Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T97141
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| Former ID |
TTDR00794
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| Target Name |
Myosin light chain kinase, smooth muscle and non-muscle isozymes
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| Gene Name |
MYLK
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| Synonyms |
210,000 molecular weight myosin light chain kinase; EC mlck; Endothelial cell (EC) MLCK isoform; MLCK; MLCK210; MYLK
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| Target Type |
Clinical Trial
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| Disease | Duodenal ulcers [ICD10: K25-K27] | ||||
| Function |
Calcium/calmodulin-dependent enzyme responsible for smooth muscle contraction via phosphorylation of a specific serine in the n-terminus of myosin light chains (mlc), an event that facilitates myosin interaction with actin filaments.
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| BioChemical Class |
Kinase
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.18
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| Sequence |
MGDVKLVASSHISKTSLSVDPSRVDSMPLTEAPAFILPPRNLCIKEGATAKFEGRVRGYP
EPQVTWHRNGQPITSGGRFLLDCGIRGTFSLVIHAVHEEDRGKYTCEATNGSGARQVTVE LTVEGSFAKQLGQPVVSKTLGDRFSAPAVETRPSIWGECPPKFATKLGRVVVKEGQMGRF SCKITGRPQPQVTWLKGNVPLQPSARVSVSEKNGMQVLEIHGVNQDDVGVYTCLVVNGSG KASMSAELSIQGLDSANRSFVRETKATNSDVRKEVTNVISKESKLDSLEAAAKSKNCSSP QRGGSPPWAANSQPQPPRESKLESCKDSPRTAPQTPVLQKTSSSITLQAARVQPEPRAPG LGVLSPSGEERKRPAPPRPATFPTRQPGLGSQDVVSKAANRRIPMEGQRDSAFPKFESKP QSQEVKENQTVKFRCEVSGIPKPEVAWFLEGTPVRRQEGSIEVYEDAGSHYLCLLKARTR DSGTYSCTASNAQGQLSCSWTLQVERLAVMEVAPSFSSVLKDCAVIEGQDFVLQCSVRGT PVPRITWLLNGQPIQYARSTCEAGVAELHIQDALPEDHGTYTCLAENALGQVSCSAWVTV HEKKSSRKSEYLLPVAPSKPTAPIFLQGLSDLKVMDGSQVTMTVQVSGNPPPEVIWLHNG NEIQESEDFHFEQRGTQHSLCIQEVFPEDTGTYTCEAWNSAGEVRTQAVLTVQEPHDGTQ PWFISKPRSVTASLGQSVLISCAIAGDPFPTVHWLRDGKALCKDTGHFEVLQNEDVFTLV LKKVQPWHAGQYEILLKNRVGECSCQVSLMLQNSSARALPRGREPASCEDLCGGGVGADG GGSDRYGSLRPGWPARGQGWLEEEDGEDVRGVLKRRVETRQHTEEAIRQQEVEQLDFRDL LGKKVSTKTLSEDDLKEIPAEQMDFRANLQRQVKPKTVSEEERKVHSPQQVDFRSVLAKK GTSKTPVPEKVPPPKPATPDFRSVLGGKKKLPAENGSSSAETLNAKAVESSKPLSNAQPS GPLKPVGNAKPAETLKPMGNAKPAETLKPMGNAKPDENLKSASKEELKKDVKNDVNCKRG HAGTTDNEKRSESQGTAPAFKQKLQDVHVAEGKKLLLQCQVSSDPPATIIWTLNGKTLKT TKFIILSQEGSLCSVSIEKALPEDRGLYKCVAKNDAGQAECSCQVTVDDAPASENTKAPE MKSRRPKSSLPPVLGTESDATVKKKPAPKTPPKAAMPPQIIQFPEDQKVRAGESVELFGK VTGTQPITCTWMKFRKQIQESEHMKVENSENGSKLTILAARQEHCGCYTLLVENKLGSRQ AQVNLTVVDKPDPPAGTPCASDIRSSSLTLSWYGSSYDGGSAVQSYSIEIWDSANKTWKE LATCRSTSFNVQDLLPDHEYKFRVRAINVYGTSEPSQESELTTVGEKPEEPKDEVEVSDD DEKEPEVDYRTVTINTEQKVSDFYDIEERLGSGKFGQVFRLVEKKTRKVWAGKFFKAYSA KEKENIRQEISIMNCLHHPKLVQCVDAFEEKANIVMVLEIVSGGELFERIIDEDFELTER ECIKYMRQISEGVEYIHKQGIVHLDLKPENIMCVNKTGTRIKLIDFGLARRLENAGSLKV LFGTPEFVAPEVINYEPIGYATDMWSIGVICYILVSGLSPFMGDNDNETLANVTSATWDF DDEAFDEISDDAKDFISNLLKKDMKNRLDCTQCLQHPWLMKDTKNMEAKKLSKDRMKKYM ARRKWQKTGNAVRAIGRLSSMAMISGLSGRKSSTGSPTSPLNAEKLESEEDVSQAFLEAV AEEKPHVKPYFSKTIRDLEVVEGSAARFDCKIEGYPDPEVVWFKDDQSIRESRHFQIDYD EDGNCSLIISDVCGDDDAKYTCKAVNSLGEATCTAELIVETMEEGEGEGEEEEE |
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| Drugs and Mode of Action | |||||
| Drug(s) | ME-3407 | Drug Info | Phase 2 | Duodenal ulcers | [1] |
| Inhibitor | ME-3407 | Drug Info | [1] | ||
| RKI-1447 | Drug Info | [2] | |||
| Pathways | |||||
| KEGG Pathway | Calcium signaling pathway | ||||
| cGMP-PKG signaling pathway | |||||
| Vascular smooth muscle contraction | |||||
| Focal adhesion | |||||
| Platelet activation | |||||
| Regulation of actin cytoskeleton | |||||
| Oxytocin signaling pathway | |||||
| Gastric acid secretion | |||||
| PANTHER Pathway | Cytoskeletal regulation by Rho GTPase | ||||
| Inflammation mediated by chemokine and cytokine signaling pathway | |||||
| Pathway Interaction Database | Aurora B signaling | ||||
| PathWhiz Pathway | Intracellular Signalling Through Prostacyclin Receptor and Prostacyclin | ||||
| Muscle/Heart Contraction | |||||
| Reactome | Smooth Muscle Contraction | ||||
| WikiPathways | Regulation of Actin Cytoskeleton | ||||
| Focal Adhesion | |||||
| Endothelin Pathways | |||||
| Muscle contraction | |||||
| MicroRNAs in cardiomyocyte hypertrophy | |||||
| References | |||||
| REF 1 | ME-3407, a new antiulcer agent, inhibits acid secretion by interfering with redistribution of H(+)-K(+)-ATPase. Am J Physiol. 1997 May;272(5 Pt 1):G1122-34. | ||||
| REF 2 | Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun 1;3(6):699-709. Epub 2012 Jan 27. | ||||
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