Kallikrein-1

KLK1
Identifiers
Aliases	KLK1, KLKR, Klk6, hK1, kallikrein 1
External IDs	OMIM: 147910; MGI: 102850; GeneCards: KLK1
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 1SPJ
Enzyme activity EC # BRENDA ExPASy KEGG MetaCyc 3.4.21.35 ↗ ↗ ↗ ↗
Gene location (Human) Chr. Chromosome 19 (human) Band 19q13.33 Start 50,819,146 bp End 50,823,787 bp
Gene location (Mouse) Chr. Chromosome 7 (mouse) Band 7 B3|7 28.74 cM Start 43,874,784 bp End 43,879,042 bp
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in body of pancreas mucosa of transverse colon parotid gland rectum skin of abdomen islet of Langerhans skin of leg beta cell skin of arm gonad Top expressed in submandibular gland parotid gland right kidney left colon human kidney pyloric antrum lacrimal gland crypt of lieberkuhn of small intestine duodenum islet of Langerhans More reference expression data BioGPS More reference expression data
Gene ontology Molecular function peptidase activity serine-type peptidase activity serine-type endopeptidase activity hydrolase activity Cellular component extracellular exosome nucleus secretory granule Biological process proteolysis regulation of systemic arterial blood pressure zymogen activation Sources:Amigo / QuickGO
Orthologs Databases NCBI: entry; OMA: entry Species Human Mouse Entrez 3816 16612 Ensembl ENSG00000167748 ENSMUSG00000063903 UniProt P06870 P15947 RefSeq (mRNA) NM_002257 NM_010639 NM_001320331 NM_001320332 RefSeq (protein) NP_002248 NP_001307260 NP_001307261 NP_034769 Location (UCSC) Chr 19: 50.82 – 50.82 Mb Chr 7: 43.87 – 43.88 Mb PubMed search
Wikidata
View/Edit Human View/Edit Mouse

Kallikrein-1, also called tissue kallikrein, is an protein that in humans is encoded by the KLK1 gene. This enzyme acts on kininogen to produce Lys-bradykinin as part of the kinin–kallikrein system.

Kallikreins are a subgroup of serine proteases having diverse physiological functions. Growing evidence suggests that many kallikreins are implicated in carcinogenesis and some have potential as novel cancer and other disease biomarkers. This gene is one of the fifteen kallikrein subfamily members located in a cluster on chromosome 19. This protein is functionally conserved in its capacity to release the vasoactive peptide, Lys-bradykinin, from low molecular weight kininogen.

Medical significance

A recombinant form of kallikrein-1, designated as DM199, is being tested as an experimental drug that acts on the kallikrein-kinin system and is developed for diabetes.

See also

• Kininogen 1

Further reading

• Clements J, Hooper J, Dong Y, Harvey T (January 2001). "The expanded human kallikrein (KLK) gene family: genomic organisation, tissue-specific expression and potential functions". Biological Chemistry. 382 (1): 5–14. doi:10.1515/BC.2001.002. PMID 11258672. S2CID 5864448.
• Lottspeich F, Geiger R, Henschen A, Kutzbach C (December 1979). "N-Terminal amino acid sequence of human urinary kallikrein homology with other serine proteases". Hoppe-Seyler's Zeitschrift für Physiologische Chemie. 360 (12): 1947–1950. PMID 393608.
• Riegman PH, Vlietstra RJ, Suurmeijer L, Cleutjens CB, Trapman J (September 1992). "Characterization of the human kallikrein locus". Genomics. 14 (1): 6–11. doi:10.1016/S0888-7543(05)80275-7. PMID 1385301.
• Henttu P, Lukkarinen O, Vihko P (April 1990). "Expression of the gene coding for human prostate-specific antigen and related hGK-1 in benign and malignant tumors of the human prostate". International Journal of Cancer. 45 (4): 654–660. doi:10.1002/ijc.2910450414. PMID 1691151. S2CID 33875411.
• Qin H, Kemp J, Yip MY, Lam-Po-Tang PR, Morris BJ (1992). "Localization of human glandular kallikrein-1 gene to chromosome 19q13.3-13.4 by in situ hybridization". Human Heredity. 41 (4): 222–226. doi:10.1159/000154005. PMID 1783409.
• Lu HS, Lin FK, Chao L, Chao J (April 1989). "Human urinary kallikrein. Complete amino acid sequence and sites of glycosylation". International Journal of Peptide and Protein Research. 33 (4): 237–249. doi:10.1111/j.1399-3011.1989.tb01277.x. PMID 2666327.
• Angermann A, Bergmann C, Appelhans H (September 1989). "Cloning and expression of human salivary-gland kallikrein in Escherichia coli". The Biochemical Journal. 262 (3): 787–793. doi:10.1042/bj2620787. PMC 1133342. PMID 2686621.
• Evans BA, Yun ZX, Close JA, Tregear GW, Kitamura N, Nakanishi S, et al. (May 1988). "Structure and chromosomal localization of the human renal kallikrein gene". Biochemistry. 27 (9): 3124–3129. doi:10.1021/bi00409a003. PMID 2898948.
• Fukushima D, Kitamura N, Nakanishi S (December 1985). "Nucleotide sequence of cloned cDNA for human pancreatic kallikrein". Biochemistry. 24 (27): 8037–8043. doi:10.1021/bi00348a030. PMID 3004571.
• Kellermann J, Lottspeich F, Geiger R, Deutzmann R (February 1988). "Human urinary kallikrein--amino acid sequence and carbohydrate attachment sites". Protein Sequences & Data Analysis. 1 (3): 177–182. PMID 3163150.
• Takahashi S, Irie A, Katayama Y, Ito K, Miyake Y (March 1986). "N-terminal amino acid sequence of human urinary prokallikrein". Journal of Biochemistry. 99 (3): 989–992. doi:10.1093/oxfordjournals.jbchem.a135563. PMID 3635530.
• Baker AR, Shine J (December 1985). "Human kidney kallikrein: cDNA cloning and sequence analysis". DNA. 4 (6): 445–450. doi:10.1089/dna.1985.4.445. PMID 3853975.
• Del Nery E, Chagas JR, Juliano MA, Prado ES, Juliano L (November 1995). "Evaluation of the extent of the binding site in human tissue kallikrein by synthetic substrates with sequences of human kininogen fragments". The Biochemical Journal. 312 (Pt 1): 233–238. doi:10.1042/bj3120233. PMC 1136249. PMID 7492318.
• Chen LM, Richards GP, Chao L, Chao J (April 1995). "Molecular cloning, purification and in situ localization of human colon kallikrein". The Biochemical Journal. 307 (Pt 2): 481–486. doi:10.1042/bj3070481. PMC 1136673. PMID 7733886.
• Clements J, Mukhtar A, Ehrlich A, Yap B (August 1994). "Glandular kallikrein gene expression in the human uterus". Brazilian Journal of Medical and Biological Research = Revista Brasileira de Pesquisas Medicas e Biologicas. 27 (8): 1855–1863. PMID 7749374.
• Lin FK, Lin CH, Chou CC, Chen K, Lu HS, Bacheller W, et al. (June 1993). "Molecular cloning and sequence analysis of the monkey and human tissue kallikrein genes". Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression. 1173 (3): 325–328. doi:10.1016/0167-4781(93)90131-v. PMID 7916636.
• Gomes RA, Juliano L, Chagas JR, Hial V (June 1997). "Characterization of kininogenase activity of an acidic proteinase isolated from human kidney". Canadian Journal of Physiology and Pharmacology. 75 (6): 757–761. doi:10.1139/cjpp-75-6-757. PMID 9276160.
• Bourgeois L, Brillard-Bourdet M, Deperthes D, Juliano MA, Juliano L, Tremblay RR, et al. (November 1997). "Serpin-derived peptide substrates for investigating the substrate specificity of human tissue kallikreins hK1 and hK2". The Journal of Biological Chemistry. 272 (47): 29590–29595. doi:10.1074/jbc.272.47.29590. PMID 9368023.
• Chen VC, Chao L, Chao J (June 2000). "Reactive-site specificity of human kallistatin toward tissue kallikrein probed by site-directed mutagenesis". Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology. 1479 (1–2): 237–246. doi:10.1016/S0167-4838(00)00044-3. PMID 10862973.

External links

• The MEROPS online database for peptidases and their inhibitors: S01.160