Targeting mitochondrial bioenergetics by combination treatment with imatinib and dichloroacetate in human erythroleukemic K ‑562 and colorectal HCT‑116 cancer cells
Int J Oncol. 2024 Apr;64(4):42. doi: 10.3892/ijo.2024.5630. Epub 2024 Mar 1.ABSTRACTTumor malignant cells are characterized by dysregulation of mitochondrial bioenergetics due to the 'Warburg effect'. In the present study, this metabolic imbalance was explored as a potential target for novel cancer chemotherapy. Imatinib (IM) downregulates the expression levels of SCΟ2 and FRATAXIN (FXN) genes involved in the heme‑dependent cytochrome c oxidase biosynthesis and assembly pathway in human erythroleukemic IM‑sensitive K‑562 chronic myeloid leukemia cells (K‑562). In the present study, it was investigated whether the ...
Source: International Journal of Oncology - March 1, 2024 Category: Cancer & Oncology Authors: Maria G Kakafika Areti A Lyta George I Gavriilidis Stefanos A Tsiftsoglou Androulla N Miliotou Ioannis S Pappas Ioannis S Vizirianakis Lefkothea C Papadopoulou Asterios S Tsiftsoglou Source Type: research
GSE221906 Concomitant inhibition of the thioredoxin system and non-homologous DNA repair potently sensitizes Philadelphia-positive lymphoid leukemia to tyrosine kinase inhibitors
Contributors : Lukasz Komorowski ; Joanna Madzio ; Agata Pastorczak ; Kacper Szczygie ł ; Martyna Poprzeczko ; Klaudyna Fidyt ; Maksymilian Bielecki ; Jaromir Hunia ; Agnieszka Dabkowska ; Tomasz Stoklosa ; Magdalena Winiarska ; Elzbieta Patkowska ; Jakub Golab ; Malgorzata FirczukSeries Type : Expression profiling by high throughput sequencingOrganism : Homo sapiensBCR-ABL1 gene fusion is an essential driver lesion in both chronic myeloid leukemia (CML) and Philadelphia-positive (Ph+) B-cell acute lymphoblastic leukemia (B-ALL). While tyrosine kinase inhibitors (TKIs) cure up to 95% of CML patients, 50 % of...
Source: GEO: Gene Expression Omnibus - March 1, 2024 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research
Imatinib/nilotinib
(Source: Reactions Weekly)
Source: Reactions Weekly - March 1, 2024 Category: Drugs & Pharmacology Source Type: research
Imatinib treatment improves hyperglycaemic dysregulation in severe COVID-19: a secondary analysis of blood biomarkers in a randomised controlled trial
SARS-CoV-2 can induce insulin resistance, which is, among others, mediated by adipose tissue dysfunction and reduced angiotensin-converting enzyme 2 (ACE2) enzymatic activity. In SARS-CoV-2-infected mice, the ... (Source: Critical Care)
Source: Critical Care - February 29, 2024 Category: Intensive Care Authors: Erik Duijvelaar, Xiaoke Pan, Harm Jan Bogaard, Etto C. Eringa and Jurjan Aman Tags: Brief Report Source Type: research
Advanced gastrointestinal stromal tumor: reliable classification of imatinib plasma trough concentration via machine learning
Patients with advanced gastrointestinal stromal tumors (GISTs) exhibiting an imatinib plasma trough concentration (IM Cmin) under 1100 ng/ml may show a reduced drug response rate, leading to the suggestion of mon... (Source: BMC Cancer)
Source: BMC Cancer - February 24, 2024 Category: Cancer & Oncology Authors: Pan Ran, Tao Tan, Jinjin Li, Hao Yang, Juan Li and Jun Zhang Tags: Research Source Type: research
Navigating the Management of Chronic Phase CML in the Era of Generic BCR::ABL1 Tyrosine Kinase Inhibitors
J Natl Compr Canc Netw. 2024 Feb;22(1):e237116. doi: 10.6004/jnccn.2023.7116.ABSTRACTOver the past several years, advances in research, treatment, and market dynamics have impacted treatment strategies in chronic myeloid leukemia in chronic phase (CML-CP). They include the broader availability of cost-effective generic imatinib, and soon other generic second-generation tyrosine kinase inhibitors (TKIs). Access to affordable generics means that all patients with CML-CP should have access to safe and highly effective lifelong therapies. When overall survival is the treatment endpoint, imatinib provides a good treatment value...
Source: Journal of the National Comprehensive Cancer Network : JNCCN - February 23, 2024 Category: Cancer & Oncology Authors: Fadi G Haddad Hagop Kantarjian Source Type: research
Investigation of the mechanism of USP28-mediated IFITM3 elevation in BCR-ABL-dependent imatinib resistance in CML
Biomed Pharmacother. 2024 Feb 22;173:116315. doi: 10.1016/j.biopha.2024.116315. Online ahead of print.ABSTRACTDue to resistance and BCR-ABLT315I-mutated, CML remains a clinical challenge. It needs new potential therapeutic targets to overcome CML resistance related to BCR-ABL. Our research revealed that the deubiquitinating enzyme USP28 was highly expressed in BCR-ABL-dependent CML patients. Similarly, a high expression of USP28 was found in the K562 cell line, particularly in the imatinib-resistant strains. Notably, USP28 directly interacted with BCR-ABL. Furthermore, when BCR-ABL and its mutant BCR-ABLT315I were overexpr...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - February 23, 2024 Category: Drugs & Pharmacology Authors: Zilin Li Yiling Xi Linglan Tu Xu Zhang Yue Huang Huizong Nie Cheng Peng Haohuan Chai Shenxin Zeng Xiaoliang Zheng Liyan Cheng Source Type: research
Pharmacovigilance study of BCR-ABL1 tyrosine kinase inhibitors: a safety analysis of the FDA adverse event reporting system
CONCLUSIONS: The results of this study demonstrated that AE signals differ among the five BCR-ABL1 TKIs. Furthermore, each BCR-ABL1 TKI displayed several new signals. These findings provide valuable information for clinicians aiming to reduce the risk of AEs during BCR-ABL1 TKI treatment.PMID:38395895 | PMC:PMC10885429 | DOI:10.1186/s40360-024-00741-x (Source: BMC Pharmacology and Toxicology)
Source: BMC Pharmacology and Toxicology - February 23, 2024 Category: Drugs & Pharmacology Authors: Dehua Zhao Xiaoqing Long Jisheng Wang Source Type: research
Navigating the Management of Chronic Phase CML in the Era of Generic BCR::ABL1 Tyrosine Kinase Inhibitors
J Natl Compr Canc Netw. 2024 Feb;22(1):e237116. doi: 10.6004/jnccn.2023.7116.ABSTRACTOver the past several years, advances in research, treatment, and market dynamics have impacted treatment strategies in chronic myeloid leukemia in chronic phase (CML-CP). They include the broader availability of cost-effective generic imatinib, and soon other generic second-generation tyrosine kinase inhibitors (TKIs). Access to affordable generics means that all patients with CML-CP should have access to safe and highly effective lifelong therapies. When overall survival is the treatment endpoint, imatinib provides a good treatment value...
Source: Journal of the National Comprehensive Cancer Network : JNCCN - February 23, 2024 Category: Cancer & Oncology Authors: Fadi G Haddad Hagop Kantarjian Source Type: research
Pharmacovigilance study of BCR-ABL1 tyrosine kinase inhibitors: a safety analysis of the FDA adverse event reporting system
CONCLUSIONS: The results of this study demonstrated that AE signals differ among the five BCR-ABL1 TKIs. Furthermore, each BCR-ABL1 TKI displayed several new signals. These findings provide valuable information for clinicians aiming to reduce the risk of AEs during BCR-ABL1 TKI treatment.PMID:38395895 | PMC:PMC10885429 | DOI:10.1186/s40360-024-00741-x (Source: BMC Pharmacology and Toxicology)
Source: BMC Pharmacology and Toxicology - February 23, 2024 Category: Drugs & Pharmacology Authors: Dehua Zhao Xiaoqing Long Jisheng Wang Source Type: research
Navigating the Management of Chronic Phase CML in the Era of Generic BCR::ABL1 Tyrosine Kinase Inhibitors
J Natl Compr Canc Netw. 2024 Feb;22(1):e237116. doi: 10.6004/jnccn.2023.7116.ABSTRACTOver the past several years, advances in research, treatment, and market dynamics have impacted treatment strategies in chronic myeloid leukemia in chronic phase (CML-CP). They include the broader availability of cost-effective generic imatinib, and soon other generic second-generation tyrosine kinase inhibitors (TKIs). Access to affordable generics means that all patients with CML-CP should have access to safe and highly effective lifelong therapies. When overall survival is the treatment endpoint, imatinib provides a good treatment value...
Source: Journal of the National Comprehensive Cancer Network : JNCCN - February 23, 2024 Category: Cancer & Oncology Authors: Fadi G Haddad Hagop Kantarjian Source Type: research
Pharmacovigilance study of BCR-ABL1 tyrosine kinase inhibitors: a safety analysis of the FDA adverse event reporting system
CONCLUSIONS: The results of this study demonstrated that AE signals differ among the five BCR-ABL1 TKIs. Furthermore, each BCR-ABL1 TKI displayed several new signals. These findings provide valuable information for clinicians aiming to reduce the risk of AEs during BCR-ABL1 TKI treatment.PMID:38395895 | PMC:PMC10885429 | DOI:10.1186/s40360-024-00741-x (Source: BMC Pharmacology and Toxicology)
Source: BMC Pharmacology and Toxicology - February 23, 2024 Category: Drugs & Pharmacology Authors: Dehua Zhao Xiaoqing Long Jisheng Wang Source Type: research
Tyrosine kinase inhibitor resistance in de novo BCR::ABL1-positive BCP-ALL beyond kinase domain mutations
Blood Adv. 2024 Feb 22:bloodadvances.2023012162. doi: 10.1182/bloodadvances.2023012162. Online ahead of print.ABSTRACTA better understanding of ABL1-kinase domain mutation-independent causes of tyrosine kinase inhibitor (TKI) resistance is needed for BCR::ABL1-positive B-cell precursor acute lymphoblastic leukemia (BCP-ALL). While TKIs have dramatically improved outcomes, a subset of patients still experiences relapsed or refractory disease. We aimed to identify potential biomarkers for intrinsic TKI resistance at diagnosis in 32 pediatric and 19 adult BCR::ABL1-positive BCP-ALL samples. Reduced ex vivo imatinib sensitivit...
Source: Adv Data - February 22, 2024 Category: Epidemiology Authors: Inge van Outersterp Judith M Boer Cesca Van De Ven Caitlin Ej Reichert Aur élie Boeree Brian Kruisinga Hester A de Groot-Kruseman Gabriele Escherich Aniko Sijs-Szabo Anita W Rijneveld Monique L den Boer Source Type: research
Multi-target rational design and synthesis of novel diphenyl-tethered pyrazolopyrimidines targeting EGFR and topoisomerase II with potential DNA intercalation and apoptosis induction
Bioorg Chem. 2024 Feb 17;145:107223. doi: 10.1016/j.bioorg.2024.107223. Online ahead of print.ABSTRACTHerein, we envisioned the design and synthesis of novel pyrazolopyrimidines (confirmed by elemental analysis, 1H and 13C NMR, and mass spectra) as multitarget-directed drug candidates acting as EGFR/TOPO II inhibitors, DNA intercalators, and apoptosis inducers. The target diphenyl-tethered pyrazolopyrimidines were synthesized starting from the reaction of phenyl hydrazine and ethoxymethylenemalononitrile to give aminopyrazole-carbonitrile 2. The latter hydrolysis with NaOH and subsequent reaction with 4-chlorobenzaldhyde a...
Source: Bioorganic Chemistry - February 22, 2024 Category: Chemistry Authors: Ahmed A Gaber Ayman Abo Elmaaty Marwa Sharaky Aliaa A Mosa Abdullah Yahya Abdullah Alzahrani Saad Shaaban Wagdy M Eldehna Ahmed A Al-Karmalawy Source Type: research
