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Cyclin-dependent kinase 9

TAK, CDK9, Cyclin-Dependent Kinase 9
The protein encoded by this gene is a member of the cyclin-dependent protein kinase (CDK) family. CDK family members are highly similar to the gene products of S. cerevisiae cdc28, and S. pombe cdc2, and known as important cell cycle regulators. This kinase was found to be a component of the multiprotein complex TAK/P-TEFb, which is an elongation factor for RNA polymerase II-directed transcription and functions by phosphorylating the C-terminal domain of the largest subunit of RNA polymerase II. This protein forms a complex with and is regulated by its regulatory subunit cyclin T or cyclin K. HIV-1 Tat protein was found to interact with this protein and cyclin T, which suggested a possible involvement of this protein in AIDS. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: PCNA, POLYMERASE, CAN, V1a, HAD
Papers using TAK antibodies
Identification of the vesicular nucleotide transporter (VNUT) in taste cells.
Meyerhof Wolfgang, In PLoS ONE, 2008
... Slices containing vallate taste buds were mounted on a glass coverslip coated with Cell-Tak (Becton Dickinson, Franklin Lakes, NJ, USA), ...
In vivo gene delivery and stable transduction of nondividing cells by a lentiviral vector
Fujinaga Koh et al., In Retrovirology, 1995
... Anti-myc, anti-HA, anti-CycT1, anti-Cdk9, and anti-Ub antibodies were purchased from Santa Cruz Biotechnology (Santa Cruz, CA) ...
Papers on TAK
Beta-arrestin-2 negatively modulates inflammation response in mouse chondrocytes induced by 4-mer hyaluronan oligosaccharide.
Campo et al., Messina, Italy. In Mol Cell Biochem, 16 Nov 2014
NF-kB activation is mediated by different pathways, in particular by the transforming growth factor-activated kinase-1 (TAK-1).
A gene-specific role for the Ssu72 RNAPII CTD phosphatase in HIV-1 Tat transactivation.
Jones et al., Los Angeles, United States. In Genes Dev, 15 Nov 2014
HIV-1 Tat stimulates transcription elongation by recruiting the P-TEFb (positive transcription elongation factor-b) (CycT1:CDK9) C-terminal domain (CTD) kinase to the HIV-1 promoter.
Structure-based lead discovery for protein kinase C zeta inhibitor design by exploiting kinase-inhibitor complex crystal structure data and potential therapeutics for preterm labour.
Li et al., Weifang, China. In Arch Pharm Res, 14 Nov 2014
CDK6 inhibitor fisetin, PIM1 inhibitor myricetin, CDK9 inhibitor flavopiridol and PknB inhibitor mitoxantrone as well as the promiscuous kinase inhibitor staurosporine showed high or moderate inhibitory activity on PKCζ, with IC50 values of 58 ± 9, 1.7 ± 0.4,
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
Okada et al., San Diego, United States. In Nature, 04 Oct 2014
TAK-875, or fasiglifam, is an orally available, potent and selective partial agonist of hGPR40 receptor, which reached phase III clinical trials for the potential treatment of type-2 diabetes mellitus.
Physiology and therapeutics of the free fatty acid receptor GPR40.
Tao et al., Auburn, United States. In Prog Mol Biol Transl Sci, Dec 2013
Recently, one of these ligands, TAK-875, has been successfully tested in phase II clinical trials with reduced risk of hypoglycemia.
Fasiglifam as a new potential treatment option for patients with type 2 diabetes.
Kaku, Kurashiki, Japan. In Expert Opin Pharmacother, Dec 2013
AREAS COVERED: This review is based on a PubMed search for all articles on fasiglifam and TAK-875.
Regulation of CDK9 activity by phosphorylation and dephosphorylation.
Breuer et al., Washington, D.C., United States. In Biomed Res Int, Dec 2013
HIV-1 transcription is regulated by CDK9/cyclin T1, which, unlike a typical cell cycle-dependent kinase, is regulated by associating with 7SK small nuclear ribonuclear protein complex (snRNP).
Spatial Variation in Genetic Diversity and Natural Selection on the Thrombospondin-Related Adhesive Protein Locus of Plasmodium vivax (PvTRAP).
Jongwutiwes et al., Bangkok, Thailand. In Plos One, Dec 2013
To gain insights into variation in the complete PvTRAP sequences of parasites in Thailand, 114 vivax malaria patients were recruited in 2006-2007 from 4 major endemic provinces bordering Myanmar (Tak in the northwest, n = 30 and Prachuap Khirikhan in the southwest, n = 25), Cambodia (Chanthaburi in the east, n = 29) and Malaysia (Yala and Narathiwat in the south, n = 30).
Interaction between HIV-1 Tat and DNA-PKcs modulates HIV transcription and class switch recombination.
Zhou et al., Beijing, China. In Int J Biol Sci, Dec 2013
Co-immunoprecipitation results revealed that DNA-PKcs forms a large complex comprised of Cyclin T1, CDK9 and Tat via direct interacting with CDK9 and Tat but not Cyclin T1.
Activation of GPR40 as a therapeutic target for the treatment of type 2 diabetes.
Burant, Ann Arbor, United States. In Diabetes Care, Aug 2013
Recent phase I and phase II clinical trials in humans have shown that the GPR40 agonist TAK-875 reduces fasting and postprandial blood glucose and lowers HbA1c with efficacy equal to that of the sulfonylurea glimepiride without inducing hypoglycemia or evidence of tachyphylaxis.
HIF1A employs CDK8-mediator to stimulate RNAPII elongation in response to hypoxia.
Espinosa et al., Boulder, United States. In Cell, Jul 2013
HIF1A induces binding of CDK8-Mediator and the super elongation complex (SEC), containing AFF4 and CDK9, to alleviate RNAPII pausing.
Efficacy and toxicity of factor Xa inhibitors.
Vanelle et al., Marseille, France. In J Pharm Pharm Sci, 2012
New antithrombotics such as rivaroxaban, apixaban, betrixaban, edoxaban, darexaban, TAK-442, LY517717, eribaxaban, otamixaban are being developed to overcome current therapeutic limitations.
The super elongation complex (SEC) family in transcriptional control.
Shilatifard et al., Kansas City, United States. In Nat Rev Mol Cell Biol, 2012
Studies indicate that the super elongation complex (SEC) consisting of ELL, P-TEFb (CDK9) and MLL required for rapid transcriptional induction in the presence or absence of paused RNA polymerase II (Pol II).
Separate domains of fission yeast Cdk9 (P-TEFb) are required for capping enzyme recruitment and primed (Ser7-phosphorylated) Rpb1 carboxyl-terminal domain substrate recognition.
Fisher et al., New York City, United States. In Mol Cell Biol, 2012
a Cdk9 carboxyl-terminal extension, distinct from the catalytic domain, mediates binding to both Pcm1 and the Pol II carboxyl-terminal domain
Phosphorylation by cyclin-dependent kinase-9 controls ubiquitin-conjugating enzyme-2A function.
Johnsen et al., Göttingen, Germany. In Cell Cycle, 2012
CDK9 phosphorylates UBE2A and regulates UBE2A-mediated monoubiquitination of both H2B and PCNA.
TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial.
Leifke et al., Ann Arbor, United States. In Lancet, 2012
We aimed to assess whether selective pharmacological activation of this receptor by TAK-875 in patients with type 2 diabetes mellitus improved glycaemic control without hypoglycaemia risk.
Cyclin-dependent kinase 7/9 inhibitor SNS-032 abrogates FIP1-like-1 platelet-derived growth factor receptor α and bcr-abl oncogene addiction in malignant hematologic cells.
Pan et al., Guangzhou, China. In Clin Cancer Res, 2012
Data show that the cyclin-dependent kinase 7/9 inhibitor (CDK7/9 inhibitor) potently inhibits FIP1L1-PDGFRalpha-positive Bcr-Abl-positive chronic myeloid leukemia (CML) cells.
Flavopiridol induces phosphorylation of AKT in a human glioblastoma cell line, in contrast to siRNA-mediated silencing of Cdk9: Implications for drug design and development.
Giordano et al., Philadelphia, United States. In Cell Cycle, 2012
siRNA-mediated inhibition of Cdk9 caused a shift from G 0/G 1 to G 2/M phase in human PC3 prostate cancer cell line.
RNAP II CTD phosphorylated on threonine-4 is required for histone mRNA 3' end processing.
Manley et al., New York City, United States. In Science, 2011
Like Ser(2), Thr(4) phosphorylation requires the CTD kinase CDK9 and is evolutionarily conserved from yeast to human.
Crystal structure of HIV-1 Tat complexed with human P-TEFb.
Price et al., Omaha, United States. In Nature, 2010
Here we describe the crystal structure of the Tat.P-TEFb complex containing HIV-1 Tat, human Cdk9 (also known as CDK9), and human cyclin T1 (also known as CCNT1).
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