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2-Arylindole-3-acetamides: FPP-Competitive inhibitors of farnesyl protein transferase
A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative m...
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| Published in: | Bioorganic & medicinal chemistry letters 2001-04, Vol.11 (7), p.865-869 |
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| Main Authors: | , , , , , , , , , , , , , , , , |
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| Language: | English |
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| container_end_page | 869 |
| container_issue | 7 |
| container_start_page | 865 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 11 |
| creator | Trotter, B.Wesley Quigley, Amy G. Lumma, William C. Sisko, John T. Walsh, Eileen S. Hamann, Christian S. Robinson, Ronald G. Bhimnathwala, Hema Kolodin, D.Garrett Zheng, Wei Buser, Carolyn A. Huber, Hans E. Lobell, Robert B. Kohl, Nancy E. Williams, Theresa M. Graham, Samuel L. Dinsmore, Christopher J. |
| description | A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed.
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| doi_str_mv | 10.1016/S0960-894X(01)00061-0 |
| format | article |
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Drug treatments</subject><subject>Protein Prenylation - drug effects</subject><subject>Protein Prenylation - physiology</subject><subject>ras Proteins - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Tumor Cells, Cultured</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><recordid>eNo90VtLHTEQB_BQlHq0_QgtC4LoQ-zkssnGF5GDNxAq1ELfQnYzoSl7OU1yhPPt3aNHn-blN8PM_An5xuCcAVM_foFRQBsj_5wCOwMAxSh8IgsmlaRCQr1HFh_kgBzm_A-ASZDyMzlgjBsptFmQ35xepU0fRz_1SAV1HRY3RI_5orp5fKTLaVhhiSU-YxXHv7GNZUq5mkIVXBoxb_pqlaaCcaxKcmMOmFzGL2Q_uD7j1109Ik8310_LO_rw8_Z-efVAkRtWKArtpectazFoJdpOmVpIXjvkWBsuZe21YpwFb1yrdFM3ug1mbgmB60aLI3LyNnZe4f8ac7FDzB32vRtxWmerNQjO1RZ-38F1O6C3qxQHlzb2_Q8zON4BlzvXh_mULuYPZwRI3czq8k3hfNNzxGRzF3Hs0MeEXbF-ipaB3eZjX_Ox2-dbYPY1HwviBZJdgWw</recordid><startdate>20010409</startdate><enddate>20010409</enddate><creator>Trotter, B.Wesley</creator><creator>Quigley, Amy G.</creator><creator>Lumma, William C.</creator><creator>Sisko, John T.</creator><creator>Walsh, Eileen S.</creator><creator>Hamann, Christian S.</creator><creator>Robinson, Ronald G.</creator><creator>Bhimnathwala, Hema</creator><creator>Kolodin, D.Garrett</creator><creator>Zheng, Wei</creator><creator>Buser, Carolyn A.</creator><creator>Huber, Hans E.</creator><creator>Lobell, Robert B.</creator><creator>Kohl, Nancy E.</creator><creator>Williams, Theresa M.</creator><creator>Graham, Samuel L.</creator><creator>Dinsmore, Christopher J.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>20010409</creationdate><title>2-Arylindole-3-acetamides: FPP-Competitive inhibitors of farnesyl protein transferase</title><author>Trotter, B.Wesley ; Quigley, Amy G. ; Lumma, William C. ; Sisko, John T. ; Walsh, Eileen S. ; Hamann, Christian S. ; Robinson, Ronald G. ; Bhimnathwala, Hema ; Kolodin, D.Garrett ; Zheng, Wei ; Buser, Carolyn A. ; Huber, Hans E. ; Lobell, Robert B. ; Kohl, Nancy E. ; Williams, Theresa M. ; Graham, Samuel L. ; Dinsmore, Christopher J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e291t-e37d4d2b1bef763bc6953425ae2e592445d76121fd9ab678587bf9d4dff27873</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Alkyl and Aryl Transferases - antagonists & inhibitors</topic><topic>Alkyl and Aryl Transferases - metabolism</topic><topic>Antineoplastic agents</topic><topic>Biological and medical sciences</topic><topic>Carrier Proteins - metabolism</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - metabolism</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General aspects</topic><topic>Heat-Shock Proteins - metabolism</topic><topic>HSP40 Heat-Shock Proteins</topic><topic>Humans</topic><topic>Indoleacetic Acids - chemical synthesis</topic><topic>Indoleacetic Acids - metabolism</topic><topic>Indoleacetic Acids - pharmacology</topic><topic>Medical sciences</topic><topic>Pharmacology. 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The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed.
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2001-04, Vol.11 (7), p.865-869 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | ScienceDirect Journals |
| subjects | Alkyl and Aryl Transferases - antagonists & inhibitors Alkyl and Aryl Transferases - metabolism Antineoplastic agents Biological and medical sciences Carrier Proteins - metabolism Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology General aspects Heat-Shock Proteins - metabolism HSP40 Heat-Shock Proteins Humans Indoleacetic Acids - chemical synthesis Indoleacetic Acids - metabolism Indoleacetic Acids - pharmacology Medical sciences Pharmacology. Drug treatments Protein Prenylation - drug effects Protein Prenylation - physiology ras Proteins - metabolism Structure-Activity Relationship Tumor Cells, Cultured |
| title | 2-Arylindole-3-acetamides: FPP-Competitive inhibitors of farnesyl protein transferase |
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