Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions

Matthew W. Parker; Craig W. Vander Kooi

doi:10.1016/j.ab.2014.02.017

Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions

Matthew W. Parker
, Craig W. Vander Kooi

Producción científica: Article › revisión exhaustiva

9 Citas (Scopus)

Resumen

Vascular endothelial growth factor-C (VEGF-C) is a secreted growth factor essential for lymphangiogenesis. VEGF-C functions in both physiological and pathological lymphangiogenesis, particularly in tumor metastasis, making it an attractive therapeutic target. Members of two families of cell surface receptors transduce VEGF-C signals: neuropilin-2 (Nrp2) and VEGF-receptor (VEGFR)-2/3. Nrp2 is a promising target for inhibition because it is highly expressed in lymphatic vessels. Here we describe a microplate-based assay for discovery of VEGF-C/Nrp2 inhibitors. We optimize this assay for use in screening an inhibitor library and identify three novel Nrp2/VEGF-C binding inhibitors from the National Institutes of Health (NIH) Clinical Collection small molecule library.

Idioma original	English
Páginas (desde-hasta)	4-6
Número de páginas	3
Publicación	Analytical Biochemistry
Volumen	453
N.º	1
DOI	https://doi.org/10.1016/j.ab.2014.02.017
Estado	Published - may 15 2014

Nota bibliográfica

Funding Information:
This work was supported by National Institutes of Health (NIH) grants R01GM094155 (C.W.V.K.) and T32HL072743 (M.W.P.).

Financiación

This work was supported by National Institutes of Health (NIH) grants R01GM094155 (C.W.V.K.) and T32HL072743 (M.W.P.).

Financiadores	Número del financiador
National Institutes of Health (NIH)	R01GM094155
National Heart, Lung, and Blood Institute (NHLBI)	T32HL072743

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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10.1016/j.ab.2014.02.017

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title = "Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions",

abstract = "Vascular endothelial growth factor-C (VEGF-C) is a secreted growth factor essential for lymphangiogenesis. VEGF-C functions in both physiological and pathological lymphangiogenesis, particularly in tumor metastasis, making it an attractive therapeutic target. Members of two families of cell surface receptors transduce VEGF-C signals: neuropilin-2 (Nrp2) and VEGF-receptor (VEGFR)-2/3. Nrp2 is a promising target for inhibition because it is highly expressed in lymphatic vessels. Here we describe a microplate-based assay for discovery of VEGF-C/Nrp2 inhibitors. We optimize this assay for use in screening an inhibitor library and identify three novel Nrp2/VEGF-C binding inhibitors from the National Institutes of Health (NIH) Clinical Collection small molecule library.",

keywords = "Assay, Inhibitor, Ligand, Neuropilin, Receptor, VEGF",

author = "Parker, \{Matthew W.\} and \{Vander Kooi\}, \{Craig W.\}",

note = "Funding Information: This work was supported by National Institutes of Health (NIH) grants R01GM094155 (C.W.V.K.) and T32HL072743 (M.W.P.). ",

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T1 - Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions

AU - Parker, Matthew W.

AU - Vander Kooi, Craig W.

N1 - Funding Information: This work was supported by National Institutes of Health (NIH) grants R01GM094155 (C.W.V.K.) and T32HL072743 (M.W.P.).

PY - 2014/5/15

Y1 - 2014/5/15

N2 - Vascular endothelial growth factor-C (VEGF-C) is a secreted growth factor essential for lymphangiogenesis. VEGF-C functions in both physiological and pathological lymphangiogenesis, particularly in tumor metastasis, making it an attractive therapeutic target. Members of two families of cell surface receptors transduce VEGF-C signals: neuropilin-2 (Nrp2) and VEGF-receptor (VEGFR)-2/3. Nrp2 is a promising target for inhibition because it is highly expressed in lymphatic vessels. Here we describe a microplate-based assay for discovery of VEGF-C/Nrp2 inhibitors. We optimize this assay for use in screening an inhibitor library and identify three novel Nrp2/VEGF-C binding inhibitors from the National Institutes of Health (NIH) Clinical Collection small molecule library.

AB - Vascular endothelial growth factor-C (VEGF-C) is a secreted growth factor essential for lymphangiogenesis. VEGF-C functions in both physiological and pathological lymphangiogenesis, particularly in tumor metastasis, making it an attractive therapeutic target. Members of two families of cell surface receptors transduce VEGF-C signals: neuropilin-2 (Nrp2) and VEGF-receptor (VEGFR)-2/3. Nrp2 is a promising target for inhibition because it is highly expressed in lymphatic vessels. Here we describe a microplate-based assay for discovery of VEGF-C/Nrp2 inhibitors. We optimize this assay for use in screening an inhibitor library and identify three novel Nrp2/VEGF-C binding inhibitors from the National Institutes of Health (NIH) Clinical Collection small molecule library.

KW - Assay

KW - Inhibitor

KW - Ligand

KW - Neuropilin

KW - Receptor

KW - VEGF

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DO - 10.1016/j.ab.2014.02.017

M3 - Article

C2 - 24583243

AN - SCOPUS:84896973250

SN - 0003-2697

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JO - Analytical Biochemistry

JF - Analytical Biochemistry

IS - 1

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Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions

Resumen

Nota bibliográfica

Financiación

ASJC Scopus subject areas

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