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The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3)

Tutkimustuotosvertaisarvioitu

Standard

The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3). / Härkönen, Henna H.; Mattsson, Johanna M.; Määttä, Juha A E; Stenman, Ulf Håkan; Koistinen, Hannu; Matero, Sanni; Windshügel, Björn; Poso, Antti; Lahtela-Kakkonen, Maija.

julkaisussa: CHEMMEDCHEM, Vuosikerta 6, Nro 12, 09.12.2011, s. 2170-2178.

Tutkimustuotosvertaisarvioitu

Harvard

Härkönen, HH, Mattsson, JM, Määttä, JAE, Stenman, UH, Koistinen, H, Matero, S, Windshügel, B, Poso, A & Lahtela-Kakkonen, M 2011, 'The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3)', CHEMMEDCHEM, Vuosikerta. 6, Nro 12, Sivut 2170-2178. https://doi.org/10.1002/cmdc.201100349

APA

Härkönen, H. H., Mattsson, J. M., Määttä, J. A. E., Stenman, U. H., Koistinen, H., Matero, S., ... Lahtela-Kakkonen, M. (2011). The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3). CHEMMEDCHEM, 6(12), 2170-2178. https://doi.org/10.1002/cmdc.201100349

Vancouver

Härkönen HH, Mattsson JM, Määttä JAE, Stenman UH, Koistinen H, Matero S et al. The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3). CHEMMEDCHEM. 2011 joulu 9;6(12):2170-2178. https://doi.org/10.1002/cmdc.201100349

Author

Härkönen, Henna H. ; Mattsson, Johanna M. ; Määttä, Juha A E ; Stenman, Ulf Håkan ; Koistinen, Hannu ; Matero, Sanni ; Windshügel, Björn ; Poso, Antti ; Lahtela-Kakkonen, Maija. / The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3). Julkaisussa: CHEMMEDCHEM. 2011 ; Vuosikerta 6, Nro 12. Sivut 2170-2178.

Bibtex - Lataa

@article{e1141042d0f64341be82a8171da3ace9,
title = "The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3)",
abstract = "Kallikrein-related peptidase3 (KLK3), also known as prostate-specific antigen (PSA), is the most useful biomarker for prostate cancer (PCa). KLK3 is suggested to play a role in regulating cancer growth through anti-angiogenic activity invivo and invitro. This feature, together with its specificity for prostate tissue, makes KLK3 an intriguing target for the design of new therapies for PCa. 3D pharmacophores for KLK3-stimulating compounds were generated based on peptides that bind specifically to KLK3 and increase its enzymatic activity. As a result of pharmacophore-based virtual screening, four small, drug-like compounds with affinity for KLK3 were discovered and validated by capillary differential scanning calorimetry. One of the compounds also stimulated the activity of KLK3, and is therefore the first published small molecule with such an activity. Target specificity: Successful 3D pharmacophore-based virtual screening resulted in the first small, drug-like molecule that stimulates the activity of kallikrein-related peptidase3 (KLK3, PSA). The compound discovered can be applied to the design of novel KLK3-stimulating compounds with the potential to inhibit tumor angiogenesis and progression of prostate cancer.",
keywords = "Angiogenesis, Kallikrein, Molecular modeling, Peptides, Virtual screening",
author = "H{\"a}rk{\"o}nen, {Henna H.} and Mattsson, {Johanna M.} and M{\"a}{\"a}tt{\"a}, {Juha A E} and Stenman, {Ulf H{\aa}kan} and Hannu Koistinen and Sanni Matero and Bj{\"o}rn Windsh{\"u}gel and Antti Poso and Maija Lahtela-Kakkonen",
year = "2011",
month = "12",
day = "9",
doi = "10.1002/cmdc.201100349",
language = "English",
volume = "6",
pages = "2170--2178",
journal = "CHEMMEDCHEM",
issn = "1860-7179",
publisher = "WILEY-V C H VERLAG GMBH",
number = "12",

}

RIS (suitable for import to EndNote) - Lataa

TY - JOUR

T1 - The Discovery of Compounds That Stimulate the Activity of Kallikrein-Related Peptidase3 (KLK3)

AU - Härkönen, Henna H.

AU - Mattsson, Johanna M.

AU - Määttä, Juha A E

AU - Stenman, Ulf Håkan

AU - Koistinen, Hannu

AU - Matero, Sanni

AU - Windshügel, Björn

AU - Poso, Antti

AU - Lahtela-Kakkonen, Maija

PY - 2011/12/9

Y1 - 2011/12/9

N2 - Kallikrein-related peptidase3 (KLK3), also known as prostate-specific antigen (PSA), is the most useful biomarker for prostate cancer (PCa). KLK3 is suggested to play a role in regulating cancer growth through anti-angiogenic activity invivo and invitro. This feature, together with its specificity for prostate tissue, makes KLK3 an intriguing target for the design of new therapies for PCa. 3D pharmacophores for KLK3-stimulating compounds were generated based on peptides that bind specifically to KLK3 and increase its enzymatic activity. As a result of pharmacophore-based virtual screening, four small, drug-like compounds with affinity for KLK3 were discovered and validated by capillary differential scanning calorimetry. One of the compounds also stimulated the activity of KLK3, and is therefore the first published small molecule with such an activity. Target specificity: Successful 3D pharmacophore-based virtual screening resulted in the first small, drug-like molecule that stimulates the activity of kallikrein-related peptidase3 (KLK3, PSA). The compound discovered can be applied to the design of novel KLK3-stimulating compounds with the potential to inhibit tumor angiogenesis and progression of prostate cancer.

AB - Kallikrein-related peptidase3 (KLK3), also known as prostate-specific antigen (PSA), is the most useful biomarker for prostate cancer (PCa). KLK3 is suggested to play a role in regulating cancer growth through anti-angiogenic activity invivo and invitro. This feature, together with its specificity for prostate tissue, makes KLK3 an intriguing target for the design of new therapies for PCa. 3D pharmacophores for KLK3-stimulating compounds were generated based on peptides that bind specifically to KLK3 and increase its enzymatic activity. As a result of pharmacophore-based virtual screening, four small, drug-like compounds with affinity for KLK3 were discovered and validated by capillary differential scanning calorimetry. One of the compounds also stimulated the activity of KLK3, and is therefore the first published small molecule with such an activity. Target specificity: Successful 3D pharmacophore-based virtual screening resulted in the first small, drug-like molecule that stimulates the activity of kallikrein-related peptidase3 (KLK3, PSA). The compound discovered can be applied to the design of novel KLK3-stimulating compounds with the potential to inhibit tumor angiogenesis and progression of prostate cancer.

KW - Angiogenesis

KW - Kallikrein

KW - Molecular modeling

KW - Peptides

KW - Virtual screening

UR - http://www.scopus.com/inward/record.url?scp=82955165662&partnerID=8YFLogxK

U2 - 10.1002/cmdc.201100349

DO - 10.1002/cmdc.201100349

M3 - Article

VL - 6

SP - 2170

EP - 2178

JO - CHEMMEDCHEM

JF - CHEMMEDCHEM

SN - 1860-7179

IS - 12

ER -