Protein kinase inhibitors, Johnson & Johnson brands, Pyrazoles, Quinoxalines). ... Saxty, Gordon (3 November 2011). "Pyrazolyl quinazoline kinase inhibitors". Google Patents. Bahleda R, Italiano A, Hierro C, ... It is a small molecule inhibitor of fibroblast growth factor receptor (FGFR) used for the treatment of cancer. FGFRs are a ... Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients with Advanced or Refractory Solid Tumors". Clin. Cancer Res. ...
CYP2D6 inhibitors, CYP3A4 inducers, Protein kinase inhibitors, Alkaloids, Lactams, Indolocarbazoles). ... Midostaurin, sold under the brand name Rydapt & Tauritmo both by Novartis, is a multi-targeted protein kinase inhibitor that ... June 2002). "Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412". ... December 2015). The multi-kinase inhibitor midostaurin (M) prolongs survival compared with placebo (P) in combination with ...
Protein kinase inhibitors, Quaternary ammonium compounds, Withdrawn drugs, Zwitterions). ... Nov 2003). "Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation". Molecular Cancer Therapeutics. Mol ... Perifosine interrupts the PI3K/AKT/mTOR pathway by acting as an allosteric AKT inhibitor targeting the pleckstrin homology ... "Aeterna Zentaris Regains North American Rights to Akt Inhibitor from Keryx". May 2012. "Aeterna Zentaris: Phase 3 Data for ...
Owens' laboratory found that activity of UGT enzymes can be lessened by kinase inhibitors and that protein kinase C and ... Her lab showed that one of these genes, UGT1A1, processes the protein bilirubin, which is a breakdown product of hemoglobin. ... tyrosine kinase enzymes can alter the enzyme specificity, likely contributing to their ability to detoxify a wide range of ...
Protein kinase inhibitors, All stub articles, Antineoplastic and immunomodulating drug stubs). ... Decernotinib is an inhibitor of Janus kinase 3 (JAK3) discovered through a process of inhouse screening of a chemical compound ... September 2015). "Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of ...
Clinical trials of protein kinase inhibitors, which block the abnormal kinase proteins involved in the development and growth ... lead to the expression of a mutated receptor tyrosine kinase protein, termed RET (REarranged during Transfection). RET is ... Cabozantinib which is a potent inhibitor of RET, MET and VEGF was evaluated in a double-blind placebo controlled trial. It was ...
Although originally thought to be a p38 mitogen-activated protein kinase (MAPK) inhibitor, it has since been reported that it ... Protein kinase inhibitors, Tert-butyl compounds, Clinical trials sponsored by Eli Lilly and Company). ... March 2016). "A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients ... January 2020). "A randomized, double-blind, placebo-controlled phase 1b/2 study of ralimetinib, a p38 MAPK inhibitor, plus ...
... protein kinase inhibitors that block the effects of the COL1A1-PDGFB fusion gene) may be added to the treatment regimen in ... nestin protein in 95% of cases, and S100 protein and melanocyte protein PMEL protein in some cases. DFSP-FS tumors have a DFSP- ... intrinsic tyrosine kinase activity and thereby to overstimulate mitogen-activated protein kinases, PI3K/AKT/mTOR, and other ... In 45% of cases, CD34 protein is absent or greatly reduced in DFSP-FS tumor cells compared to DFSP tumor cells. Like DFSP tumor ...
It is a selective rho-associated coiled-coil-containing protein kinase 1 (ROCK1) inhibitor, where ROCK1 is "an important ... Sharma R (2016-08-04). "ayurajan: Ripasudil , Kinase Inhibitor , ROCK Inhibitor , Treatment of Glaucoma , Treatment of Ocular ... Isobe T, Mizuno K, Kaneko Y, Ohta M, Koide T, Tanabe S (August 2014). "Effects of K-115, a rho-kinase inhibitor, on aqueous ... Ripasudil (trade name Glanatec), a derivative of fasudil, is a rho kinase inhibitor drug (previously known as K-115) used for ...
Non-receptor tyrosine kinase inhibitors, Protein kinase inhibitors, Aminopyrimidines, All stub articles, Antineoplastic and ... It is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. ... The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM). "Ojjaara- momelotinib tablet ... It is a Janus kinase inhibitor and it is taken by mouth. The most common adverse reactions include dizziness, fatigue, ...
... acetic acid derivatives as protein kinase inhibitors. Surugatoxin has not been demonstrated to be effective in either of these ...
July 1998). "Identification of a novel inhibitor of mitogen-activated protein kinase kinase". The Journal of Biological ... "Mitogen-activated protein/extracellular signal-regulated kinase kinase (MEK) inhibitors restore anoikis sensitivity in human ... "Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy". ... U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was found to functionally ...
Protein kinase inhibitors). ... "Definition of AXL inhibitor BGB324". NCI Drug Dictionary. ... Bemcentinib, also known as BGB324 or R428, is an experimental oral small molecule that is an inhibitor of AXL kinase. ... Bemcentinib targets and binds to the intracellular catalytic kinase domain of AXL receptor tyrosine kinase and inhibits its ... Davidsen KT, Haaland GS, Lie MK, Lorens JB, Engelsen AS (2017). "The role of Axl receptor tyrosine kinase in tumor cell ...
Protein kinase inhibitors, Succinimides, All stub articles, Antineoplastic and immunomodulating drug stubs). ... It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase in vitro. (MET is a growth factor receptor.) ... Tivantinib is being tested clinically as a highly selective MET inhibitor. However, the mechanism of action of tivantinib is ...
Protein kinase inhibitors, Experimental drugs, Isopropyl compounds). ... Doree M, Galas S (1994). "The cyclin-dependent protein kinases and the control of cell division". FASEB J. 8 (14): 1114-1121. ... Seciclib causes egg activation by inhibiting protein kinases which results in the inactivation of the maturation promoting ... Schang LM, Rosenberg A, Schaffer PA (2000). "Roscovitine, a specific inhibitor of cellular cyclin-dependent kinases, inhibits ...
Protein kinase inhibitors, All stub articles, Heterocyclic compound stubs). ... Y-27632 is a biochemical tool used in the study of the rho-associated protein kinase (ROCK) signaling pathways. Y-27632 ... 1997). "Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension". Nature. 389 (6654 ... "Rho-Associated Kinase Inhibitor (Y-27632) Attenuates Doxorubicin-Induced Apoptosis of Human Cardiac Stem Cells". PLOS ONE. 10 ( ...
Protein kinase inhibitors, Astellas Pharma, Cyclobutanes, Imidazopyrazines, Antineoplastic drugs, All stub articles, ... It is an inhibitor of the insulin receptor and of the insulin-like growth factor 1 receptor (IGF-1R). This prevents tumor cell ... a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor". Future Medicinal Chemistry. 1 (6 ...
Protein kinase inhibitors). ... 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, ... "Combining the receptor tyrosine kinase inhibitor AEE788 and the mammalian target of rapamycin (mTOR) inhibitor RAD001 strongly ... a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor ... Meco D, Servidei T, Zannoni GF, Martinelli E, Prisco MG, de Waure C, Riccardi R (Oct 2010). "Dual Inhibitor AEE788 Reduces ...
Protein kinase inhibitors, Experimental cancer drugs, Cyclobutanes, Amines, Nitrogen heterocycles, Heterocyclic compounds with ... It acts as an allosteric AKT inhibitor. It is a highly selective inhibitor of pan-Akt, namely, of all three Akt isoforms Akt1, ... December 2011). "First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors". ... MK-2206 dihydrochloride (CAS 1032350-13-2) inc structure diagram MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor ...
Protein kinase inhibitors, Aminopyrimidines, Trifluoromethyl compounds, Dimethylamino compounds). ... December 2005). "NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib- ... Santos FP, Kantarjian H, Cortes J, Quintas-Cardama A (December 2010). "Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor ... Imatinib was the first Bcr-Abl tyrosine-kinase inhibitor and was highly successful in treatment of chronic myelogenous leukemia ...
Protein kinase inhibitors, Breakthrough therapy, Specialty drugs, Pfizer brands, Cyclopentanes, Lactams). ... It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Palbociclib was the first CDK4/6 inhibitor to be ... It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. In the G1 phase of the cell cycle, mammalian cells ... 2009). "PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen ...
Protein kinase inhibitors, Pyridines, Respiratory chemical irritants). ... "Cyclin-Dependent Kinase (CDK)4/6 Inhibitor Abemaciclib for Neurofibromatosis Type I (NF1) Related Atypical Neurofibromas". www. ... It was developed by Eli Lilly and it acts as a CDK inhibitor selective for CDK4 and CDK6. It was designated as a breakthrough ... This result suggests that there may be a mechanism of action other than inhibition of a cyclin-dependent kinase. After oral ...
Protein kinase inhibitors). ... kinase inhibitor for the treatment of cancer. It was discovered ... a Potent Inhibitor of Cyclin Dependent Kinases (CDKs), Janus Kinase 2 (JAK2), and Fms-like Tyrosine Kinase-3 (FLT3) for the ... Blachly JS, Byrd JC, Grever M (April 2016). "Cyclin-dependent kinase inhibitors for the treatment of chronic lymphocytic ... Discovery of Kinase Spectrum Selective Macrocycle (16E)-14-Methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)] ...
Protein kinase inhibitors, Sulfonamides, 1-Piperidinyl compounds, Lactams, All stub articles, Pharmacology stubs). ... Hesperadin works as an inhibitor, attaching to the active sites of Aurora A and Aurora B kinases. Hauf, Silke; Cole, Richard W ... Hesperadin is an aurora kinase inhibitor. The small molecule inhibits chromosome alignment and segregation by limiting the ... Hesperadin, like other miotic inhibitors, limits and sometimes can stop the process of mitosis in cells. For this reason, some ...
Protein kinase inhibitors, Aminopyrimidines). ... Cerdulatinib is a small molecule SYK/JAK kinase inhibitor in ... December 2014). "The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell ... "Syk inhibitors in clinical development for hematological malignancies". Journal of Hematology & Oncology. 10 (1): 145. doi: ...
Protein kinase inhibitors, Pyrazoles, Pyrimidines, Nitriles). ... is a small molecule checkpoint kinase inhibitor, mainly active ...
Protein kinase inhibitors, Chemotherapeutic adjuvants, Pyridines, Piperazines, Spiro compounds, Amides, Guanidines, All stub ... Trilaciclib may help protect bone marrow cells from damage caused by chemotherapy by inhibiting cyclin-dependent kinase 4/6, a ... a CDK 4/6 Inhibitor, in Extensive Stage Small Cell Lung Cancer (SCLC)" at ClinicalTrials.gov Clinical trial number NCT02499770 ... a CDK 4/6 Inhibitor, in Patients With Previously Treated Extensive Stage SCLC Receiving Topotecan Chemotherapy" at ...
At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L). K252a ... This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and ... Protein kinase inhibitors, TrkB antagonists, Tertiary alcohols, Methyl esters, All stub articles, Biochemistry stubs). ... has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase ...
Protein kinase inhibitors, Quinazolines). ... it is an inhibitor of Rho-associated coiled-coil kinase 2 ( ... "Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or ... It is in the class of drugs known as serine/threonine kinase inhibitors. Specifically, ... Park J, Chun KH (5 May 2020). "Identification of novel functions of the ROCK2-specific inhibitor KD025 by bioinformatics ...
"Primary-structure requirements for inhibition by the heat-stable inhibitor of the cAMP-dependent protein kinase". PNAS. 83 (6 ... It should not be confused with 5'-AMP-activated protein kinase (AMP-activated protein kinase). Protein kinase A, more precisely ... Protein kinase Signal transduction G protein-coupled receptor Serine/threonine-specific protein kinase Myosin light-chain ... out of 540 different protein kinase genes that make up the human kinome, only one other protein kinase, casein kinase 2, is ...
Liu B, Shuai K (2001). "Induction of apoptosis by protein inhibitor of activated Stat1 through c-Jun NH2-terminal kinase ... and glycine-rich protein 2 (CRP2) is a novel marker of hepatic stellate cells and binding partner of the protein inhibitor of ... protein inhibitor of activated STAT) proteins differ in their ability to modulate steroid receptor-dependent transcriptional ... "Entrez Gene: PIAS1 protein inhibitor of activated STAT, 1". Ling Y, Sankpal UT, Robertson AK, McNally JG, Karpova T, Robertson ...