peptide KLK2b(c1)

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Ligands
peptide KLK2b(c1)

GtoPdb Ligand ID: 8484

Compound class: Peptide or derivative

Comment: Peptide KLK2b(c1) is a selective inhibitor of glandular kallikrein (KLK2) [4], a testis-specific serine protease. KLK2 inhibitors are being investigated as novel therapeutics to prevent the metastasis of prostate cancer [1-3,5-7].

References
1. Avgeris M, Mavridis K, Scorilas A. (2012) Kallikrein-related peptidases in prostate, breast, and ovarian cancers: from pathobiology to clinical relevance. Biol Chem, 393 (5): 301-17. [PMID:22505514]
2. Koistinen H, Hekim C, Wu P, Närvänen A, Stenman UH. (2014) Evaluation of peptides as protease inhibitors and stimulators. Methods Mol Biol, 1088: 147-58. [PMID:24146402]
3. Koistinen H, Närvänen A, Pakkala M, Hekim C, Mattsson JM, Zhu L, Laakkonen P, Stenman UH. (2008) Development of peptides specifically modulating the activity of KLK2 and KLK3. Biol Chem, 389 (6): 633-42. [PMID:18627344]
4. Pakkala M, Hekim C, Soininen P, Leinonen J, Koistinen H, Weisell J, Stenman UH, Vepsäläinen J, Närvänen A. (2007) Activity and stability of human kallikrein-2-specific linear and cyclic peptide inhibitors. J Pept Sci, 13 (5): 348-53. [PMID:17436344]
5. Satkunasivam R, Zhang W, Trachtenberg J, Toi A, Yu C, Diamandis E, Kattan MW, Narod SA, Nam RK. (2014) Human kallikrein-2 gene and protein expression predicts prostate cancer at repeat biopsy. Springerplus, 3: 295. [PMID:25279276]
6. Whitbread AK, Veveris-Lowe TL, Lawrence MG, Nicol DL, Clements JA. (2006) The role of kallikrein-related peptidases in prostate cancer: potential involvement in an epithelial to mesenchymal transition. Biol Chem, 387 (6): 707-14. [PMID:16800731]
7. Williams SA, Xu Y, De Marzo AM, Isaacs JT, Denmeade SR. (2010) Prostate-specific antigen (PSA) is activated by KLK2 in prostate cancer ex vivo models and in prostate-targeted PSA/KLK2 double transgenic mice. Prostate, 70 (7): 788-96. [PMID:20058238]

References

1. Avgeris M, Mavridis K, Scorilas A. (2012)
Kallikrein-related peptidases in prostate, breast, and ovarian cancers: from pathobiology to clinical relevance.
Biol Chem, 393 (5): 301-17. [PMID:22505514]

2. Koistinen H, Hekim C, Wu P, Närvänen A, Stenman UH. (2014)
Evaluation of peptides as protease inhibitors and stimulators.
Methods Mol Biol, 1088: 147-58. [PMID:24146402]

3. Koistinen H, Närvänen A, Pakkala M, Hekim C, Mattsson JM, Zhu L, Laakkonen P, Stenman UH. (2008)
Development of peptides specifically modulating the activity of KLK2 and KLK3.
Biol Chem, 389 (6): 633-42. [PMID:18627344]

4. Pakkala M, Hekim C, Soininen P, Leinonen J, Koistinen H, Weisell J, Stenman UH, Vepsäläinen J, Närvänen A. (2007)
Activity and stability of human kallikrein-2-specific linear and cyclic peptide inhibitors.
J Pept Sci, 13 (5): 348-53. [PMID:17436344]

5. Satkunasivam R, Zhang W, Trachtenberg J, Toi A, Yu C, Diamandis E, Kattan MW, Narod SA, Nam RK. (2014)
Human kallikrein-2 gene and protein expression predicts prostate cancer at repeat biopsy.
Springerplus, 3: 295. [PMID:25279276]

6. Whitbread AK, Veveris-Lowe TL, Lawrence MG, Nicol DL, Clements JA. (2006)
The role of kallikrein-related peptidases in prostate cancer: potential involvement in an epithelial to mesenchymal transition.
Biol Chem, 387 (6): 707-14. [PMID:16800731]

7. Williams SA, Xu Y, De Marzo AM, Isaacs JT, Denmeade SR. (2010)
Prostate-specific antigen (PSA) is activated by KLK2 in prostate cancer ex vivo models and in prostate-targeted PSA/KLK2 double transgenic mice.
Prostate, 70 (7): 788-96. [PMID:20058238]