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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Conclusion and Perspective With in-depth understandings of antibodies, linkers, and payloads, ADCs have also achieved great development. The linkage strategy and target diversity have already improved the delivery of the payloads to tumor tissues and reduced exposure to normal tissues. With the development of payloads, some novel potent payloads are used by ADCs, which allows researchers to exploit novel linkers to attach the antibody and payloads without disturbing their potency (Dragovich et al., 2018). Furthermore, some irrelevant antigen-target ADCs also may exert toxicity to tumor cells due to the vascular gap of tum...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
in N, Serrano I, Midwinter W, Wilk A, Bardaji A, Ingold N, Buchan R, Tayal U, Pascual-Figal DA, de Marvao A, Ahmad M, Garcia-Pinilla JM, Pantazis A, Dominguez F, Baksi AJ, O'Regan DP, Rosen SD, Prasad SK, Lara-Pezzi E, Provencio M, Lyon AR, Alonso-Pulpon L, Cook SA, DePalma SR, Barton PJR, Aplenc R, Seidman JG, Ky B, Ware JS, Seidman CE Abstract BACKGROUND: Cancer therapy-induced cardiomyopathy (CCM) is associated with cumulative drug exposures and pre-existing cardiovascular disorders. These parameters incompletely account for substantial inter-individual susceptibility to CCM. We hypothesized that rare variants ...
Source: Circulation - Category: Cardiology Authors: Tags: Circulation Source Type: research
Discussion Suppressor of cytokine signaling 1 is an essential molecule for maintaining immune homeostasis and subverting inflammation. Disorders arising from excess inflammation or SOCS1 deficiency can be potentially treated with SOCS1 mimetics (Ahmed et al., 2015). While SOCS1 has promising potential in many disorders, it should be noted that new targets and actions of SOCS1 are still being discovered and not all the effects of this protein are beneficial in autoimmune diseases and cancer. For instance, SOCS1 degrades IRS1 and IRS2, required for insulin signaling, via the SOCS Box domain, thus, limiting its potential in ...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
Personalized Dendritic Cell Vaccines—Recent Breakthroughs and Encouraging Clinical Results Beatris Mastelic-Gavillet, Klara Balint, Caroline Boudousquie, Philippe O. Gannon and Lana E. Kandalaft* Department of Oncology, Center for Experimental Therapeutics, Ludwig Center for Cancer Research, University of Lausanne, Lausanne, Switzerland With the advent of combined immunotherapies, personalized dendritic cell (DC)-based vaccination could integrate the current standard of care for the treatment of a large variety of tumors. Due to their proficiency at antigen presentation, DC are key coordinators of the innate...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
In conclusion, MPT0G413 and BTZ synergistically inhibit MM viability, providing a framework for the clinical evaluation of combined therapies for MM. Introduction Multiple myeloma (MM) is a B cell malignancy characterized by the proliferation of bone marrow (BM) plasma cells and the production of large amounts of abnormal immunoglobulins (1) In the United States, it was estimated that 30,770 new MM cases would be diagnosed in 2018, accounting for 1.8% of newly diagnosed cancer cases (2). Furthermore, 12,770 MM-related deaths in 2018 accounted for an estimated 2.1% of all cancer deaths (2). In the past decade, MM t...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research
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
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