Property Summary

NCBI Gene PubMed Count 115
Grant Count 206
R01 Count 124
Funding $14,253,774.15
PubMed Score 806.39
PubTator Score 585.89

Knowledge Summary

Patent (30,266)

Expression

  Differential Expression (6)

Disease log2 FC p
chronic lymphosyte leukemia -1.900 0.000
psoriasis 2.300 0.000
osteosarcoma 1.731 0.000
acute quadriplegic myopathy 1.075 0.000
intraductal papillary-mucinous neoplasm ... -1.200 0.002
ovarian cancer 2.500 0.000

Synonym

Accession Q9NZJ5 A0AVH1 A0AVH2 B2RCU9 O95846 Q53QY0 Q53SB1
Symbols PEK
WRS
PERK

Gene

PDB

4G31   4G34   4M7I   4X7H   4X7J   4X7K   4X7L   4X7N   4X7O   4YZS  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (4)

AID Type Active / Inconclusive / Inactive Description
1416 screening 370 / 0 / 217747 Primary cell-based high-throughput screening assay to measure PERK inhibition
1522 confirmatory 0 / 0 / 118 Dose response cell-based high-throughput screening assay to measure PERK inhibition
1528 confirmatory 0 / 0 / 118 Counterscreen assay for PERK inhibitors: Dose response cell-based high throughput screening assay to measure inhibition of PERK at 6 hours
1842 summary 0 / 0 / 10 Summary of probe development efforts to identify inhibitors of RNA-dependent protein kinase (PKR)-like ER kinase (PERK)

Gene RIF (91)

PMID Text
26642955 This study demonstrates a new role for CREB as a regulator of ER stress, which is required to properly respond to stressful conditions, such as hypoxia.
26634309 Using drugs that specifically inhibit or activate the PERK or IRE1alpha sensors, we demonstrate that signalling through the PERK axis activates this expression, through a transcriptional mechanism
26486079 Data show CGK733 induced microtubule associated protein LC3B formation upstream of AMP-activated protein kinase and protein kinase RNA-like endoplasmic reticulum kinase/CCAAT-enhancer-binding protein homologous protein pathways and p21 Cip1 expression.
26446798 Nitric oxide can S-nitrosylate the endoplasmic reticulum stress sensors IRE1alapha and PERK.
26279443 In human alveolar epithelial A549 cells, Lipopolysaccharide induces autophagic cell death that depends on the activation of the PERK branch of the unfolded protein response upon endoplasmic reticulum (ER) stress .
26259235 CGK733-induced intracellular calcium sequestration in pancreatic tumor cells is correlated with the PERK/CHOP signaling pathway and may also be involved in the dysregulations of calcium-binding proteins.
26225772 In this review, we particularly focused on the novel, intriguing and complicated role of PERK in ER stress-decided cell fate, and also discussed more roles of PERK in restoring cellular homeostasis
26078722 PERK-activated osteosarcomatous autophagy via inhibition of the mTORC1 pathway prevents cell apoptosis.
25976933 These results confirm that HIV infection activates stress-response components and that antiretroviral therapy contributes to changes in the unfolded protein response activation profile.
25925385 interface mutations that disrupt tetramer formation in vitro reduce phosphorylation of PERK and its target eIF2alpha in cells.
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AA Sequence

MERAISPGLLVRALLLLLLLLGLAARTVAAGRARGLPAPTAEAAFGLGAAAAPTSATRVPAAGAVAAAEV      1 - 70
TVEDAEALPAAAGEQEPRGPEPDDETELRPRGRSLVIISTLDGRIAALDPENHGKKQWDLDVGSGSLVSS     71 - 140
SLSKPEVFGNKMIIPSLDGALFQWDQDRESMETVPFTVESLLESSYKFGDDVVLVGGKSLTTYGLSAYSG    141 - 210
KVRYICSALGCRQWDSDEMEQEEDILLLQRTQKTVRAVGPRSGNEKWNFSVGHFELRYIPDMETRAGFIE    211 - 280
STFKPNENTEESKIISDVEEQEAAIMDIVIKVSVADWKVMAFSKKGGHLEWEYQFCTPIASAWLLKDGKV    281 - 350
IPISLFDDTSYTSNDDVLEDEEDIVEAARGATENSVYLGMYRGQLYLQSSVRISEKFPSSPKALESVTNE    351 - 420
NAIIPLPTIKWKPLIHSPSRTPVLVGSDEFDKCLSNDKFSHEEYSNGALSILQYPYDNGYYLPYYKRERN    421 - 490
KRSTQITVRFLDNPHYNKNIRKKDPVLLLHWWKEIVATILFCIIATTFIVRRLFHPHPHRQRKESETQCQ    491 - 560
TENKYDSVSGEANDSSWNDIKNSGYISRYLTDFEPIQCLGRGGFGVVFEAKNKVDDCNYAIKRIRLPNRE    561 - 630
LAREKVMREVKALAKLEHPGIVRYFNAWLEAPPEKWQEKMDEIWLKDESTDWPLSSPSPMDAPSVKIRRM    631 - 700
DPFATKEHIEIIAPSPQRSRSFSVGISCDQTSSSESQFSPLEFSGMDHEDISESVDAAYNLQDSCLTDCD    701 - 770
VEDGTMDGNDEGHSFELCPSEASPYVRSRERTSSSIVFEDSGCDNASSKEEPKTNRLHIGNHCANKLTAF    771 - 840
KPTSSKSSSEATLSISPPRPTTLSLDLTKNTTEKLQPSSPKVYLYIQMQLCRKENLKDWMNGRCTIEERE    841 - 910
RSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVGDFGLVTAMDQDEEEQTVLTPMPAYAR    911 - 980
HTGQVGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYPFSTQMERVRTLTDVRNLKFPPLFTQKYPCE    981 - 1050
YVMVQDMLSPSPMERPEAINIIENAVFEDLDFPGKTVLRQRSRSLSSSGTKHSRQSNNSHSPLPSN       1051 - 1116
//

Text Mined References (120)

PMID Year Title
27238082 2016 Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance.
26642955 2016 CREB is activated by ER stress and modulates the unfolded protein response by regulating the expression of IRE1? and PERK.
26634309 2015 The Malat1 long non-coding RNA is upregulated by signalling through the PERK axis of unfolded protein response during flavivirus infection.
26486079 2015 CGK733-induced LC3 II formation is positively associated with the expression of cyclin-dependent kinase inhibitor p21Waf1/Cip1 through modulation of the AMPK and PERK/CHOP signaling pathways.
26446798 2015 Regulation of the unfolded protein response via S-nitrosylation of sensors of endoplasmic reticulum stress.
26279443 2015 Lipopolysaccharide Induces Autophagic Cell Death through the PERK-Dependent Branch of the Unfolded Protein Response in Human Alveolar Epithelial A549 Cells.
26268696 2015 TMEM33: a new stress-inducible endoplasmic reticulum transmembrane protein and modulator of the unfolded protein response signaling.
26259235 2015 PERK/CHOP contributes to the CGK733-induced vesicular calcium sequestration which is accompanied by non-apoptotic cell death.
26225772 2015 Protein kinase R-like ER kinase and its role in endoplasmic reticulum stress-decided cell fate.
26078722 2015 PERK-mediated Autophagy in Osteosarcoma Cells Resists ER Stress-induced Cell Apoptosis.
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