Induction of cytotoxicity and apoptosis in FLT3 mutant expressing cells using novel pyrimido cyanoacrylates and quinoline derivatives

ConclusionThe five novel heterocyclic compounds (E1QAC1-5) had cytotoxic effects and induced apoptosis in FD-FLT3 cells. Therefore, it is worthwhile to consider them as potential lead compound for development of new therapeutic agents for AML patients.
Source: Biomedicine and Pharmacotherapy - Category: Drugs & Pharmacology Source Type: research

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Adults diagnosed with acute myeloid leukemia have a poor prognosis, with only 30% surviving at five years. Despite advances in our understanding of the molecular underpinnings of AML, the chemotherapy backbone used to treat most patients (combination cytarabine and anthracycline) remains unchanged since 1973.With the goal of identifying a new differentiation therapy, we previously performed a small molecule phenotypic screen to find compounds that triggered myeloid maturation. Unexpectedly, our most active hits were inhibitors of the enzyme dihydroorotate dehydrogenase (DHODH). The DHODH-inhibitor brequinar demonstrated dr...
Source: Blood - Category: Hematology Authors: Tags: 616. Acute Myeloid Leukemia: Novel Therapy, excluding Transplantation: Poster II Source Type: research
IntroductionChemotherapy induced clonal selection and development are major contributors to disease relapse and resistance to therapy in AML. An immediate response to chemotherapy in intracellular signalling networks can be detected within minutes in vivo. (Irish J. et al 2004) We hypothesize that by analyzing the immediate intracellular chemotherapy response we might reveal which cancer clones are resistant to therapy and how they might be targeted. (Anensen N. et al Clin Cancer Res 2006), (Øyan M. et al BMC Cancer 2009)CyTOF combines the principles of conventional flow cytometry with time-of-flight mass spectromet...
Source: Blood - Category: Hematology Authors: Tags: 617. Acute Myeloid Leukemia: Biology, Cytogenetics, and Molecular Markers in Diagnosis and Prognosis: Poster I Source Type: research
Conclusion: Older patients with AML receiving intensive and non-intensive chemotherapy experience similar QOL impairments and high rates of psychological distress. These findings underscore the need to develop supportive care interventions for older patients with AML, regardless of their initial treatment strategy.DisclosuresBrunner: Takeda: Research Funding; Novartis: Research Funding; Celgene: Consultancy, Research Funding. Fathi: Celgene: Consultancy, Honoraria, Research Funding; Jazz: Honoraria; Boston Biomedical: Consultancy, Honoraria; Astellas: Honoraria; Agios: Honoraria, Research Funding; Seattle Genetics: Consult...
Source: Blood - Category: Hematology Authors: Tags: 904. Outcomes Research-Malignant Conditions: Poster I Source Type: research
ConclusionsIn our population based analysis, we show that although the OS of t-AML is significantly worse than primary AML, those t-AML diagnosed and treated in recent years (2006-2015) had significantly better survival compared to earlier treatment periods. Among all primaries, outcomes of t-AML particularly following lung cancers are dismal compared to other primaries.DisclosuresGerds: Celgene: Consultancy; Apexx Oncology: Consultancy; CTI Biopharma: Consultancy; Incyte: Consultancy. Nazha: MEI: Consultancy. Carraway: FibroGen: Consultancy; Jazz: Speakers Bureau; Balaxa: Membership on an entity's Board of Directors or ad...
Source: Blood - Category: Hematology Authors: Tags: 904. Outcomes Research-Malignant Conditions: Poster I Source Type: research
Introduction: Acute Myeloid Leukemia (AML) is an aggressive disease associated with poor health related quality of life (HRQoL) and short overall survival (OS), particularly for patients' ineligible for intensive chemotherapy. The HRQoL was evaluated in a cohort of patients with AML who were not considered eligible for standard chemotherapy based on the Functional Assessment of Cancer Therapy - Leukemia (FACT-Leu) collected at baseline of AML2002 study (NCT02472145).Methods: This analysis was based on a randomized, phase 2/3, parallel design study conducted in patients with AML. Patients' perceptions to HRQoL were evaluate...
Source: Blood - Category: Hematology Authors: Tags: 904. Outcomes Research-Malignant Conditions: Poster II Source Type: research
In this study we characterized mechanisms behind this niche-mediated chemoresistance.
Source: Experimental Hematology - Category: Hematology Authors: Source Type: research
AbstractResistance to apoptosis is one of the hallmarks of cancer and members of the B-cell lymphoma 2 (BCL-2) family of proteins are central regulators of apoptosis. Many cancers become resistant to chemotherapy and apoptosis by up-regulating BCL-2 and other family members, making these proteins attractive targets for cancer therapy. Venetoclax is an orally administered, small-molecule apoptosis stimulant that targets BCL-2 proteins by acting as a BCL-2 homology domain 3 (BH3) mimetic. The drug is approved in the USA and EU as a monotherapy for the for the treatment of certain patients with chronic lymphocytic leukemia (C...
Source: Targeted Oncology - Category: Cancer & Oncology Source Type: research
CONCLUSION Cognitive impairment can affect daily functioning, quality of life, and capacity to work in patients with cancer and those in remission. Consequently, cognitive assessment is now an important and necessary part of a comprehensive oncological care plan. Cancer-related cognitive impairment might be due to the direct effects of the cancer itself, nonspecific factors, or comorbid conditions that are independent of the disease and/or due to the adverse effects of the treatment or combination of treatments given for the disease. The prevalence and extent of cognitive impairment associated with cancer is recognized but...
Source: Innovations in Clinical Neuroscience - Category: Neuroscience Authors: Tags: Cognition Current Issue Neuro oncology Neurology Review cancer chemotherapy cognitive impairment neuropsychological assessment treatment Source Type: research
imann, Andreas Trumpp, Bernd Dörken, Johannes Zuber, Hinrich Gronemeyer, Michael Hummel, Gunnar Dittmar, Soyoung Lee &Clemens A. Schmitt Cellular senescence is a stress-responsive cell-cycle arrest program that terminates the further expansion of (pre-)malignant cells. Key signalling components of the senescence machinery, such as p16INK4a, p21CIP1 and p53, as well as trimethylation of lysine 9 at histone H3 (H3K9me3), also operate as critical regulators of stem-cell functions (which are collectively termed ‘stemness’). In cancer cells, a gain of stemness may have profound i...
Source: Nature - Category: Research Authors: Tags: Letter Source Type: research
AbstractImmunocompromised patients are at high risk of invasive fungal infections (IFI), in particular those with haematological malignancies undergoing remission-induction chemotherapy for acute myeloid leukaemia (AML) or myelodysplastic syndrome (MDS) and recipients of allogeneic haematopoietic stem cell transplants (HSCT). Despite the development of new treatment options in the past decades, IFI remains a concern due to substantial morbidity and mortality in these patient populations. In addition, the increasing use of new immune modulating drugs in cancer therapy has opened an entirely new spectrum of at risk periods. ...
Source: Annals of Hematology - Category: Hematology Source Type: research
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