LCK expression is a potential biomarker for distinguishing primary central nervous system lymphoma from glioblastoma multiforme

Ge, Le; Xu, Lixia; Lu, Shan; Yan, Hua

doi:10.1002/2211-5463.12849

Cited by 4 publications

(5 citation statements)

References 22 publications

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“…LCK was expressed at a high level in primary central nervous system lymphoma patients but at a low level in GBM patients. However, LCK expression positively correlated with the levels of infiltrating B cells in diffuse large B-cell lymphoma and GBM [132].…”

Section: Lck Inhibitorsmentioning

confidence: 94%

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Small Molecule Tyrosine Kinase Inhibitors (TKIs) for Glioblastoma Treatment

Frumento,

Grossi,

Falesiedi

et al. 2024

IJMS

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In the last decade, many small molecules, usually characterized by heterocyclic scaffolds, have been designed and synthesized as tyrosine kinase inhibitors (TKIs). Among them, several compounds have been tested at preclinical and clinical levels to treat glioblastoma multiforme (GBM). GBM is the most common and aggressive type of cancer originating in the brain and has an unfavorable prognosis, with a median survival of 15–16 months and a 5-year survival rate of 5%. Despite recent advances in treating GBM, it represents an incurable disease associated with treatment resistance and high recurrence rates. For these reasons, there is an urgent need for the development of new pharmacological agents to fight this malignancy. In this review, we reported the compounds published in the last five years, which showed promising activity in GBM preclinical models acting as TKIs. We grouped the compounds based on the targeted kinase: first, we reported receptor TKIs and then, cytoplasmic and peculiar kinase inhibitors. For each small molecule, we included the chemical structure, and we schematized the interaction with the target for some representative compounds with the aim of elucidating the mechanism of action. Finally, we cited the most relevant clinical trials.

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Section: Lck Inhibitorsmentioning

confidence: 94%

“…It is involved in T-cell receptor signaling, also playing a crucial role in mediating B-cell receptor signaling in chronic lymphocytic leukemia cells. Furthermore, its expression was detected in several neural tissues, including hippocampus, cerebellum, and retina [132].…”

Section: Lck Inhibitorsmentioning

confidence: 99%

Small Molecule Tyrosine Kinase Inhibitors (TKIs) for Glioblastoma Treatment

Frumento,

Grossi,

Falesiedi

et al. 2024

IJMS

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“…The role of these proteins in tumor progression is not entirely understood. Nonetheless, most of these proteins have been implicated in the oncogenesis and developmental process of gliomas (Mills et al, 2011;Ge et al, 2020;Li et al, 2020;Moriconi et al, 2021).…”

Section: Cluster Analysismentioning

confidence: 99%

A Bayesian nonparametric approach to personalized treatment selection

Pedone¹,

Argiento²,

Stingo³

2022

Preprint

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Precision medicine is an approach for disease treatment that defines treatment strategies based on the individual characteristics of the patients. Motivated by an open problem in cancer genomics, we develop a novel model that flexibly clusters patients with similar predictive characteristics and similar treatment responses; this approach identifies, via predictive inference, which one among a set of therapeutic strategies is better suited for a new patient. The proposed method is fully model-based, avoiding uncertainty underestimation attained when treatment assignment is performed by adopting heuristic clustering procedures, and belongs to the class of product partition models with covariates, here extended to include the cohesion induced by the normalized generalized gamma process. The method performs particularly well in scenarios characterized by large heterogeneity of the predictive covariates, in simulation studies. A cancer genomics case study illustrates the potential benefits in terms of treatment response yielded by the proposed approach. Finally, being model-based, the approach allows estimating clusters' specific random effects and then identify patients that are more likely to benefit from personalized treatment.

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“…Other studies showed that Lck functions as a therapeutic target in acute myeloid leukaemia (AML) [53][54][55] . A recent study showed that Lck was expressed at a high level in primary central nervous system lymphoma (PCNSL) patients 56 . Lck expression was also detected in cholangiocarcinoma 57,58 , breast cancer 12,13,59,60 , colon cancer 14,15,61,62 , and lung carcinoma 16,62,63 .…”

Section: Lck-related Diseasesmentioning

confidence: 99%

New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and docking insights

Elkamhawy

Ali

Lee

2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Lymphocyte-specific protein tyrosine kinase (Lck), a non-receptor Src family kinase, has a vital role in various cellular processes such as cell cycle control, cell adhesion, motility, proliferation, and differentiation. Lck is reported as a key factor regulating the functions of T-cell including the initiation of TCR signalling, T-cell development, in addition to T-cell homeostasis. Alteration in expression and activity of Lck results in numerous disorders such as cancer, asthma, diabetes, rheumatoid arthritis, atherosclerosis, and neuronal diseases. Accordingly, Lck has emerged as a novel target against different diseases. Herein, we amass the research efforts in literature and pharmaceutical patents during the last decade to develop new Lck inhibitors. Additionally, structure-activity relationship studies (SAR) and docking models of these new inhibitors within the active site of Lck were demonstrated offering deep insights into their different binding modes in a step towards the identification of more potent, selective, and safe Lck inhibitors.

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LCK expression is a potential biomarker for distinguishing primary central nervous system lymphoma from glioblastoma multiforme

Cited by 4 publications

References 22 publications

Small Molecule Tyrosine Kinase Inhibitors (TKIs) for Glioblastoma Treatment

Small Molecule Tyrosine Kinase Inhibitors (TKIs) for Glioblastoma Treatment

A Bayesian nonparametric approach to personalized treatment selection

New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and docking insights

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