• The most extensively studied member is DAPK1 (based on the publications number and Protein Data Bank reported crystal structures) that plays fundamental biological roles depending on the cellular context. (inpst.net)
  • In continuous cell lines, mRNA expression was down-regulated, as well as compared with nonmalignant bronchial epithelial cells, and its protein was not detected by Western blotting in 17 of 23 (74%) cell lines. (nih.gov)
  • Broad in its range of techniques and thoroughly detailed to help ensure experimental success, Protein Kinase Protocols offers both novice and experienced investigators powerful tools for understanding the functional roles of specific protein kinases within signaling cascades and for identification and evaluation of novel therapeutic targets. (springer.com)
  • Here we review recent developments in the area of these cardiotrophic kinases, highlighting the utility of animal models that are helping to identify molecular targets in the human condition. (jci.org)
  • Therefore, proteins that regulate the GPCR signaling are likely to be critical for a variety of diseases and represent important therapeutic targets. (eurekalert.org)
  • The interdisciplinary nature of this meeting stems from appreciation that only joint effort of investigators studying the mechanisms of GRK action in different model system from pure proteins to living animals will overcome challenges that remain in the GRK field and will allow to fully exploit the potential of GRKs as therapeutic targets. (eurekalert.org)
  • In view of the fact that most of these kinases are activated in heart disease and their inhibition has been shown to improve cardiac function, it is suggested that these kinases form excellent targets for drug development for therapy of heart disease. (mdpi.com)
  • The compounds KT 5720, Rottlerin and quercetin were found to inhibit many protein kinases, sometimes much more potently than their presumed targets, and conclusions drawn from their use in cell-based experiments are likely to be erroneous. (psu.edu)
  • The ability to determine structure-activity relationships (SAR) and identify cellular targets from cell lysates and tissues is of great utility for kinase inhibitor drug discovery. (rsc.org)
  • Stringent selection criteria for target identification were applied to deduce 28 protein targets for dasatinib and 31 protein targets for our general type II kinase inhibitor in HeLa cell lysate. (rsc.org)
  • Additional kinase and protein targets were identified with the general type II inhibitor analogs, with small structural changes leading to divergent target profiles. (rsc.org)
  • Our rapid workflow profiled cellular targets for six small molecules within a week, demonstrating that an unbiased proteomics screen of cellular targets yields valuable SAR information and may be incorporated at an early stage in kinase inhibitor development. (rsc.org)
  • Protein kinases are key focus targets in drug discovery. (perkinelmer.com)
  • In contrast to the classical MAP kinases, these atypical MAPKs require only a single residue in their activation loops to be phosphorylated. (wikipedia.org)
  • Four human protein kinases (underlined) representing the four major families in the CMGC group (CDKs, MAPKs, GSK3, and CDK-like) were included in the alignment to anchor the position of these families in the tree. (asmscience.org)
  • We have catalogued the protein kinase complement of the human genome (the "kinome") using public and proprietary genomic, complementary DNA, and expressed sequence tag (EST) sequences. (sciencemag.org)
  • This provides a starting point for comprehensive analysis of protein phosphorylation in normal and disease states, as well as a detailed view of the current state of human genome analysis through a focus on one large gene family. (sciencemag.org)
  • With the advent of DNA cloning and sequencing in the mid-1970s, it rapidly became clear that a large family of eukaryotic protein kinases exists, and the burgeoning numbers of protein kinases led to the speculation that a vertebrate genome might encode as many as 1001 protein kinases ( 1 ). (sciencemag.org)
  • The near-completion of the human genome sequence now allows the identification of almost all human protein kinases. (sciencemag.org)
  • The figure depicts only the CMGC branch of a larger tree constructed (by J. Packer, Abbott Laboratories) from a Hidden Markov Model-derived alignment of all protein kinases in the P. falciparum genome. (asmscience.org)
  • The presence of closely related kinases in regions of the genome known to have arisen by genome duplication indicates that these kinases probably arose by divergence from common ancestors. (plantphysiol.org)
  • The completed sequence of the Arabidopsis genome provides the first opportunity to identify all of the protein kinases present in a model plant. (plantphysiol.org)
  • The human protein kinase family is divided into the following groups: AGC kinases - containing PKA, PKC and PKG. (wikipedia.org)
  • At least 125 of the 500+ human protein kinases are serine/threonine kinases (STK). (wikipedia.org)
  • New nucleic acid sequences are provided which encode 3' untranslated regions of human protein kinase C alpha polynucleotide probes for PKC alpha are also disclosed. (google.com.au)
  • 10. An antisense oligonuclcotide 5 to 50 nucleotides in length comprising a nucleotide sequence which is complementary to the long mRNA transcript of human protein kinase C-α and which is not complementary to the short mRNA transcript of human protein kinase C-α. (google.com.au)
  • 13. A polynucleotide probe comprising a nuclcotide sequence complementary to the long mRNA transcript of human protein kinase C-α. (google.com.au)
  • 15. A method of inhibiting the expression of human protein kinase C-α in vitro comprising contacting human cells with a therapeutically effective amount of an antisense oligonucleotide 5 to 50 nucleotides in length, said antisense oligonucleotide comprising a nucleotide sequence complementary to a portion of the sequence set forth in SEQ ID NO: 105. (google.com.au)
  • As the world's leading gene company, OriGene offers comprehensive product solutions for studying human protein kinases. (origene.com)
  • Important subgroups are the kinases of the ERK subfamily, typically activated by mitogenic signals, and the stress-activated protein kinases JNK and p38. (wikipedia.org)
  • In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. (hindawi.com)
  • Curcumin has anti-breast cancer activity related to the activities of protein kinases on cell signal pathway. (greenmedinfo.com)
  • Src (pronounced "sarc" as it is short for sarcoma) is a proto-oncogene encoding a tyrosine kinase originally discovered by J. Michael Bishop and Harold E. Varmus, for which they were awarded the 1989 Nobel Prize in Physiology or Medicine. (wikipedia.org)
  • MAP kinases are found in eukaryotes only, but they are fairly diverse and encountered in all animals, fungi and plants, and even in an array of unicellular eukaryotes. (wikipedia.org)
  • By this analysis, there were 53 distinct kinase functions in the early common ancestor of all these eukaryotes, and there has been much gain and loss since then. (kinase.com)
  • In addition, phosphorylation sites may act through combinatorial mechanisms or through cross-talk with other posttranslational modifications (PTMs) 1 ( 17 , 18 ), thus further increasing the complexity of kinase regulatory networks. (mcponline.org)
  • In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated methods for the analysis of kinase-mediated signaling cascades, with emphasis on the identification of proteins according to their interactive relationships and the analysis of their functional properties. (springer.com)
  • Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test. (drugbank.ca)
  • Ceritinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. (drugbank.ca)
  • 3.3 Anaplastic Lymphoma Kinase. (whsmith.co.uk)
  • The identification of protein kinase C iota as a regulator of the Mammalian heat shock response using functional genomic screens. (ebi.ac.uk)
  • Mitogen-activated protein kinases have been implicated in ventilator-induced lung injury though their functional significance remains incomplete. (plos.org)
  • Phosphorylation usually alters the functional characteristics of the target protein and can act as an on/off switch for protein functions. (sigmaaldrich.com)
  • Dr. Khalil Ahmed is a Professor at the University of Minnesota, and a Senior Research Career Scientist at Minneapolis VA Health Care System, Minneapolis, Minnesota, U.S.A. He has a long history of studies on the functional biology of protein kinase CK2 in normal and neoplastic cells. (springer.com)
  • LC Sciences is a genomics and proteomics company offering innovative, customizable, and comprehensive microarray services for nucleic acid/protein profiling and functional analysis, biomarker-discovery, novel drug screening, and the custom development of diagnostic devices. (bio-medicine.org)
  • Working in cell lines and mouse models of glioblastoma multiforme, the most lethal form of brain tumor, senior author Zhimin Lu, Ph.D., associate professor of Neuro-Oncology at MD Anderson, and colleagues show that pyruvate kinase M2 (PKM2) fuels tumor growth by influencing a histone protein. (news-medical.net)