Target Information

Target General Infomation
Target ID
T01908
Former ID
TTDC00028
Target Name
Tissue kallikrein
Gene Name
KLK2
Synonyms
Glandular kallikrein; KLK; Kallikrein; hGK; KLK2
Target Type
Discontinued
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.
BioChemical Class
Peptidase
Target Validation
T01908
UniProt ID
P20151
EC Number
EC 3.4.21.35
Sequence
MWDLVLSIALSVGCTGAVPLIQSRIVGGWECEKHSQPWQVAVYSHGWAHCGGVLVHPQWV
LTAAHCLKKNSQVWLGRHNLFEPEDTGQRVPVSHSFPHPLYNMSLLKHQSLRPDEDSSHD
LMLLRLSEPAKITDVVKVLGLPTQEPALGTTCYASGWGSIEPEEFLRPRSLQCVSLHLLS
NDMCARAYSEKVTEFMLCAGLWTGGKDTCGGDSGGPLVCNGVLQGITSWGPEPCALPEKP
AVYTKVVHYRKWIKDTIAANP
Structure
4NFE; 4NFF
Drugs and Mode of Action
Drug(s) Dermolastin Drug Info Discontinued in Phase 2 Atopic dermatitis [547642]
Inhibitor Dermolastin Drug Info [536190], [536840], [537435], [551533]
DM-107 Drug Info [543612]
hK2p01 derivative KLK2 inhibitor Drug Info [528079]
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 547642Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071)
Ref 528079Novel peptide inhibitors of human kallikrein 2. J Biol Chem. 2006 May 5;281(18):12555-60. Epub 2006 Mar 9.
Ref 536190rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82.
Ref 536840Bioreactor 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 537435Optimization 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 543612(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 551533Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.

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