiform mole, and medical abortion. In the medical world, methotrexate is a citostatic drug used in neoplastic diseases. The clinical pharmacology data regarding methotrexate is presented, alongside route of administration and therapeutic effects in malignant disease, hydatiform mole, and medical abortion. The use of methotrexate in medical abortion and ectopic pregnancy is a great accomplishment, as it replaces a surgical intervention marred by characteristic side effects, with similar results.
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46

Oki, Yasuhiro, Jaroslav Jelinek, Hagop M. Kantarjian, and Jean-Pierre J. Issa. "Hypomethylation Induction and Molecular Response after Decitabine Therapy in Chronic Myelomonocytic Leukemia (CMML)." Blood 108, no. 11 (2006): 2322. http://dx.doi.org/10.1182/blood.v108.11.2322.2322.

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Abstract Decitabine has shown therapeutic activity in patients with MDS and CMML. The mechanisms of response to therapy remain incompletely understood. In particular, the relative contribution of this drug’s ability to induce hypomethylation and cytotoxicity remains unclear. To address this issue, we studied the dynamics of neoplastic cell clearance during decitabine treatment determined by quantitative monitoring of the mutant allele using pyrosequencing. DNA extracted from peripheral blood mononuclear cells from consented patients with CMML in a decitabine phase II study were first screened
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47

Greggs, Willie M., Christine L. Clouser, Steven E. Patterson, and Louis M. Mansky. "Discovery of drugs that possess activity against feline leukemia virus." Journal of General Virology 93, no. 4 (2012): 900–905. http://dx.doi.org/10.1099/vir.0.039909-0.

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Feline leukemia virus (FeLV) is a gammaretrovirus that is a significant cause of neoplastic-related disorders affecting cats worldwide. Treatment options for FeLV are limited, associated with serious side effects, and can be cost-prohibitive. The development of drugs used to treat a related retrovirus, human immunodeficiency virus type 1 (HIV-1), has been rapid, leading to the approval of five drug classes. Although structural differences affect the susceptibility of gammaretroviruses to anti-HIV drugs, the similarities in mechanism of replication suggest that some anti-HIV-1 drugs may also in
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48

Alomari, Safwan, Irma Zhang, Adrian Hernandez, et al. "Drug Repurposing for Glioblastoma and Current Advances in Drug Delivery—A Comprehensive Review of the Literature." Biomolecules 11, no. 12 (2021): 1870. http://dx.doi.org/10.3390/biom11121870.

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Glioblastoma (GBM) is the most common primary malignant brain tumor in adults with an extremely poor prognosis. There is a dire need to develop effective therapeutics to overcome the intrinsic and acquired resistance of GBM to current therapies. The process of developing novel anti-neoplastic drugs from bench to bedside can incur significant time and cost implications. Drug repurposing may help overcome that obstacle. A wide range of drugs that are already approved for clinical use for the treatment of other diseases have been found to target GBM-associated signaling pathways and are being rep
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49

Rozhkov, A. A., R. I. Nuriev, and M. I. Sekacheva. "Molecular diagnostics and targeted treatment approaches in pediatric oncology (literature review)." Medical alphabet, no. 38 (January 23, 2021): 29–33. http://dx.doi.org/10.33667/2078-5631-2020-38-29-33.

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The continuous evolution of new technologies in the field of molecular diagnostics and genome analysis, the development of new approaches in pharmacogenetics and the emergence of a range of different targeted drugs have expanded the possibilities of clinical practice, resulting in personalized approaches to treatment. The diagnosis and therapy of pediatric oncological diseases are some of the vivid examples of the successful application of a personalized approach in clinical practice. Today, many pediatric neoplastic diseases are successfully treated with targeted drugs, which significantly in
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50

Rocca, Carmine, Ernestina Marianna De Francesco, Teresa Pasqua, et al. "Mitochondrial Determinants of Anti-Cancer Drug-Induced Cardiotoxicity." Biomedicines 10, no. 3 (2022): 520. http://dx.doi.org/10.3390/biomedicines10030520.

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Mitochondria are key organelles for the maintenance of myocardial tissue homeostasis, playing a pivotal role in adenosine triphosphate (ATP) production, calcium signaling, redox homeostasis, and thermogenesis, as well as in the regulation of crucial pathways involved in cell survival. On this basis, it is not surprising that structural and functional impairments of mitochondria can lead to contractile dysfunction, and have been widely implicated in the onset of diverse cardiovascular diseases, including ischemic cardiomyopathy, heart failure, and stroke. Several studies support mitochondrial t
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