Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer
[Display omitted] Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2018-02, Vol.26 (3), p.590-602 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Monastyrskyi, Andrii Nilchan, Napon Quereda, Victor Noguchi, Yoshihiko Ruiz, Claudia Grant, Wayne Cameron, Michael Duckett, Derek Roush, William |
| description | [Display omitted]
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers. |
| doi_str_mv | 10.1016/j.bmc.2017.12.020 |
| format | Article |
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Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2017.12.020</identifier><identifier>PMID: 29289448</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Binding Sites ; Breast cancer ; Casein kinase 1 delta and epsilon ; Casein Kinase Idelta - antagonists & inhibitors ; Casein Kinase Idelta - metabolism ; Casein Kinase Iepsilon - antagonists & inhibitors ; Casein Kinase Iepsilon - metabolism ; Catalytic Domain ; Cell Line, Tumor ; Female ; Half-Life ; Humans ; Inhibitor ; Kinase ; Male ; Mice ; Mice, Inbred C57BL ; Microsomes, Liver - drug effects ; Microsomes, Liver - metabolism ; Molecular Docking Simulation ; Permeability - drug effects ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacokinetics ; Protein Kinase Inhibitors - pharmacology ; Protein Kinase Inhibitors - therapeutic use ; Rats ; Structure-Activity Relationship ; Transplantation, Heterologous ; Triple Negative Breast Neoplasms - drug therapy ; Triple Negative Breast Neoplasms - metabolism ; Triple Negative Breast Neoplasms - pathology</subject><ispartof>Bioorganic & medicinal chemistry, 2018-02, Vol.26 (3), p.590-602</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c451t-94a3a42ef5b0ca22cfffe1962af2ce63c35fbdad87a8d0a58ecbcbfb8686fd753</citedby><cites>FETCH-LOGICAL-c451t-94a3a42ef5b0ca22cfffe1962af2ce63c35fbdad87a8d0a58ecbcbfb8686fd753</cites><orcidid>0000-0002-1145-1822 ; 0000-0001-9785-5897</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2017.12.020$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,777,781,882,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29289448$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Monastyrskyi, Andrii</creatorcontrib><creatorcontrib>Nilchan, Napon</creatorcontrib><creatorcontrib>Quereda, Victor</creatorcontrib><creatorcontrib>Noguchi, Yoshihiko</creatorcontrib><creatorcontrib>Ruiz, Claudia</creatorcontrib><creatorcontrib>Grant, Wayne</creatorcontrib><creatorcontrib>Cameron, Michael</creatorcontrib><creatorcontrib>Duckett, Derek</creatorcontrib><creatorcontrib>Roush, William</creatorcontrib><title>Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.</description><subject>Animals</subject><subject>Binding Sites</subject><subject>Breast cancer</subject><subject>Casein kinase 1 delta and epsilon</subject><subject>Casein Kinase Idelta - antagonists & inhibitors</subject><subject>Casein Kinase Idelta - metabolism</subject><subject>Casein Kinase Iepsilon - antagonists & inhibitors</subject><subject>Casein Kinase Iepsilon - metabolism</subject><subject>Catalytic Domain</subject><subject>Cell Line, Tumor</subject><subject>Female</subject><subject>Half-Life</subject><subject>Humans</subject><subject>Inhibitor</subject><subject>Kinase</subject><subject>Male</subject><subject>Mice</subject><subject>Mice, Inbred C57BL</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - metabolism</subject><subject>Molecular Docking Simulation</subject><subject>Permeability - drug effects</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacokinetics</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Protein Kinase Inhibitors - therapeutic use</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><subject>Transplantation, Heterologous</subject><subject>Triple Negative Breast Neoplasms - drug therapy</subject><subject>Triple Negative Breast Neoplasms - metabolism</subject><subject>Triple Negative Breast Neoplasms - pathology</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kctuEzEUhq0K1KaFB-gGeVkWM_VlxrGFhFSF3kQlNrDFsj3HrcPMONiTSLwXfY08E47SVrBh5WP5P5-PzofQKSU1JVScL2s7uJoROq8pqwkjB2hGG9FUnCv6Cs2IErIiUokjdJzzkhDCGkUP0RFTTKqmkTP0_RNsoI-rAcYJR4-7temxMxnCiH-EsRSYbn-f0-0jPlt83pXbx_c4jA_BhimmjH1MeEpgpmeCLZc8FcboIL1Br73pM7x9Ok_Qt6vLr4ub6u7L9e3i4q5yTUunSjWGm4aBby1xhjHnvQeqBDOeORDc8dbbznRybmRHTCvBWWe9lUIK381bfoI-7rmrtR2gc2WWZHq9SmEw6ZeOJuh_X8bwoO_jRreScN7yAjh7AqT4cw150kPIDvrejBDXWVMlOWuFkrRE6T7qUsw5gX_5hhK986KXunjROy-aMl28lJ53f8_30vEsogQ-7ANQtrQJkHR2AcoKu5DATbqL4T_4Pzk1owA</recordid><startdate>20180201</startdate><enddate>20180201</enddate><creator>Monastyrskyi, Andrii</creator><creator>Nilchan, Napon</creator><creator>Quereda, Victor</creator><creator>Noguchi, Yoshihiko</creator><creator>Ruiz, Claudia</creator><creator>Grant, Wayne</creator><creator>Cameron, Michael</creator><creator>Duckett, Derek</creator><creator>Roush, William</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-1145-1822</orcidid><orcidid>https://orcid.org/0000-0001-9785-5897</orcidid></search><sort><creationdate>20180201</creationdate><title>Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer</title><author>Monastyrskyi, Andrii ; Nilchan, Napon ; Quereda, Victor ; Noguchi, Yoshihiko ; Ruiz, Claudia ; Grant, Wayne ; Cameron, Michael ; Duckett, Derek ; Roush, William</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c451t-94a3a42ef5b0ca22cfffe1962af2ce63c35fbdad87a8d0a58ecbcbfb8686fd753</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Animals</topic><topic>Binding Sites</topic><topic>Breast cancer</topic><topic>Casein kinase 1 delta and epsilon</topic><topic>Casein Kinase Idelta - antagonists & inhibitors</topic><topic>Casein Kinase Idelta - metabolism</topic><topic>Casein Kinase Iepsilon - antagonists & inhibitors</topic><topic>Casein Kinase Iepsilon - metabolism</topic><topic>Catalytic Domain</topic><topic>Cell Line, Tumor</topic><topic>Female</topic><topic>Half-Life</topic><topic>Humans</topic><topic>Inhibitor</topic><topic>Kinase</topic><topic>Male</topic><topic>Mice</topic><topic>Mice, Inbred C57BL</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - metabolism</topic><topic>Molecular Docking Simulation</topic><topic>Permeability - drug effects</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacokinetics</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Protein Kinase Inhibitors - therapeutic use</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><topic>Transplantation, Heterologous</topic><topic>Triple Negative Breast Neoplasms - drug therapy</topic><topic>Triple Negative Breast Neoplasms - metabolism</topic><topic>Triple Negative Breast Neoplasms - pathology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Monastyrskyi, Andrii</creatorcontrib><creatorcontrib>Nilchan, Napon</creatorcontrib><creatorcontrib>Quereda, Victor</creatorcontrib><creatorcontrib>Noguchi, Yoshihiko</creatorcontrib><creatorcontrib>Ruiz, Claudia</creatorcontrib><creatorcontrib>Grant, Wayne</creatorcontrib><creatorcontrib>Cameron, Michael</creatorcontrib><creatorcontrib>Duckett, Derek</creatorcontrib><creatorcontrib>Roush, William</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Monastyrskyi, Andrii</au><au>Nilchan, Napon</au><au>Quereda, Victor</au><au>Noguchi, Yoshihiko</au><au>Ruiz, Claudia</au><au>Grant, Wayne</au><au>Cameron, Michael</au><au>Duckett, Derek</au><au>Roush, William</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2018-02-01</date><risdate>2018</risdate><volume>26</volume><issue>3</issue><spage>590</spage><epage>602</epage><pages>590-602</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>29289448</pmid><doi>10.1016/j.bmc.2017.12.020</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-1145-1822</orcidid><orcidid>https://orcid.org/0000-0001-9785-5897</orcidid><oa>free_for_read</oa></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry, 2018-02, Vol.26 (3), p.590-602 |
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| subjects | Animals Binding Sites Breast cancer Casein kinase 1 delta and epsilon Casein Kinase Idelta - antagonists & inhibitors Casein Kinase Idelta - metabolism Casein Kinase Iepsilon - antagonists & inhibitors Casein Kinase Iepsilon - metabolism Catalytic Domain Cell Line, Tumor Female Half-Life Humans Inhibitor Kinase Male Mice Mice, Inbred C57BL Microsomes, Liver - drug effects Microsomes, Liver - metabolism Molecular Docking Simulation Permeability - drug effects Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Rats Structure-Activity Relationship Transplantation, Heterologous Triple Negative Breast Neoplasms - drug therapy Triple Negative Breast Neoplasms - metabolism Triple Negative Breast Neoplasms - pathology |
| title | Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer |
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