Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T01908
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| Former ID |
TTDC00028
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| Target Name |
Tissue kallikrein
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| Gene Name |
KLK2
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| Synonyms |
Glandular kallikrein; KLK; Kallikrein; hGK; KLK2
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| Target Type |
Discontinued
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| Disease | Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | ||||
| Function |
Glandular kallikreins cleave Met-Lys andArg-Ser bonds in kininogen to release Lys-bradykinin.
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| BioChemical Class |
Peptidase
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| Target Validation |
T01908
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| UniProt ID | |||||
| EC Number |
EC 3.4.21.35
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| Sequence |
MWDLVLSIALSVGCTGAVPLIQSRIVGGWECEKHSQPWQVAVYSHGWAHCGGVLVHPQWV
LTAAHCLKKNSQVWLGRHNLFEPEDTGQRVPVSHSFPHPLYNMSLLKHQSLRPDEDSSHD LMLLRLSEPAKITDVVKVLGLPTQEPALGTTCYASGWGSIEPEEFLRPRSLQCVSLHLLS NDMCARAYSEKVTEFMLCAGLWTGGKDTCGGDSGGPLVCNGVLQGITSWGPEPCALPEKP AVYTKVVHYRKWIKDTIAANP |
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| Structure |
4NFE; 4NFF
|
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| Drugs and Mode of Action | |||||
| Drug(s) | Dermolastin | Drug Info | Discontinued in Phase 2 | Atopic dermatitis | [1] |
| Inhibitor | Dermolastin | Drug Info | [2], [3], [4], [5] | ||
| DM-107 | Drug Info | [6] | |||
| hK2p01 derivative KLK2 inhibitor | Drug Info | [7] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Endocrine and other factor-regulated calcium reabsorption | ||||
| NetPath Pathway | IL2 Signaling Pathway | ||||
| Pathway Interaction Database | Coregulation of Androgen receptor activity | ||||
| Regulation of Androgen receptor activity | |||||
| Reactome | Activation of Matrix Metalloproteinases | ||||
| Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) | |||||
| Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 | |||||
| WikiPathways | Prostate Cancer | ||||
| References | |||||
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071) | ||||
| REF 2 | rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82. | ||||
| REF 3 | Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20. | ||||
| REF 4 | Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34. | ||||
| REF 5 | Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009. | ||||
| REF 6 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2372). | ||||
| REF 7 | Novel peptide inhibitors of human kallikrein 2. J Biol Chem. 2006 May 5;281(18):12555-60. Epub 2006 Mar 9. | ||||
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