Results 41 to 50 of about 1,603 (142)

Nickel pyrithione induces apoptosis in chronic myeloid leukemia cells resistant to imatinib via both Bcr/Abl-dependent and Bcr/Abl-independent mechanisms

open access: yesJournal of Hematology & Oncology, 2016
Background Acquired imatinib (IM) resistance is frequently characterized by Bcr-Abl mutations that affect IM binding and kinase inhibition in patients with chronic myelogenous leukemia (CML).
Xiaoying Lan   +13 more
doaj   +1 more source

Targeting BCR-ABL+ stem/progenitor cells and BCR-ABL-T315I mutant cells by effective inhibition of the BCR-ABL-Tyr177-GRB2 complex

open access: yesOncotarget, 2017
Treatment of BCR-ABL+ human leukemia has been significantly improved by ABL tyrosine kinase inhibitors (TKIs), but they are not curative for most patients and relapses are frequently associated with BCR-ABL mutations, warranting new targets for improved treatments.
Chen, Min   +5 more
openaire   +3 more sources

Oncogenic KRAS Rewires Stress Granule Dynamics: Mechanisms and Therapeutic Opportunities

open access: yesThe Kaohsiung Journal of Medical Sciences, EarlyView.
ABSTRACT Stress granules (SGs) are dynamic, membrane‐less structures that form in response to various cellular stresses, including metabolic, oxidative, and therapeutic challenges. They function as adaptive hubs and reorganize protein synthesis and signaling networks to help cells survive under stress. In cancer, these condensates are often hijacked to
Msimisi Ndzinisa   +2 more
wiley   +1 more source

Ponatinib is a pan-BCR-ABL kinase inhibitor: MD simulations and SIE study. [PDF]

open access: yesPLoS ONE, 2013
BCR-ABL kinase domain inhibition can be used to treat chronic myeloid leukemia. The inhibitors such as imatinib, dasatinib and nilotinib are effective drugs but are resistant to some BCR-ABL mutations.
Karunakar Tanneeru, Lalitha Guruprasad
doaj   +1 more source

Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms

open access: yesMedicinal Research Reviews, EarlyView.
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino   +3 more
wiley   +1 more source

The FABD domain is critical for the oncogenicity of BCR/ABL in chronic myeloid leukaemia

open access: yesCell Communication and Signaling
Background Abnormally expressed BCR/ABL protein serves as the basis for the development of chronic myeloid leukaemia (CML). The F-actin binding domain (FABD), which is a crucial region of the BCR/ABL fusion protein, is also located at the carboxyl end of
Renren Zheng   +8 more
doaj   +1 more source

Update on Non‐Biological and RNA‐Based Therapeutics in Chronic Inflammatory Diseases: Precision Medicine Through Small Molecules: An EAACI Position Paper

open access: yesAllergy, EarlyView.
ABSTRACT In the last decades, critical advancements in research technology and knowledge on disease mechanisms steered therapeutic approaches for chronic inflammatory diseases towards unprecedented target specificity. For allergic and chronic lung diseases, biologic drugs pioneered this goal, acquiring on the way—through the clinical use of monoclonal ...
F. Roth‐Walter   +20 more
wiley   +1 more source

Mixed-Lineage Leukemia

open access: yesIndonesian Journal of Cancer, 2022
Introduction: Acute Leukemia with Mixed Lineage phenotype (MLL) is leukemia that consists of cells characterized by mixed lineage markers, both from myeloid and lymphoid cells.
Suci Iriani   +3 more
doaj   +1 more source

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren   +8 more
wiley   +1 more source

New Inhibitors of Bcr-Abl Based on 2,6,9-Trisubstituted Purine Scaffold Elicit Cytotoxicity in Chronic Myeloid Leukemia-Derived Cell Lines Sensitive and Resistant to TKIs

open access: yesPharmaceutics
Bcr-Abl is an oncoprotein with aberrant tyrosine kinase activity involved in the progression of chronic myeloid leukemia (CML) and has been targeted by inhibitors such as imatinib and nilotinib.
Thalia Delgado   +12 more
doaj   +1 more source

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