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Identification
NameTenecteplase
Accession NumberDB00031  (BTD00019, BIOD00019)
TypeBiotech
GroupsApproved
Description

Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.

Protein structureDb00031
Related Articles
Protein chemical formulaC2561H3919N747O781S40
Protein average weight58951.2 Da
Sequences
>DB00031 sequence
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG
TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGNWSTAESGAECTQWNSSA
LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC
YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK
PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAAAAKHRRS
PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH
KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL
SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG
PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
t- PA
t-plasminogen activator
Tissue-type plasminogen activator precursor
tPA
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TnkasekitGenentech, Inc.2000-06-02Not applicableUs
Tnkasepowder for solution50 mgintravenousHoffmann La Roche Limited2001-10-18Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIWGD229O42W
CAS number191588-94-0
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of myocardial infarction and lysis of intracoronary emboli
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of actionTenecteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)
Clearance
  • 99 – 119 mL/min [acute myocardial infarction patients]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Tenecteplase Action PathwayDrug actionSMP00283
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Kit
Powder for solutionintravenous50 mg
Prices
Unit descriptionCostUnit
Tnkase 50 mg kit3238.76USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1341432 No2003-06-172020-06-17Canada
CA2129660 No2005-06-282013-05-28Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.528Not Available
isoelectric point7.61Not Available
References
Synthesis ReferenceNot Available
General References
  1. Gurbel PA, Hayes K, Bliden KP, Yoho J, Tantry US: The platelet-related effects of tenecteplase versus alteplase versus reteplase. Blood Coagul Fibrinolysis. 2005 Jan;16(1):1-7. [PubMed:15650539 ]
  2. Melzer C, Richter C, Rogalla P, Borges AC, Theres H, Baumann G, Laule M: Tenecteplase for the treatment of massive and submassive pulmonary embolism. J Thromb Thrombolysis. 2004 Aug;18(1):47-50. [PubMed:15744554 ]
  3. Ohman EM, Van de Werf F, Antman EM, Califf RM, de Lemos JA, Gibson CM, Oliverio RL, Harrelson L, McCabe C, DiBattiste P, Braunwald E: Tenecteplase and tirofiban in ST-segment elevation acute myocardial infarction: results of a randomized trial. Am Heart J. 2005 Jul;150(1):79-88. [PubMed:16084152 ]
  4. De Luca G, Suryapranata H, Chiariello M: Tenecteplase followed by immediate angioplasty is more effective than tenecteplase alone for people with STEMI. Commentary. Evid Based Cardiovasc Med. 2005 Dec;9(4):284-7. Epub 2005 Nov 2. [PubMed:16380055 ]
  5. Authors unspecified: Primary versus tenecteplase-facilitated percutaneous coronary intervention in patients with ST-segment elevation acute myocardial infarction (ASSENT-4 PCI): randomised trial. Lancet. 2006 Feb 18;367(9510):569-78. [PubMed:16488800 ]
External Links
ATC CodesB01AD11
AHFS Codes
  • 20:12.20
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabTenecteplase may increase the anticoagulant activities of Abciximab.
AcenocoumarolTenecteplase may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tenecteplase.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tenecteplase.
AnagrelideAnagrelide may increase the anticoagulant activities of Tenecteplase.
ApixabanTenecteplase may increase the anticoagulant activities of Apixaban.
AprotininThe therapeutic efficacy of Tenecteplase can be decreased when used in combination with Aprotinin.
ArgatrobanTenecteplase may increase the anticoagulant activities of Argatroban.
Bismuth SubsalicylateThe risk or severity of adverse effects can be increased when Bismuth Subsalicylate is combined with Tenecteplase.
BivalirudinTenecteplase may increase the anticoagulant activities of Bivalirudin.
CaffeineCaffeine may increase the anticoagulant activities of Tenecteplase.
CangrelorCangrelor may increase the anticoagulant activities of Tenecteplase.
CilostazolCilostazol may increase the anticoagulant activities of Tenecteplase.
CitalopramCitalopram may increase the anticoagulant activities of Tenecteplase.
Citric AcidTenecteplase may increase the anticoagulant activities of Citric Acid.
ClopidogrelClopidogrel may increase the anticoagulant activities of Tenecteplase.
Dabigatran etexilateTenecteplase may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinTenecteplase may increase the anticoagulant activities of Dalteparin.
DanaparoidTenecteplase may increase the anticoagulant activities of Danaparoid.
DesirudinTenecteplase may increase the anticoagulant activities of Desirudin.
DesvenlafaxineDesvenlafaxine may increase the anticoagulant activities of Tenecteplase.
DiclofenacDiclofenac may increase the anticoagulant activities of Tenecteplase.
DicoumarolTenecteplase may increase the anticoagulant activities of Dicoumarol.
DiflunisalDiflunisal may increase the anticoagulant activities of Tenecteplase.
DihydrocodeineDihydrocodeine may increase the anticoagulant activities of Tenecteplase.
DipyridamoleDipyridamole may increase the anticoagulant activities of Tenecteplase.
DuloxetineDuloxetine may increase the anticoagulant activities of Tenecteplase.
Edetic AcidTenecteplase may increase the anticoagulant activities of Edetic Acid.
EdoxabanTenecteplase may increase the anticoagulant activities of Edoxaban.
EnoxaparinTenecteplase may increase the anticoagulant activities of Enoxaparin.
EpoprostenolThe risk or severity of adverse effects can be increased when Tenecteplase is combined with Epoprostenol.
EptifibatideEptifibatide may increase the anticoagulant activities of Tenecteplase.
EscitalopramEscitalopram may increase the anticoagulant activities of Tenecteplase.
Ethyl biscoumacetateTenecteplase may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacEtodolac may increase the anticoagulant activities of Tenecteplase.
FenoprofenFenoprofen may increase the anticoagulant activities of Tenecteplase.
FloctafenineFloctafenine may increase the anticoagulant activities of Tenecteplase.
FluoxetineFluoxetine may increase the anticoagulant activities of Tenecteplase.
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Tenecteplase.
FluvoxamineFluvoxamine may increase the anticoagulant activities of Tenecteplase.
Fondaparinux sodiumTenecteplase may increase the anticoagulant activities of Fondaparinux sodium.
HeparinTenecteplase may increase the anticoagulant activities of Heparin.
IbuprofenIbuprofen may increase the anticoagulant activities of Tenecteplase.
IloprostThe risk or severity of adverse effects can be increased when Tenecteplase is combined with Iloprost.
IndomethacinIndomethacin may increase the anticoagulant activities of Tenecteplase.
KetoprofenKetoprofen may increase the anticoagulant activities of Tenecteplase.
KetorolacKetorolac may increase the anticoagulant activities of Tenecteplase.
LevomilnacipranLevomilnacipran may increase the anticoagulant activities of Tenecteplase.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Tenecteplase.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Tenecteplase.
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Tenecteplase.
MeloxicamMeloxicam may increase the anticoagulant activities of Tenecteplase.
MilnacipranMilnacipran may increase the anticoagulant activities of Tenecteplase.
NabumetoneNabumetone may increase the anticoagulant activities of Tenecteplase.
NadroparinTenecteplase may increase the anticoagulant activities of Nadroparin.
NaproxenNaproxen may increase the anticoagulant activities of Tenecteplase.
OxaprozinOxaprozin may increase the anticoagulant activities of Tenecteplase.
ParoxetineParoxetine may increase the anticoagulant activities of Tenecteplase.
PhenindioneTenecteplase may increase the anticoagulant activities of Phenindione.
PhenprocoumonTenecteplase may increase the anticoagulant activities of Phenprocoumon.
PiroxicamPiroxicam may increase the anticoagulant activities of Tenecteplase.
PrasugrelPrasugrel may increase the anticoagulant activities of Tenecteplase.
RivaroxabanTenecteplase may increase the anticoagulant activities of Rivaroxaban.
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Tenecteplase.
SertralineSertraline may increase the anticoagulant activities of Tenecteplase.
SulindacSulindac may increase the anticoagulant activities of Tenecteplase.
SulodexideTenecteplase may increase the anticoagulant activities of Sulodexide.
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Tenecteplase.
TicagrelorTicagrelor may increase the anticoagulant activities of Tenecteplase.
TiclopidineTiclopidine may increase the anticoagulant activities of Tenecteplase.
TinzaparinTenecteplase may increase the anticoagulant activities of Tinzaparin.
TirofibanTirofiban may increase the anticoagulant activities of Tenecteplase.
TolmetinTolmetin may increase the anticoagulant activities of Tenecteplase.
TreprostinilTenecteplase may increase the anticoagulant activities of Treprostinil.
VenlafaxineVenlafaxine may increase the anticoagulant activities of Tenecteplase.
VilazodoneVilazodone may increase the anticoagulant activities of Tenecteplase.
VorapaxarVorapaxar may increase the anticoagulant activities of Tenecteplase.
VortioxetineVortioxetine may increase the anticoagulant activities of Tenecteplase.
WarfarinTenecteplase may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
activator
General Function:
Serine-type peptidase activity
Specific Function:
Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin ...
Gene Name:
PLG
Uniprot ID:
P00747
Molecular Weight:
90568.415 Da
References
  1. Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235 ]
  2. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656 ]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Structural molecule activity
Specific Function:
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelializati...
Gene Name:
FGA
Uniprot ID:
P02671
Molecular Weight:
94972.455 Da
References
  1. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656 ]
  2. Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235 ]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Urokinase plasminogen activator receptor activity
Specific Function:
Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.
Gene Name:
PLAUR
Uniprot ID:
Q03405
Molecular Weight:
36977.62 Da
References
  1. Maupas-Schwalm F, Auge N, Robinet C, Cambus JP, Parsons SJ, Salvayre R, Negre-Salvayre A: The sphingomyelin/ceramide pathway is involved in ERK1/2 phosphorylation, cell proliferation, and uPAR overexpression induced by tissue-type plasminogen activator. FASEB J. 2004 Sep;18(12):1398-400. Epub 2004 Jul 1. [PubMed:15231724 ]
  2. Bankl HC, Samorapoompichit P, Pikula B, Latinovic L, Bankl H, Lechner K, Valent P: Characterization of human prostate mast cells and their increase in periprostatic vein thrombosis. Am J Clin Pathol. 2001 Jul;116(1):97-106. [PubMed:11447759 ]
  3. Ferrier CM, Van Geloof WL, Straatman H, Van De Molengraft FJ, Van Muijen GN, Ruiter DJ: Spitz naevi may express components of the plasminogen activation system. J Pathol. 2002 Sep;198(1):92-9. [PubMed:12210068 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis.
Gene Name:
SERPINE1
Uniprot ID:
P05121
Molecular Weight:
45059.695 Da
References
  1. Lindberg P, Kinnby B, Lecander I, Lang NP, Matsson L: Increasing expression of tissue plasminogen activator and plasminogen activator inhibitor type 2 in dog gingival tissues with progressive inflammation. Arch Oral Biol. 2001 Jan;46(1):23-31. [PubMed:11163592 ]
  2. Hattori M, Azami Y: Searching for preventive measures of cardiovascular events in aged Japanese taxi drivers--the daily rhythm of cardiovascular risk factors during a night duty day. J Hum Ergol (Tokyo). 2001 Dec;30(1-2):321-6. [PubMed:14564902 ]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Inhibits urokinase-type plasminogen activator. The monocyte derived PAI-2 is distinct from the endothelial cell-derived PAI-1.
Gene Name:
SERPINB2
Uniprot ID:
P05120
Molecular Weight:
46595.84 Da
References
  1. Verkleij-Hagoort AC, Ursem NT, Hop WC, Geurts-Moespot A, Steegers EA, Sweep FC, Steegers-Theunissen RP: Complex congenital malformations and the impact of the plasminogen activator system and beta-hCG in amniotic fluid. Eur J Obstet Gynecol Reprod Biol. 2007 Nov;135(1):47-52. Epub 2006 Dec 1. [PubMed:17141398 ]
  2. Bremer HA, Brommer EJ, Wallenburg HC: Effects of labor and delivery on fibrinolysis. Eur J Obstet Gynecol Reprod Biol. 1994 Jun 30;55(3):163-8. [PubMed:7958159 ]
  3. Stump DC, Thienpont M, Collen D: Purification and characterization of a novel inhibitor of urokinase from human urine. Quantitation and preliminary characterization in plasma. J Biol Chem. 1986 Sep 25;261(27):12759-66. [PubMed:3091604 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Kringle domain binding
Specific Function:
Tetranectin binds to plasminogen and to isolated kringle 4. May be involved in the packaging of molecules destined for exocytosis.
Gene Name:
CLEC3B
Uniprot ID:
P05452
Molecular Weight:
22536.665 Da
References
  1. Westergaard UB, Andersen MH, Heegaard CW, Fedosov SN, Petersen TE: Tetranectin binds hepatocyte growth factor and tissue-type plasminogen activator. Eur J Biochem. 2003 Apr;270(8):1850-4. [PubMed:12694198 ]
  2. Kamper EF, Kopeikina LT, Koutsoukos V, Stavridis J: Plasma tetranectin levels and disease activity in patients with rheumatoid arthritis. J Rheumatol. 1997 Feb;24(2):262-8. [PubMed:9034981 ]
  3. Vuckovic B, Deric M: [Lipoprotein(a): a link between thrombogenesis and atherogenesis]. Med Pregl. 2007 Jan-Feb;60(1-2):37-41. [PubMed:17853709 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Structural molecule activity
Specific Function:
Together with KRT19, helps to link the contractile apparatus to dystrophin at the costameres of striated muscle.
Gene Name:
KRT8
Uniprot ID:
P05787
Molecular Weight:
53703.76 Da
References
  1. Kralovich KR, Li L, Hembrough TA, Webb DJ, Karns LR, Gonias SL: Characterization of the binding sites for plasminogen and tissue-type plasminogen activator in cytokeratin 8 and cytokeratin 18. J Protein Chem. 1998 Nov;17(8):845-54. [PubMed:9988531 ]
  2. Hembrough TA, Kralovich KR, Li L, Gonias SL: Cytokeratin 8 released by breast carcinoma cells in vitro binds plasminogen and tissue-type plasminogen activator and promotes plasminogen activation. Biochem J. 1996 Aug 1;317 ( Pt 3):763-9. [PubMed:8760360 ]
  3. Hembrough TA, Li L, Gonias SL: Cell-surface cytokeratin 8 is the major plasminogen receptor on breast cancer cells and is required for the accelerated activation of cell-associated plasminogen by tissue-type plasminogen activator. J Biol Chem. 1996 Oct 11;271(41):25684-91. [PubMed:8810346 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
S100 protein binding
Specific Function:
Calcium-regulated membrane-binding protein whose affinity for calcium is greatly enhanced by anionic phospholipids. It binds two calcium ions with high affinity. May be involved in heat-stress response. Inhibits PCSK9-enhanced LDLR degradation, probably reduces PCSK9 protein levels via a translational mechanism but also competes with LDLR for binding with PCSK9 (PubMed:18799458, PubMed:24808179...
Gene Name:
ANXA2
Uniprot ID:
P07355
Molecular Weight:
38603.63 Da
References
  1. Diaz VM, Hurtado M, Thomson TM, Reventos J, Paciucci R: Specific interaction of tissue-type plasminogen activator (t-PA) with annexin II on the membrane of pancreatic cancer cells activates plasminogen and promotes invasion in vitro. Gut. 2004 Jul;53(7):993-1000. [PubMed:15194650 ]
  2. Kang HM, Choi KS, Kassam G, Fitzpatrick SL, Kwon M, Waisman DM: Role of annexin II tetramer in plasminogen activation. Trends Cardiovasc Med. 1999 Apr-May;9(3-4):92-102. [PubMed:10578524 ]
  3. MacLeod TJ, Kwon M, Filipenko NR, Waisman DM: Phospholipid-associated annexin A2-S100A10 heterotetramer and its subunits: characterization of the interaction with tissue plasminogen activator, plasminogen, and plasmin. J Biol Chem. 2003 Jul 11;278(28):25577-84. Epub 2003 Apr 30. [PubMed:12730231 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Zinc ion binding
Specific Function:
Calcium-binding chaperone that promotes folding, oligomeric assembly and quality control in the endoplasmic reticulum (ER) via the calreticulin/calnexin cycle. This lectin interacts transiently with almost all of the monoglucosylated glycoproteins that are synthesized in the ER. Interacts with the DNA-binding domain of NR3C1 and mediates its nuclear export. Involved in maternal gene expression ...
Gene Name:
CALR
Uniprot ID:
P27797
Molecular Weight:
48141.2 Da
References
  1. Allen S, Bulleid NJ: Calnexin and calreticulin bind to enzymically active tissue-type plasminogen activator during biosynthesis and are not required for folding to the native conformation. Biochem J. 1997 Nov 15;328 ( Pt 1):113-9. [PubMed:9359841 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Poly(a) rna binding
Specific Function:
Calcium-binding protein that interacts with newly synthesized glycoproteins in the endoplasmic reticulum. It may act in assisting protein assembly and/or in the retention within the ER of unassembled protein subunits. It seems to play a major role in the quality control apparatus of the ER by the retention of incorrectly folded proteins. Associated with partial T-cell antigen receptor complexes...
Gene Name:
CANX
Uniprot ID:
P27824
Molecular Weight:
67567.695 Da
References
  1. Allen S, Bulleid NJ: Calnexin and calreticulin bind to enzymically active tissue-type plasminogen activator during biosynthesis and are not required for folding to the native conformation. Biochem J. 1997 Nov 15;328 ( Pt 1):113-9. [PubMed:9359841 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor activity
Specific Function:
Endocytic receptor involved in endocytosis and in phagocytosis of apoptotic cells. Required for early embryonic development. Involved in cellular lipid homeostasis. Involved in the plasma clearance of chylomicron remnants and activated LRPAP1 (alpha 2-macroglobulin), as well as the local metabolism of complexes between plasminogen activators and their endogenous inhibitors. May modulate cellula...
Gene Name:
LRP1
Uniprot ID:
Q07954
Molecular Weight:
504601.695 Da
References
  1. Moestrup SK, Nielsen S, Andreasen P, Jorgensen KE, Nykjaer A, Roigaard H, Gliemann J, Christensen EI: Epithelial glycoprotein-330 mediates endocytosis of plasminogen activator-plasminogen activator inhibitor type-1 complexes. J Biol Chem. 1993 Aug 5;268(22):16564-70. [PubMed:8344937 ]
  2. Nykjaer A, Petersen CM, Moller B, Jensen PH, Moestrup SK, Holtet TL, Etzerodt M, Thogersen HC, Munch M, Andreasen PA, et al.: Purified alpha 2-macroglobulin receptor/LDL receptor-related protein binds urokinase.plasminogen activator inhibitor type-1 complex. Evidence that the alpha 2-macroglobulin receptor mediates cellular degradation of urokinase receptor-bound complexes. J Biol Chem. 1992 Jul 25;267(21):14543-6. [PubMed:1378833 ]
  3. Hu K, Yang J, Tanaka S, Gonias SL, Mars WM, Liu Y: Tissue-type plasminogen activator acts as a cytokine that triggers intracellular signal transduction and induces matrix metalloproteinase-9 gene expression. J Biol Chem. 2006 Jan 27;281(4):2120-7. Epub 2005 Nov 22. [PubMed:16303771 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on March 14, 2016 09:57