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https://www.readbyqxmd.com/read/29788766/design-synthesis-and-3d-qsar-based-pharmacophore-study-of-novel-imatinib-analogs-as-antitumor-apoptotic-agents
#1
Iten M Fawzy, Khairia M Youssef, Deena S Lasheen, Nasser Sm Ismail, Khaled Am Abouzid
AIM: Imatinib possesses various mechanisms for combating cancer, making the development of imatinib analogs an attractive target for cancer research. METHOD: Two series of analogs were designed and synthesized, maintaining the essential pharmacophoric features in imatinib structure. The synthesized compounds were subjected to cell-based antiproliferative assays against nonsmall lung (A549) and colon cancer cell lines. In addition, flow cytometry cell cycle and caspase-3 colorimetric assays were performed...
May 23, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29786668/scf-c-kit-signaling-increased-mucin2-production-by-maintaining-atoh1-expression-in-mucinous-colorectal-adenocarcinoma
#2
Ping Shen, Shu Yang, Haimei Sun, Guilan Li, Bo Wu, Fengqing Ji, Tingyi Sun, Deshan Zhou
Mucinous colorectal adenocarcinoma (MCA) patients often a show high risk of malignant potential and a poorer survival rate. Given that the pathological feature and oncobiological characteristics of MCA are correlated with its abundant extracellular mucin2 (MUC2), we paid interest toward investigating the key factor that promotes MUC2 production exposure to highly-activated stem cell factor (SCF)/c-KIT signaling, which we believed to contribute to MCA formation. Long-term azoxymethane and dextran sodium sulfate treatment successfully induced MCA only in wild-type (WT) mice at week 37 and 43, while all c-kit loss-of-function mutant mice (Wadsm/m ) developed non-MCA...
May 22, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29780937/vogt-koyanagi-harada-disease-like-presentation-in-patients-with-chronic-myeloid-leukemia
#3
Saurabh Mistry, S Sudharshan, Suganeswari Ganesan, Ashraf Banu Akbar, Jyotirmay Biswas
Purpose: To report two rare cases of chronic myeloid leukemia (CML) on tyrosine kinase inhibitors presenting as bilateral serous retinal detachment and ocular inflammation, simulating Vogt-Koyanagi-Harada (VKH) disease. Methods: Case series and review of literature. Result: Two young patients (one male and one female) with CML on treatment with tyrosine kinase inhibitors (imatinib and dasatanib) under remission presented with bilateral sudden vision loss...
June 2018: American Journal of Ophthalmology Case Reports
https://www.readbyqxmd.com/read/29780651/fatal-outcome-of-imatinib-in-a-patient-with-idiopathic-hypereosinophilic-syndrome
#4
Ashraf Abugroun, Ahmed Chaudhary, Gabriel Rodriguez
Cytokine storm is a poorly explained clinical entity caused by an undesired and aggrandized immune system response leading to unregulated activation of the proinflammatory cascade, often contributing to multisystem organ failure and even death. Its potentially diverse etiologies and sepsis-like presentation have made it even more challenging to diagnose, and so far, no well-established treatment protocol has been proposed. Its association with certain medications, especially with monoclonal antibodies, has well been reported in literature...
2018: Case Reports in Oncological Medicine
https://www.readbyqxmd.com/read/29777794/regulatory-t-cell-targeted-hybrid-nanoparticles-combined-with-immuno-checkpoint-blockage-for-cancer-immunotherapy
#5
Wenquan Ou, Raj Kumar Thapa, Liyuan Jiang, Soe Zar Chi, Milan Gautam, Jae-Hoon Chang, Jee-Heon Jeong, Sae Kwang Ku, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Immunosuppression in tumor microenvironments induced by regulatory T (Treg) cells is regarded a critical mechanism of tumor immune escape and poses a major impediment to cancer immunotherapy. In this study, we developed tLyp1 peptide-conjugated hybrid nanoparticles for targeting Treg cells in the tumor microenvironment. The tLyp1 peptide-modified hybrid nanoparticles presented good stability and effective targeting to Treg cells, and they enhanced the effect of imatinib in downregulating Treg cell suppression through inhibition of STAT3 and STAT5 phosphorylation...
May 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29774130/targeting-invadopodia-mediated-breast-cancer-metastasis-by-using-abl-kinase-inhibitors
#6
Tomer Meirson, Alessandro Genna, Nikola Lukic, Tetiana Makhnii, Joel Alter, Ved P Sharma, Yarong Wang, Abraham O Samson, John S Condeelis, Hava Gil-Henn
Metastatic dissemination of cancer cells from the primary tumor and their spread to distant sites in the body is the leading cause of mortality in breast cancer patients. While researchers have identified treatments that shrink or slow metastatic tumors, no treatment that permanently eradicates metastasis exists at present. Here, we show that the ABL kinase inhibitors imatinib, nilotinib, and GNF-5 impede invadopodium precursor formation and cortactin-phosphorylation dependent invadopodium maturation, leading to decreased actin polymerization in invadopodia, reduced extracellular matrix degradation, and impaired matrix proteolysis-dependent invasion...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29773593/safety-and-efficacy-of-second-line-bosutinib-for-chronic-phase-chronic-myeloid-leukemia-over-a-five-year-period-final-results-of-a-phase-1-2-study
#7
Carlo Gambacorti-Passerini, Jorge E Cortes, Jeff H Lipton, Hagop M Kantarjian, Dong-Wook Kim, Philippe Schafhausen, Rocco Crescenzo, Nathalie Bardy-Bouxin, Mark Shapiro, Kay Noonan, Eric Leip, Liza DeAnnuntis, Tim H Brümmendorf, H Jean Khoury
Bosutinib is a Src/Abl tyrosine kinase inhibitor indicated for adults with newly-diagnosed Ph+ chronic myeloid leukemia or with resistant/intolerant disease. We report the final results of a phase 1/2 study of second-line bosutinib in chronic phase chronic myeloid leukemia patients after imatinib failure (n=284). Median follow-up and treatment durations were 54.8 (range, 0.6-96.3) and 25.6 (0.2&-96.3) months, respectively. At years 2 and 5, 54% and 40% of patients, respectively, remained on bosutinib. Cumulative major cytogenetic response and complete cytogenetic response rates (newly-attained or maintained from baseline) were 58% and 46%, respectively, by year 2 and 60% and 50% by year 5...
May 17, 2018: Haematologica
https://www.readbyqxmd.com/read/29770723/the-impact-of-azole-antifungal-drugs-on-imatinib-metabolism-in-human-liver-microsomes
#8
Xingxian Luo, Taifeng Li, Ze Yu, Xuecai Xue, Haiyang Zhao, Na Li, Liping Ma, Changqing Yang, Lin Huanglin, Wangyu Feng
1. Imatinib is widely used for the treatment of hematologic malignancies. It is common that imatinib is clinically co-prescribed with azole antifungal agents since these patients are more prone to invasive antifungal infection. The present study was to investigate the effects of azole antifungal drugs, including ketoconazole, fluconazole, voriconazole, itraconazole and posaconazole on imatinib metabolism. 2. The main metabolites, 1-OH midazolam and N-desmethyl imatinib, were determined in the absence and in the presence of various levels of ketoconazole, fluconazole, voriconazole, itraconazole and posaconazole...
May 17, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29766411/gastrointestinal-stromal-tumors-risk-of-recurrence-stratification-by-tumor-volume-is-a-best-predictor-compared-with-risk-based-on-mitosis-and-tumor-size
#9
Leonardo S Lino-Silva, Patricia Segales-Rojas, Eduardo Aguilar-Cruz, Rosa A Salcedo-Hernández, César Zepeda-Najar
PURPOSE: Gastrointestinal stromal tumors (GIST) have the potential to recur and metastasize. Several prognostic schemes have been developed, mostly based on the mitotic count, diameter, and tumor site. However, these systems are not precise enough. The research question was whether the tumor size determined by volumetry allows a better risk stratification than the traditional system, and our aim was to determine the value of tumor volumetry, a feasible and simple parameter, in the recurrence of GIST...
May 16, 2018: Journal of Gastrointestinal Cancer
https://www.readbyqxmd.com/read/29764854/preclinical-antitumor-activity-of-a-novel-anti-c-kit-antibody-drug-conjugate-against-mutant-and-wild-type-c-kit-positive-solid-tumors
#10
Tinya J Abrams, Anu Connor, Christie P Fanton, Steven B Cohen, Thomas Huber, Kathy Miller, E Erica Hong, Xiaohong Niu, Janine Kline, Marjorie Ison-Dugenny, Sarah Harris, Dana B Walker, Klaus R Krauser, Francesco Galimi, Zhen Wang, Majid Ghoddusi, Keith G Mansfield, Si Tuen Lee-Hoeflich, Jocelyn Holash, Nancy Pryer, William Kluwe, Seth A Ettenberg, William R Sellers, Emma Lees, Paul Kwon, Judith A Abraham, Siew Schleyer
PURPOSE: c-KIT overexpression is well-recognized in cancers such as GIST, SCLC, melanoma, NSCLC and AML. Treatment with the small molecule inhibitors imatinib, sunitinib and regorafenib result in resistance (c-KIT mutant tumors) or limited activity (c-KIT wildtype tumors). We selected an anti-c-KIT ADC approach to evaluate the anti-cancer activity in multiple disease models. EXPERIMENTAL DESIGN: A humanized anti-c-KIT antibody LMJ729 was conjugated to the microtubule destabilizing maytansinoid, DM1, via a non-cleavable linker (SMCC)...
May 15, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29760836/concomitant-atm-mutations-identified-by-next-generation-sequencing-in-a-patient-with-new-onset-acute-myeloid-leukemia-following-imatinib-treatment-for-chronic-myeloid-leukemia
#11
Matthew K Stein, Melissa Crawley, Eric Vick, Mike G Martin
No abstract text is available yet for this article.
April 2018: World Journal of Oncology
https://www.readbyqxmd.com/read/29760553/a-favorable-outcome-of-advanced-dermatofibrosarcoma-protuberans-under-treatment-with-sunitinib-after-imatinib-failure
#12
Wei Xiao, Yi Que, Ruiqing Peng, Ya Ding, Jingjing Zhao, Xizhi Wen, Desheng Weng, Xiaoshi Zhang, Yuanxiang Guan, Xing Zhang
While traditional cytotoxic agents play a limited role in advanced dermatofibrosarcoma protuberans (DFSP), the treatment of sunitinib for patients with advanced DFSP after imatinib failure is not well defined. The objective of this case report was to analyze the relationship between molecular mechanisms and clinical outcomes of sunitinib treatment in patients with advanced DFSP after imatinib failure. In this case report, a 37-year-old man suffered from advanced DFSP progression after surgical operation, microwave ablation, and chemotherapy...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29760538/gastrointestinal-stromal-tumors-a-multidisciplinary-challenge
#13
REVIEW
Juan Manuel Sanchez-Hidalgo, Manuel Duran-Martinez, Rafael Molero-Payan, Sebastian Rufian-Peña, Alvaro Arjona-Sanchez, Angela Casado-Adam, Antonio Cosano-Alvarez, Javier Briceño-Delgado
Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal tumors located in the alimentary tract. Its usual manifestation is gastrointestinal bleeding. However, small asymptomatic lesions are frequently detected as incidental finding. Characteristically, most GISTs (> 95%) are positive for the KIT protein (CD117) by IHC staining and approximately 80%-90% of GISTs carry a mutation in the c-KIT or PDGFRA genes. Mutational analysis should be performed when planning adjuvant and neoadjuvant therapy, due to its possible resistance to conventional treatment...
May 14, 2018: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29755776/gastrointestinal-stromal-tumors-in-the-imatinib-era-15-years-experience-of-a-tertiary-center
#14
Armando Peixoto, Pedro Costa-Moreira, Marco Silva, Ana Luísa Santos, Susana Lopes, Filipe Vilas-Boas, Pedro Moutinho-Ribeiro, Guilherme Macedo
Gastrointestinal stromal tumors (GISTs) were associated with a disease free survival rate of disease of 50% at 5 years, but the actual natural history since the advent of imatinib is poorly described. Our objective was to evaluate the evolution in the treatment and prognosis of patients with GISTs since the start of imatinib. Retrospective analysis of GISTs diagnosed between January 2000 and June 2015 in a Portuguese large volume center. We included 131 patients, 55% female, with a mean age of 64±14 years, followed for a median of 30 months; 64% of cases had gastric involvement; 92% of the tumors were c-Kit positive; 95% of patients were operated...
April 2018: Journal of Gastrointestinal Oncology
https://www.readbyqxmd.com/read/29755704/breastfeeding-in-patients-with-chronic-myeloid-leukaemia-case-series-with-measurements-of-drug-concentrations-in-maternal-milk-and-literature-review
#15
Ekaterina Chelysheva, Sergey Aleshin, Evgenia Polushkina, Roman Shmakov, Igor Shokhin, Ghermes Chilov, Anna Turkina
Breastfeeding in patients with chronic myeloid leukaemia (CML) during tyrosine kinase inhibitors (TKIs) therapy is not recommended but interruption of TKI treatment may cause the loss of remission. We studied the 3 cases of pregnancy and breastfeeding in women with CML and observed that stopping treatment without major molecular response may end in haematological relapse. The concentrations of nilotinib and imatinib in maternal milk were measured and nilotinib distribution in human breast milk was demonstrated for the first time...
2018: Mediterranean Journal of Hematology and Infectious Diseases
https://www.readbyqxmd.com/read/29752602/clinicopathological-features-and-prognosis-of-primary-gists-with-tumor-rupture-in-the-real-world
#16
Toshirou Nishida, Haruhiko Cho, Seiichi Hirota, Toru Masuzawa, Gaku Chiguchi, Toshimasa Tsujinaka
BACKGROUND: Patients with ruptured gastrointestinal stromal tumor (GIST) are recommended for imatinib adjuvant therapy; however, their clinicopathological features and prognosis in the era of imatinib are unknown. PATIENTS AND METHODS: The study cohort included 665 patients with histologically proven primary GISTs who underwent R0 or R1 surgery between 2003 and 2007; the validation cohort included 182 patients between 2000 and 2014. The definitions of tumor rupture in the study included perforation at tumor site, tumor fracture, piecemeal resection including open biopsy, and macroscopic injuries to the pseudocapsule...
May 11, 2018: Annals of Surgical Oncology
https://www.readbyqxmd.com/read/29749314/glycolysis-inhibition-as-a-strategy-for-hepatocellular-carcinoma-treatment
#17
Andreia Alves, Ana Catarina Mamede, Marco Alves, Pedro F Oliveira, Sandra Moreira Rocha, Filomena Botelho, Claudio Jorge Maia
Hepatocellular carcinoma (HCC) is the most frequently detected primary malignant liver tumor, representing a worldwide public health problem due to its high morbidity and mortality rates. The HCC is commonly detected in advanced stage, precluding the use of treatments with curative intent. For this reason, it is crucial to find effective therapies for HCC. Cancer cells have a high dependence of glycolysis for ATP production, especially under hypoxic environment. Such dependence provides a reliable possible strategy to specifically target cancer cells based on the inhibition of glycolysis...
April 30, 2018: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/29745093/imatinib-therapy-after-resection-of-high-risk-gastrointestinal-stromal-tumors-in-chinese-patients-a-median-follow-up-of-48-months
#18
Cheng Lei, Bing Zhao, Qisan Wang, Lei Ge, Haijiang Wang
PURPOSE: Adjuvant imatinib can be given for gastrointestinal stromal tumors (GISTs), but adequate risk stratification is necessary to select patients who will benefit from this therapy. We aimed to investigate the treatment methods and prognostic factors of high risk GISTs. METHODS: This retrospective study included 108 patients who underwent tumor resection for high-risk GISTs between January 2003 and February 2017. The patients were divided into two groups: a group of patients received postoperative imatinib adjuvant therapy (Adjuvant therapy group), and the other group was not treated with imatinib until they were found to have disease progression (Followup observation group)...
March 2018: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29742077/philadelphia-chromosome-positive-acute-lymphoblastic-leukemia-in-adults-current-treatments-and-future-perspectives
#19
Musa Yilmaz, Hagop Kantarjian, Farhad Ravandi-Kashani, Nicholas J Short, Elias Jabbour
Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL) accounts for approximately one-fourth of cases of adult ALL. It typically presents with an aggressive clinical course, responds poorly to standard chemotherapy, and carries a high risk for relapse. The landscape of Ph+ ALL therapy has changed favorably since the development of tyrosine kinase inhibitors (TKIs). With the successful incorporation of TKIs into chemotherapy regimens, remissions occur more frequently and patients live longer...
March 2018: Clinical Advances in Hematology & Oncology: H&O
https://www.readbyqxmd.com/read/29741440/bosutinib-dasatinib-imatinib-nilotinib-and-ponatinib-differentially-affect-the-vascular-molecular-pathways-and-functionality-of-human-endothelial-cells
#20
Ayala Gover-Proaktor, Galit Granot, Metsada Pasmanik-Chor, Oren Pasvolsky, Saar Shapira, Oshrat Raz, Pia Raanani, Avi Leader
The tyrosine kinase inhibitors (TKIs), nilotinib, ponatinib, and dasatinib (but not bosutinib or imatinib), are associated with vascular adverse events (VAEs) in chronic myeloid leukemia (CML). Though the mechanism is inadequately understood, an effect on vascular cells has been suggested. We investigated the effect of imatinib, nilotinib, dasatinib, bosutinib, and ponatinib on tube formation, cell viability, and gene expression of human vascular endothelial cells (HUVECs). We found a distinct genetic profile in HUVECs treated with dasatinib, ponatinib, and nilotinib compared to bosutinib and imatinib, who resembled untreated samples...
May 9, 2018: Leukemia & Lymphoma
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