Genomic discovery of an evolutionarily programmed modality for small-molecule targeting of an intractable protein surface

Autor: Dylan T. Stiles, Keith Robison, Alan S. Mann, Brian R. Bowman, Tara Hardy, Michelle L. Stewart, Siavash Mostafavi, Gregory L. Verdine, Seung-Joo Lee, Morgenstern Jay P, Zhigang Weng, Mathew E. Sowa, Sukrat Arya, Andrew M. Fry, Kyle Kenyon, Ende Pan, Richard D. Klausner, Khian Hong Pua, Roy M. Pollock, Sharon A. Townson, Minyun Zhou, Uddhav Kumar Shigdel, Andrew T Rajczewski, Joshua A. V. Blodgett, Daniel W. Udwary, Daniel C. Gray

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America, vol 117, iss 29
Proceedings of the National Academy of Sciences of the United States of America

Significance This manuscript reports on a member of the FK506/rapamycin family, WDB002, and the realization that FKBP-mediated recognition is a genetically programmable modality that enables engagement of topologically flat targets. FKBP-mediated rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3ebc35e6171956666cc689edb272560
https://escholarship.org/uc/item/96w4n83f

Abstract A06: Biophysical and biochemical characterization of KRAS G12C inhibition through the SMARTTM platform

Autor: Earl W. May, Meizhong Jin, Gizem Akcay, Anna Kohlmann, Sharon A. Townson, Linlong Xue, Alexander Yuzhakov, Cindy C. Benod, Ganesh Iyer, Alec D Silver, Alan S. Mann, Nicholas Perl, Minyun Zhou

Publikováno v: Molecular Cancer Research. 18:A06-A06

RAS proteins are small GTPases involved in cell proliferation, survival, and differentiation, and are mutationally activated in about a third of all human cancers. These mutations drive cancer by impairing GTPase activity so that the RAS protein is f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a684bd2145303e77787eba23f3670755
https://doi.org/10.1158/1557-3125.ras18-a06