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Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT)
[Image: see text] In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encode...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2015
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4434457/ https://www.ncbi.nlm.nih.gov/pubmed/26005528 http://dx.doi.org/10.1021/acsmedchemlett.5b00025 |
| _version_ | 1782371769437388800 |
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| author | Yang, Hongfang Medeiros, Patricia F. Raha, Kaushik Elkins, Patricia Lind, Kenneth E. Lehr, Ruth Adams, Nicholas D. Burgess, Joelle L. Schmidt, Stanley J. Knight, Steven D. Auger, Kurt R. Schaber, Michael D. Franklin, G. Joseph Ding, Yun DeLorey, Jennifer L. Centrella, Paolo A. Mataruse, Sibongile Skinner, Steven R. Clark, Matthew A. Cuozzo, John W. Evindar, Ghotas |
| author_facet | Yang, Hongfang Medeiros, Patricia F. Raha, Kaushik Elkins, Patricia Lind, Kenneth E. Lehr, Ruth Adams, Nicholas D. Burgess, Joelle L. Schmidt, Stanley J. Knight, Steven D. Auger, Kurt R. Schaber, Michael D. Franklin, G. Joseph Ding, Yun DeLorey, Jennifer L. Centrella, Paolo A. Mataruse, Sibongile Skinner, Steven R. Clark, Matthew A. Cuozzo, John W. Evindar, Ghotas |
| author_sort | Yang, Hongfang |
| collection | PubMed |
| description | [Image: see text] In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray crystal structure of a representative inhibitor from this chemotype demonstrated a unique binding mode in the p110α protein. |
| format | Online Article Text |
| id | pubmed-4434457 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2015 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-44344572016-05-14 Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT) Yang, Hongfang Medeiros, Patricia F. Raha, Kaushik Elkins, Patricia Lind, Kenneth E. Lehr, Ruth Adams, Nicholas D. Burgess, Joelle L. Schmidt, Stanley J. Knight, Steven D. Auger, Kurt R. Schaber, Michael D. Franklin, G. Joseph Ding, Yun DeLorey, Jennifer L. Centrella, Paolo A. Mataruse, Sibongile Skinner, Steven R. Clark, Matthew A. Cuozzo, John W. Evindar, Ghotas ACS Med Chem Lett [Image: see text] In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray crystal structure of a representative inhibitor from this chemotype demonstrated a unique binding mode in the p110α protein. American Chemical Society 2015-03-20 /pmc/articles/PMC4434457/ /pubmed/26005528 http://dx.doi.org/10.1021/acsmedchemlett.5b00025 Text en Copyright © 2015 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
| spellingShingle | Yang, Hongfang Medeiros, Patricia F. Raha, Kaushik Elkins, Patricia Lind, Kenneth E. Lehr, Ruth Adams, Nicholas D. Burgess, Joelle L. Schmidt, Stanley J. Knight, Steven D. Auger, Kurt R. Schaber, Michael D. Franklin, G. Joseph Ding, Yun DeLorey, Jennifer L. Centrella, Paolo A. Mataruse, Sibongile Skinner, Steven R. Clark, Matthew A. Cuozzo, John W. Evindar, Ghotas Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT) |
| title | Discovery of a Potent Class of PI3Kα Inhibitors
with Unique Binding Mode via Encoded Library Technology (ELT) |
| title_full | Discovery of a Potent Class of PI3Kα Inhibitors
with Unique Binding Mode via Encoded Library Technology (ELT) |
| title_fullStr | Discovery of a Potent Class of PI3Kα Inhibitors
with Unique Binding Mode via Encoded Library Technology (ELT) |
| title_full_unstemmed | Discovery of a Potent Class of PI3Kα Inhibitors
with Unique Binding Mode via Encoded Library Technology (ELT) |
| title_short | Discovery of a Potent Class of PI3Kα Inhibitors
with Unique Binding Mode via Encoded Library Technology (ELT) |
| title_sort | discovery of a potent class of pi3kα inhibitors
with unique binding mode via encoded library technology (elt) |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4434457/ https://www.ncbi.nlm.nih.gov/pubmed/26005528 http://dx.doi.org/10.1021/acsmedchemlett.5b00025 |
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