Inhibition of discoidin domain receptor (DDR)-1 with nilotinib alters CSF miRNAs and is associated with reduced inflammation and vascular fibrosis in Alzheimer ’s disease
Discoidin Domain Receptor (DDR)-1 is activated by collagen. Nilotinib is a tyrosine kinase inhibitor that is FDA-approved for leukemia and potently inhibits DDR-1. Individuals diagnosed with mild –moderate Alzh... (Source: Journal of Neuroinflammation)
Source: Journal of Neuroinflammation - May 16, 2023 Category: Neurology Authors: Max Stevenson, Rency Varghese, Michaeline L. Hebron, Xiaoguang Liu, Nick Ratliff, Amelia Smith, R. Scott Turner and Charbel Moussa Tags: Research Source Type: research
Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation
Eur J Med Chem. 2023 Apr 21;255:115385. doi: 10.1016/j.ejmech.2023.115385. Online ahead of print.ABSTRACTStructure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as the P2 ligands in combination with darunavir-like hydroxyethylamine sulfonamide isosteres. These heterocyclic ligands are inherent to kinase inhibitor drugs, such as nilotinib and imatinib. These ligands are designed to make hydrogen bonding interactions with the backbone...
Source: European Journal of Medicinal Chemistry - May 7, 2023 Category: Chemistry Authors: Arun K Ghosh Jennifer L Mishevich Satish Kovela Ryan Shaktah Ajay K Ghosh Megan Johnson Yuan-Fang Wang Andres Wong-Sam Johnson Agniswamy Masayuki Amano Yuki Takamatsu Shin-Ichiro Hattori Irene T Weber Hiroaki Mitsuya Source Type: research
Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation
Eur J Med Chem. 2023 Apr 21;255:115385. doi: 10.1016/j.ejmech.2023.115385. Online ahead of print.ABSTRACTStructure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as the P2 ligands in combination with darunavir-like hydroxyethylamine sulfonamide isosteres. These heterocyclic ligands are inherent to kinase inhibitor drugs, such as nilotinib and imatinib. These ligands are designed to make hydrogen bonding interactions with the backbone...
Source: European Journal of Medicinal Chemistry - May 7, 2023 Category: Chemistry Authors: Arun K Ghosh Jennifer L Mishevich Satish Kovela Ryan Shaktah Ajay K Ghosh Megan Johnson Yuan-Fang Wang Andres Wong-Sam Johnson Agniswamy Masayuki Amano Yuki Takamatsu Shin-Ichiro Hattori Irene T Weber Hiroaki Mitsuya Source Type: research
Nilotinib cause moyamoya disease in the treatment of chronic myelogenous leukemia in chronic phase: A case report
Asian J Surg. 2023 May 1:S1015-9584(23)00521-3. doi: 10.1016/j.asjsur.2023.04.020. Online ahead of print.NO ABSTRACTPMID:37137777 | DOI:10.1016/j.asjsur.2023.04.020 (Source: Asian Journal of Surgery)
Source: Asian Journal of Surgery - May 3, 2023 Category: Surgery Authors: Jin-Ping Liang Rui-Hua Mi Lin Chen Xu-Dong Wei Source Type: research
CNS demyelination associated with nilotinib
(Source: Neurological Sciences)
Source: Neurological Sciences - May 3, 2023 Category: Neurology Source Type: research
Clinical management of second-generation tyrosine kinase inhibitor therapy in patients with newly diagnosed chronic myeloid leukemia in the chronic phase, focusing on age and dose effects
In this study, we retrospectively analyzed 178 patients with newly diagnosed CML-CP who were treated with dasatinib or nilotinib, focusing on age and dose effects. Efficacy as measured by cumulative major molecular response (MMR) and molecular response 4.5 rates did not differ significantly between the younger group and elderly group. Elderly patients who started nilotinib at a reduced dose had similar or better efficacy outcomes (including cumulative MMR and continuation ratios) than other groups, and elderly patients who started dasatinib at a reduced dose had the lowest MMR ratio and longest MMR duration. Effects of dos...
Source: International Journal of Hematology - May 2, 2023 Category: Hematology Authors: Michihide Tokuhira Yuta Kimura Takayuki Tabayashi Naoki Watanabe Shun Tsuchiya Tomoiku Takaku Noriyoshi Iriyama Eriko Sato Tomonori Nakazato Toru Mitsumori Maho Ishikawa Hiroyuki Fujita Masahiro Kizaki Miki Ando Yoshihiro Hatta Eisaku Iwanaga Tatsuya Kawa Source Type: research
Imatinib/nilotinib
(Source: Reactions Weekly)
Source: Reactions Weekly - May 1, 2023 Category: Drugs & Pharmacology Source Type: research
Expansions of tumor-reactive Vdelta1 gamma-delta T cells in newly diagnosed patients with chronic myeloid leukemia
AbstractRecent studies have underscored the importance of gamma-delta ( γδ) T cells in mediating potent MHC-unrestricted cytotoxicity in numerous malignancies. Here, we analyzed Vδ1 and Vδ2 γδ T cell subsets in newly diagnosed chronic myeloid leukemia (CML) patients (n = 40) who had initiated tyrosine kinase inhibitor (TKI) therapy including imatinib (n = 22), nilotinib (n = 14) and dasatinib (n = 4). Patient peripheral blood samples were analyzed at diagnosis and monitored prospectively at 3, 6, 12 and 18 months post-TKI. γδ T cells isolated from healthy donors and CML patients were used against K...
Source: Cancer Immunology, Immunotherapy - April 18, 2023 Category: Cancer & Oncology Source Type: research
Tyrosine Kinase Inhibitor-associated Cerebral Arterial Occlusive Disease Treated with High-flow Bypass Surgery: A Case Report
NMC Case Rep J. 2023 Mar 24;10:61-66. doi: 10.2176/jns-nmc.2022-0298. eCollection 2023.ABSTRACTNilotinib, one of the tyrosine kinase inhibitors, has been used to treat chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Nilotinib-associated cerebral arterial occlusive disease, which is treated with medicine with/without bypass surgery or stenting, has been sporadically reported to occur. The mechanism of the nilotinib-associated cerebral disease has not been clarified and is still controversial. Here we present the case of a 39-year-old woman with Ph+ ALL treated with...
Source: Atherosclerosis - April 17, 2023 Category: Cardiology Authors: Yurie Rai Takayuki Hara Source Type: research
Tyrosine Kinase Inhibitor-associated Cerebral Arterial Occlusive Disease Treated with High-flow Bypass Surgery: A Case Report
NMC Case Rep J. 2023 Mar 24;10:61-66. doi: 10.2176/jns-nmc.2022-0298. eCollection 2023.ABSTRACTNilotinib, one of the tyrosine kinase inhibitors, has been used to treat chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Nilotinib-associated cerebral arterial occlusive disease, which is treated with medicine with/without bypass surgery or stenting, has been sporadically reported to occur. The mechanism of the nilotinib-associated cerebral disease has not been clarified and is still controversial. Here we present the case of a 39-year-old woman with Ph+ ALL treated with...
Source: Atherosclerosis - April 17, 2023 Category: Cardiology Authors: Yurie Rai Takayuki Hara Source Type: research
