Nilotinib exhibits less toxicity than imatinib and influences the immune state by modulating iNOS, p-p38 and p-JNK in LPS/IFN gamma-activated macrophages
In conclusion, our results reveal that, in addition to its anticancer activity, nilotinib can exhibit immune modulatory effects on macrophages through its effects on iNOS, IL-6, p-p38 and p-JNK.PMID:38061604 | DOI:10.1016/j.tiv.2023.105754 (Source: Toxicology in Vitro)
Source: Toxicology in Vitro - December 7, 2023 Category: Toxicology Authors: Arzu Zeynep Karabay Tulin Ozkan Asli Koc Yalda Hekmatshoar A Selen Gurkan-Alp Asuman Sunguroglu Source Type: research
A novel L-shaped ortho-quinone analog as PLK1 inhibitor blocks prostate cancer cells in G < sub > 2 < /sub > phase
Biochem Pharmacol. 2023 Dec 2:115960. doi: 10.1016/j.bcp.2023.115960. Online ahead of print.ABSTRACTProstate cancer is the most common malignant tumor among men worldwide. Currently, the main treatments are radical prostatectomy, radiotherapy, chemotherapy, and endocrine therapy. However, most of them are poorly effective and induce side effects. Polo-like kinase 1 (PLK1) regulates cell cycle and mitosis. Its inhibitor BI2536 promotes the therapeutic effect of nilotinib in chronic myeloid leukemia, enhances the sensitivity of neural tube cell tumors to radiation therapy and PLK1 silencing enhances the sensitivity of squamo...
Source: Biochemical Pharmacology - December 4, 2023 Category: Drugs & Pharmacology Authors: Shaowei Zhang Jia Yu Xin Tan Sha Cheng Hanfei Liu Zhiyao Li Shinan Wei Weidong Pan Heng Luo Source Type: research
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease
Bioorg Med Chem. 2023 Nov 10;96:117532. doi: 10.1016/j.bmc.2023.117532. Online ahead of print.ABSTRACTAbelson tyrosine kinase (c-Abl) is involved in various biological processes in neurodegenerative diseases and is an attractive target for anti-PD (Parkinson's disease) drug discovery. Based on our previous work, we designed several novel c-Abl inhibitors through a conformational constrained strategy and evaluated their pharmacological activities. Among them, compound A6 exhibited superior inhibitory activity against c-Abl than nilotinib in the homogenous time-resolved fluorescence (HTRF) assay. Furthermore, A6 displayed hi...
Source: Bioorganic and Medicinal Chemistry - November 25, 2023 Category: Chemistry Authors: Zichao Yang Yangcheng Ai Guowu Wu Fengqiu Guo Zilong Yang Beijun Cheng Lishun Zhang Mingxia Li Jianjun Chen Jiajie Zhang Tingting Zhang Source Type: research
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease
Bioorg Med Chem. 2023 Nov 10;96:117532. doi: 10.1016/j.bmc.2023.117532. Online ahead of print.ABSTRACTAbelson tyrosine kinase (c-Abl) is involved in various biological processes in neurodegenerative diseases and is an attractive target for anti-PD (Parkinson's disease) drug discovery. Based on our previous work, we designed several novel c-Abl inhibitors through a conformational constrained strategy and evaluated their pharmacological activities. Among them, compound A6 exhibited superior inhibitory activity against c-Abl than nilotinib in the homogenous time-resolved fluorescence (HTRF) assay. Furthermore, A6 displayed hi...
Source: Bioorganic and Medicinal Chemistry - November 25, 2023 Category: Chemistry Authors: Zichao Yang Yangcheng Ai Guowu Wu Fengqiu Guo Zilong Yang Beijun Cheng Lishun Zhang Mingxia Li Jianjun Chen Jiajie Zhang Tingting Zhang Source Type: research
Moyamoya disease presenting with symptomatic ischemic stroke during new-generation tyrosine kinase inhibitor treatment: two illustrative cases
AbstractTyrosine kinase inhibitors (TKIs) have been widely used to treat chronic myeloid leukemia. Nilotinib and ponatinib, which are second- and third-generation TKIs, have been reported to cause cerebrovascular arterial complications. Here, we present two cases of moyamoya disease presenting with symptomatic ischemic stroke during new-generation TKI treatment. We judged that new-generation TKI treatment was a factor in symptomatic ischemic stroke of unknown moyamoya disease in both cases. Noninvasive examinations using magnetic resonance imaging or carotid ultrasonography should be performed before and during new-generat...
Source: Acta Neurochirurgica - November 6, 2023 Category: Neurosurgery Source Type: research
Nilotinib treatment induces cognitive impairment by elevating hippocampal oxidative stress in rats
CONCLUSIONS: Nilotinib treatment produced significant impairment of cognitive function by inducing oxidative stress in the hippocampal tissue of rats.PMID:37916379 | DOI:10.26355/eurrev_202310_34189 (Source: European Review for Medical and Pharmacological Sciences)
Source: European Review for Medical and Pharmacological Sciences - November 2, 2023 Category: Drugs & Pharmacology Authors: S H Alharbi A H Alhowail M A Aldubayan S K Alenezi M J Anwar Source Type: research
Nilotinib treatment induces cognitive impairment by elevating hippocampal oxidative stress in rats
CONCLUSIONS: Nilotinib treatment produced significant impairment of cognitive function by inducing oxidative stress in the hippocampal tissue of rats.PMID:37916379 | DOI:10.26355/eurrev_202310_34189 (Source: Pharmacological Reviews)
Source: Pharmacological Reviews - November 2, 2023 Category: Drugs & Pharmacology Authors: S H Alharbi A H Alhowail M A Aldubayan S K Alenezi M J Anwar Source Type: research
Nilotinib treatment induces cognitive impairment by elevating hippocampal oxidative stress in rats
CONCLUSIONS: Nilotinib treatment produced significant impairment of cognitive function by inducing oxidative stress in the hippocampal tissue of rats.PMID:37916379 | DOI:10.26355/eurrev_202310_34189 (Source: European Review for Medical and Pharmacological Sciences)
Source: European Review for Medical and Pharmacological Sciences - November 2, 2023 Category: Drugs & Pharmacology Authors: S H Alharbi A H Alhowail M A Aldubayan S K Alenezi M J Anwar Source Type: research
