Kris, Mark G. (2003). "Efficacy of Gefitinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in ... Articles with short description, Short description matches Wikidata, Tyrosine kinase inhibitors, Receptor antagonists, Growth ... "A specific inhibitor of the epidermal growth factor receptor tyrosine kinase". Science. 265 (5175): 1093-1095. doi:10.1126/ ... HER2 inhibitors at the Drugs.com website. VEGF/VEGFR inhibitors at the Drugs.com website. Cancer growth blockers at the Cancer ...
... is a class of inhibitors[jargon] that targets the Src kinase family of tyrosine kinase, which is transcribed by ... kinase inhibitor) are both inhibitors of Lck and FynT. Dasatinib Rivera-Torres J, José ES (2019). "Src Tyrosine Kinase ... Apr 2013). "A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic ... Because of the crucial position of the Src kinase in cells, Src inhibitors are potential antineoplastic agents for e.g. ...
"Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3". Nature. 445 (7126): 437-41. Bibcode: ... ErbB3 is a member of the epidermal growth factor receptor (EGFR/ERBB) family of receptor tyrosine kinases. The kinase-impaired ... Receptor tyrosine-protein kinase erbB-3, also known as HER3 (human epidermal growth factor receptor 3), is a membrane bound ... Roskoski R (2014). "The ErbB/HER family of protein-tyrosine kinases and cancer". Pharmacol. Res. 79: 34-74. doi:10.1016/j.phrs. ...
Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug ... It is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits ... "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (3): 179 ... This treatment must be the sole tyrosine kinase inhibitor subsidised for this condition. Pazopanib has also demonstrated ...
... is a kinase inhibitor which inhibits Janus kinase 3 and tyrosine kinase. Ritlecitinib was approved for medical use ... Non-receptor tyrosine kinase inhibitors, Pyrrolopyrimidines, Carboxamides, Piperidines, Pfizer brands, All stub articles, ...
Approved drugs that inhibit BTK: Ibrutinib (Imbruvica), a selective Bruton's tyrosine kinase inhibitor. Acalabrutinib ( ... Bruton's tyrosine kinase (abbreviated Btk or BTK), also known as tyrosine-protein kinase BTK, is a tyrosine kinase that is ... a Brain-penetrant Bruton s Tyrosine Kinase Inhibitor, for the Modulation of Chronically Inflamed White Matter Lesions in ... "Bruton's tyrosine kinase (Btk) associates with protein kinase C mu". FEBS Letters. 461 (1-2): 68-72. doi:10.1016/S0014-5793(99) ...
It is a small molecule inhibitor of multiple tyrosine kinases. Sitravatinib is being developed by Mirati Therapeutics. Ongoing ... a tyrosine kinase inhibitor". Cancer Communications. 40 (7): 285-300. doi:10.1002/cac2.12040. PMC 7365458. PMID 32525624. " ... and certain patients who are naïve to checkpoint inhibitor therapy. Yang Y, Ji N, Cai CY, Wang JQ, Lei ZN, Teng QX, Wu ZX, Cui ... including in a combination trial with nivolumab in those who are resistant to checkpoint inhibitor therapy, ...
... these regions are targeted in therapies to downregulate BCR-ABL1 kinase activity. Tyrosine kinase inhibitors specific to such ... a tyrosine kinase, and the BCR-ABL1 transcript is also translated into a tyrosine kinase containing domains from both the BCR ... Leoni V, Biondi A (2015). "Tyrosine kinase inhibitors in BCR-ABL positive acute lymphoblastic leukemia". Haematologica. 100 (3 ... "The Tyrosine Kinase c-Abl Responds to DNA Damage by Activating the Homeodomain-interacting Protein Kinase 2". Journal of ...
Roskoski R (September 2014). "ErbB/HER protein-tyrosine kinases: Structures and small molecule inhibitors". Pharmacological ...
"Selectivity Profile of the Tyrosine Kinase 2 Inhibitor Deucravacitinib Compared with Janus Kinase 1/2/3 Inhibitors". ... It is a tyrosine kinase 2 (TYK2) inhibitor and it is taken by mouth. It was developed by Bristol Myers Squibb. Deucravacitinib ... It acts as a highly selective allosteric inhibitor of non-receptor tyrosine-protein kinase 2 (TYK2). The chemical structure of ... Non-receptor tyrosine kinase inhibitors, Triazoles, Cyclopropyl compounds, Pyridazines, Methoxy compounds, Carboxamides, All ...
It is an inhibitor of the kinases fms-like tyrosine kinase 3 (FLT3), Janus kinase 2 (JAK2), tropomyosin receptor kinase (trk) A ... Non-receptor tyrosine kinase inhibitors, Receptor tyrosine kinase inhibitors). ... Janus kinase inhibitor Shabbir M, Stuart R (2010). "Lestaurtinib, a multitargeted tyrosinse kinase inhibitor: from bench to ... Lestaurtinib was identified early on as a trk receptor tyrosine kinase (RTK) inhibitor, with a concentration inhibiting 50% of ...
It acts as an inhibitor of FLT3, hence it is a tyrosine kinase inhibitor. It was developed by Astellas Pharma. In April 2018, ... Tyrosine kinase inhibitors, Orphan drugs, Astellas Pharma, All stub articles, Antineoplastic and immunomodulating drug stubs). ... January 2017). "Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor". Blood. 129 (2): 257-260. doi:10.1182/ ...
Angiogenesis inhibitors, Tyrosine kinase inhibitors, Experimental cancer drugs). ... April 2000). "PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, ... the clinical development of a tyrosine kinase inhibitor of angiogenesis in solid tumours". Expert Opin Investig Drugs. 16 (3): ... Vatalanib (INN, codenamed PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis. It is ...
February 2017). "High-throughput screening of tyrosine kinase inhibitor cardiotoxicity with human induced pluripotent stem ... "High-throughput screening of tyrosine kinase inhibitor cardiotoxicity with human induced pluripotent stem cells". Science ... ALK5 inhibitor SB431412 and MEK (mitogen-activated protein kinase) inhibitor PD0325901 - which was found to increase the ... August 2011). "Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell- ...
... against a wide spectrum of protein tyrosine kinases. Levitzki demonstrated (1993) that such an inhibitor of Bcr-Abl kinase ... "Effects of the Tyrosine Kinase Inhibitor AG957 and an Anti-Fas Receptor Antibody on CD34+ Chronic Myelogenous Leukemia ... "pioneering signal transduction therapy and for developing tyrosine kinase inhibitors as effective agents against cancer and a ... Synthesis and biological activity of protein tyrosine kinase inhibitors". Journal of Medicinal Chemistry. 32 (10): 2344-2352. ...
Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug ... It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). Erlotinib was approved ... As with other ATP competitive small molecule tyrosine kinase inhibitors, such as imatinib in CML, patients rapidly develop ... 2012). "Comparison of the efficacy and safety of EFGR tyrosine kinase inhibitor monotherapy with standard second-line ...
These include tyrosine kinase inhibitors (TKIs), monoclonal antibodies, and proteasome inhibitors. Immunotherapy is a type of ...
Scott IC, Scott DL (2014). "Spleen tyrosine kinase inhibitors for rheumatoid arthritis: where are we now?". Drugs. 74 (4): 415- ... Tyrosine-protein kinase SYK, also known as spleen tyrosine kinase, is an enzyme which in humans is encoded by the SYK gene. SYK ... SYK Spleen tyrosine kinase". Chan AC, Iwashima M, Turck CW, Weiss A (November 1992). "ZAP-70: a 70 kd protein-tyrosine kinase ... along with ZAP70, is a member of the Syk family of tyrosine kinases. These cytoplasmic non-receptor tyrosine kinases share a ...
... discovery of dual inhibitors of tyrosine and phosphoinositide kinases". Nature Chemical Biology. 4 (11): 691-699. doi:10.1038/ ... the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases and ...
The developed tyrosine kinase inhibitor, imatinib mesylate, has had a tremendous effect on stopping cancer progression in the ... Sorafenib is a kinase inhibitor used as a treatment for kidney and liver cancer. The kinase inhibitor blocks serine-threonine ... The most novel research is being done in tyrosine kinase inhibitors; however M2 acute myeloid leukemia treatment research ... BCR-Abl is constitutively active due chromosome translocation; therefore it over-phosphorylates the tyrosine kinase. Imatinib ...
It is a small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment ... Sunitinib blocks the tyrosine kinase activities of KIT, PDGFR, VEGFR2 and other tyrosine kinases involved in the development of ... This concept led to the invention of many small-molecule tyrosine kinase inhibitors, including Gleevec, Sutent, Tarceva and ... "Phase II study of SU11248, a multi-targeted tyrosine kinase inhibitor in patients with previously treated metastatic breast ...
Since tyrosine kinase inhibitors (TKIs) are metabolized in the liver, interaction of TKIs with OATP1B1 and OATP1B3 can be ... Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug ... "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabolism and Drug Interactions. ... Annaert P, Ye ZW, Stieger B, Augustijns P (March 2010). "Interaction of HIV protease inhibitors with OATP1B1, 1B3, and 2B1" ( ...
For inoperable tumors, treatment with tyrosine kinase inhibitors may be attempted. In general, the prospect of cure is best in ... for which surgical removal is not possible or only incompletely possible can also be treated with tyrosine kinase inhibitors. ... tyrosine kinase KIT) regulates mast cell differentiation, proliferation, activation and lifespan via stem cell factor binding. ...
Gotink, Kristy J.; Verheul, Henk M. W. (2010-03-01). "Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of ... Various angiogenesis inhibitors have been developed to interfere with different steps in the process. Bevacizumab (Avastin) is ... Sorafenib and sutinib are additional angiogenesis inhibitors that bind and block receptors on endothelial cells that have ... Cook, Kristina M.; Figg, William D. (2010-07-01). "Angiogenesis inhibitors: current strategies and future prospects". CA: A ...
Angiogenesis inhibitors, Receptor tyrosine kinase inhibitors, Quinazolines, Amines, Bromoarenes, Fluoroarenes, Phenol ethers, ... an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases". Cancer Research. 62 ( ... and RET tyrosine kinases. RET tyrosine kinases; it weakly inhibits VEGFR-3. Vandetanib is well absorbed from the gut, reaches ... Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug ...
... potassium leak channels by the tyrosine kinase inhibitor genistein". British Journal of Pharmacology. 154 (8): 1680-90. doi: ...
September 2018). "Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1". ... positive chronic myeloid leukemia in chronic phase who have previously been treated with two or more tyrosine kinase inhibitors ... Non-receptor tyrosine kinase inhibitors, Novartis brands, Orphan drugs, Pyrrolidines, Pyridines, Pyrazoles, Carboxamides, ... Asciminib is a protein kinase inhibitor. The most common adverse reactions include upper respiratory tract infections, ...
Bruon's tyrosine kinase inhibitor, ibrutinib, to block the B-cell maturating actions of this kianase; 4) BCL inhibitor ... Bruton's tyrosine kinase inhibitor produced overall and complete response rates of 38% and 18%, respectively; the Bcl inhibitor ... Phosphoinositide 3-kinase inhibitors such as copanlisib, duvelisib, and idelalisib which block the phosphoinositide 3-kinase ... Phosphoionsitide 3-kinase inhibitors produced overall response rates of 10-12.5 months in 42-59%; tisagenlecleuce cells ...
Nikolinakos P, Heymach JV (June 2008). "The tyrosine kinase inhibitor cediranib for non-small cell lung cancer and other ... Receptor tyrosine kinase inhibitors, Indole ethers at the benzene ring, Quinazolines, AstraZeneca brands, Fluoroarenes, ... an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with cisplatin and gemcitabine in patients ... vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer". Cancer Research. 65 (10 ...
"Targeting abnormal DNA double-strand break repair in tyrosine kinase inhibitor-resistant chronic myeloid leukemias". Oncogene. ... "Interactions of the DNA ligase IV-XRCC4 complex with DNA ends and the DNA-dependent protein kinase". Journal of Biological ... "Rational design of human DNA ligase inhibitors that target cellular DNA replication and repair". Cancer Res. 68 (9): 3169-77. ...