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small molecular inhibitors against vap-1  (Astellas)

 
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    Astellas small molecular inhibitors against vap-1
    Crystallographic structure of <t>VAP-1</t> . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.
    Small Molecular Inhibitors Against Vap 1, supplied by Astellas, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/small molecular inhibitors against vap-1/product/Astellas
    Average 90 stars, based on 1 article reviews
    small molecular inhibitors against vap-1 - by Bioz Stars, 2026-02
    90/100 stars

    Images

    1) Product Images from "Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation"

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    Journal: Antioxidants & Redox Signaling

    doi: 10.1089/ars.2017.7418

    Crystallographic structure of VAP-1 . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.
    Figure Legend Snippet: Crystallographic structure of VAP-1 . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.

    Techniques Used: Binding Assay

    VAP-1 is expressed in vascular endothelium and smooth muscle in human liver and tonsil. Triple stainings using anti-VAP-1, anti-smooth muscle actin (SMA), and anti-CD31 (pan-endothelial antibodies) are shown. Note that liver sinusoids ( arrowheads ) stain brightly with anti-VAP-1 but are devoid of smooth muscle present in larger vessels. Similarly, smaller capillaries are VAP-1/CD31 positive but lack SMA in tonsil ( arrows ).
    Figure Legend Snippet: VAP-1 is expressed in vascular endothelium and smooth muscle in human liver and tonsil. Triple stainings using anti-VAP-1, anti-smooth muscle actin (SMA), and anti-CD31 (pan-endothelial antibodies) are shown. Note that liver sinusoids ( arrowheads ) stain brightly with anti-VAP-1 but are devoid of smooth muscle present in larger vessels. Similarly, smaller capillaries are VAP-1/CD31 positive but lack SMA in tonsil ( arrows ).

    Techniques Used: Staining

    Functions of VAP-1 in health and disease. VAP-1 has multiple different physiological functions ( blue boxes ), and it is involved in their aberrations during different disease states ( yellow boxes ). Many of these processes are interdependent, and the role of VAP-1 in leukocyte extravasation is likely to contribute heavily to many of them.
    Figure Legend Snippet: Functions of VAP-1 in health and disease. VAP-1 has multiple different physiological functions ( blue boxes ), and it is involved in their aberrations during different disease states ( yellow boxes ). Many of these processes are interdependent, and the role of VAP-1 in leukocyte extravasation is likely to contribute heavily to many of them.

    Techniques Used:

    A working model for VAP-1 function in the leukocyte extravasation cascade. A blood-borne leukocyte makes sequential contacts with the endothelial cell expressing VAP-1. When the two cell types (STEP 1) come in contact with each other (STEP 2) , a leukocyte counter-receptor of VAP-1 interacts in an enzyme activity-independent manner with the endothelial VAP-1. Thereafter, the same (or another) leukocyte surface molecule is used as a substrate in the VAP-1-mediated oxidative deamination reaction (STEP 3) . This results in the formation of a covalent but transient binding between the two cell types. After the catalytic reaction, the leukocyte surface molecule is modified into an aldehyde, a signaling molecule hydrogen peroxide is formed, and VAP-1 enzyme is converted back to the original state (STEP 4) . Note that the order of the proposed STEPs 2 and 3 is hypothetical.
    Figure Legend Snippet: A working model for VAP-1 function in the leukocyte extravasation cascade. A blood-borne leukocyte makes sequential contacts with the endothelial cell expressing VAP-1. When the two cell types (STEP 1) come in contact with each other (STEP 2) , a leukocyte counter-receptor of VAP-1 interacts in an enzyme activity-independent manner with the endothelial VAP-1. Thereafter, the same (or another) leukocyte surface molecule is used as a substrate in the VAP-1-mediated oxidative deamination reaction (STEP 3) . This results in the formation of a covalent but transient binding between the two cell types. After the catalytic reaction, the leukocyte surface molecule is modified into an aldehyde, a signaling molecule hydrogen peroxide is formed, and VAP-1 enzyme is converted back to the original state (STEP 4) . Note that the order of the proposed STEPs 2 and 3 is hypothetical.

    Techniques Used: Expressing, Activity Assay, Binding Assay, Modification


    Figure Legend Snippet: Selected Small-Molecule Vascular Adhesion Protein-1 Inhibitors

    Techniques Used:


    Figure Legend Snippet: Preclinical Models of Vascular Adhesion Protein-1 Targeting

    Techniques Used: Transmigration Assay, Infection, Western Blot


    Figure Legend Snippet: Soluble Vascular Adhesion Protein-1 Levels in Different Human Diseases

    Techniques Used: Activity Assay, Magnetic Resonance Imaging, Transplantation Assay

    VAP-1 can be used as a target for imaging. Representative sagittal ( left ), transaxial ( middle ), and coronal ( right ) multiplane PET images of [ 18 F]FDR-Siglec-9 (VAP-1 ligand) biodistribution in a rat. The images are summation from 10 to 60 min postinjection. Reproduced with permission from Chemical Communication [from Li et al. ].
    Figure Legend Snippet: VAP-1 can be used as a target for imaging. Representative sagittal ( left ), transaxial ( middle ), and coronal ( right ) multiplane PET images of [ 18 F]FDR-Siglec-9 (VAP-1 ligand) biodistribution in a rat. The images are summation from 10 to 60 min postinjection. Reproduced with permission from Chemical Communication [from Li et al. ].

    Techniques Used: Imaging



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    small molecular inhibitors against vap-1  (Astellas)
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    Astellas small molecular inhibitors against vap-1
    Crystallographic structure of <t>VAP-1</t> . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.
    Small Molecular Inhibitors Against Vap 1, supplied by Astellas, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/small molecular inhibitors against vap-1/product/Astellas
    Average 90 stars, based on 1 article reviews
    small molecular inhibitors against vap-1 - by Bioz Stars, 2026-02
    90/100 stars
    		  Buy from Supplier

    Image Search Results


    Crystallographic structure of VAP-1 . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: Crystallographic structure of VAP-1 . (A) Two identical monomers are colored blue and wheat . Copper (Cu) ion is orange and TPQ in each chain is presented as green spheres . (B) Docking of Siglec-9 peptide ( green ) into the active site of VAP-1. This binding mode is presented in Aalto et al. and assumes that the peptide binds covalently to TPQ. Courtesy of Dr. Tiina Salminen. Siglec, sialic acid-binding immunoglobulin-type lectins; TPQ, topaquinone; VAP-1, vascular adhesion protein-1.

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques: Binding Assay

    VAP-1 is expressed in vascular endothelium and smooth muscle in human liver and tonsil. Triple stainings using anti-VAP-1, anti-smooth muscle actin (SMA), and anti-CD31 (pan-endothelial antibodies) are shown. Note that liver sinusoids ( arrowheads ) stain brightly with anti-VAP-1 but are devoid of smooth muscle present in larger vessels. Similarly, smaller capillaries are VAP-1/CD31 positive but lack SMA in tonsil ( arrows ).

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: VAP-1 is expressed in vascular endothelium and smooth muscle in human liver and tonsil. Triple stainings using anti-VAP-1, anti-smooth muscle actin (SMA), and anti-CD31 (pan-endothelial antibodies) are shown. Note that liver sinusoids ( arrowheads ) stain brightly with anti-VAP-1 but are devoid of smooth muscle present in larger vessels. Similarly, smaller capillaries are VAP-1/CD31 positive but lack SMA in tonsil ( arrows ).

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques: Staining

    Functions of VAP-1 in health and disease. VAP-1 has multiple different physiological functions ( blue boxes ), and it is involved in their aberrations during different disease states ( yellow boxes ). Many of these processes are interdependent, and the role of VAP-1 in leukocyte extravasation is likely to contribute heavily to many of them.

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: Functions of VAP-1 in health and disease. VAP-1 has multiple different physiological functions ( blue boxes ), and it is involved in their aberrations during different disease states ( yellow boxes ). Many of these processes are interdependent, and the role of VAP-1 in leukocyte extravasation is likely to contribute heavily to many of them.

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques:

    A working model for VAP-1 function in the leukocyte extravasation cascade. A blood-borne leukocyte makes sequential contacts with the endothelial cell expressing VAP-1. When the two cell types (STEP 1) come in contact with each other (STEP 2) , a leukocyte counter-receptor of VAP-1 interacts in an enzyme activity-independent manner with the endothelial VAP-1. Thereafter, the same (or another) leukocyte surface molecule is used as a substrate in the VAP-1-mediated oxidative deamination reaction (STEP 3) . This results in the formation of a covalent but transient binding between the two cell types. After the catalytic reaction, the leukocyte surface molecule is modified into an aldehyde, a signaling molecule hydrogen peroxide is formed, and VAP-1 enzyme is converted back to the original state (STEP 4) . Note that the order of the proposed STEPs 2 and 3 is hypothetical.

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: A working model for VAP-1 function in the leukocyte extravasation cascade. A blood-borne leukocyte makes sequential contacts with the endothelial cell expressing VAP-1. When the two cell types (STEP 1) come in contact with each other (STEP 2) , a leukocyte counter-receptor of VAP-1 interacts in an enzyme activity-independent manner with the endothelial VAP-1. Thereafter, the same (or another) leukocyte surface molecule is used as a substrate in the VAP-1-mediated oxidative deamination reaction (STEP 3) . This results in the formation of a covalent but transient binding between the two cell types. After the catalytic reaction, the leukocyte surface molecule is modified into an aldehyde, a signaling molecule hydrogen peroxide is formed, and VAP-1 enzyme is converted back to the original state (STEP 4) . Note that the order of the proposed STEPs 2 and 3 is hypothetical.

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques: Expressing, Activity Assay, Binding Assay, Modification

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: Selected Small-Molecule Vascular Adhesion Protein-1 Inhibitors

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques:

    VAP-1 can be used as a target for imaging. Representative sagittal ( left ), transaxial ( middle ), and coronal ( right ) multiplane PET images of [ 18 F]FDR-Siglec-9 (VAP-1 ligand) biodistribution in a rat. The images are summation from 10 to 60 min postinjection. Reproduced with permission from Chemical Communication [from Li et al. ].

    Journal: Antioxidants & Redox Signaling

    Article Title: Vascular Adhesion Protein-1: A Cell Surface Amine Oxidase in Translation

    doi: 10.1089/ars.2017.7418

    Figure Lengend Snippet: VAP-1 can be used as a target for imaging. Representative sagittal ( left ), transaxial ( middle ), and coronal ( right ) multiplane PET images of [ 18 F]FDR-Siglec-9 (VAP-1 ligand) biodistribution in a rat. The images are summation from 10 to 60 min postinjection. Reproduced with permission from Chemical Communication [from Li et al. ].

    Article Snippet: Astellas, Pharmaxis, and Promaxigen have developed small molecular inhibitors against VAP-1.

    Techniques: Imaging