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

Design of Potent and Selective Hybrid Inhibitors of the Mitotic Kinase Nek2: Structure–Activity Relationship, Structural Biology, and Cellular Activity

Autor: Kwai-Ming J. Cheung, Joanne E. Baxter, Andrew M. Fry, K. Boxall, Savade Solanki, Swen Hoelder, Tara Hardy, Paolo Innocenti, Lisa Pickard, Fiona C. Rowan, Corine Mas-Droux, G.W. Aherne, Maura Westlake, Richard Bayliss, Sharon Yeoh

Publikováno v: Journal of Medicinal Chemistry. 55:3228-3241

We report herein a series of Nek2 inhibitors based on an aminopyridine scaffold. These compounds have been designed by combining key elements of two previously discovered chemical series. Structure based design led to aminopyridine (R)-21, a potent a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0ca4fb1393808f0e7b8cbff3fe2a1136
https://doi.org/10.1021/jm201683b

An undecided coiled coil: the leucine zipper of Nek2 kinase exhibits atypical conformational exchange dynamics

Autor: Rebecca, Croasdale, Frank J, Ivins, Fred, Muskett, Tina, Daviter, David J, Scott, Tara, Hardy, Steven J, Smerdon, Andrew M, Fry, Mark, Pfuhl

Publikováno v: The Journal of Biological Chemistry

Leucine zippers are oligomerization domains used in a wide range of proteins. Their structure is based on a highly conserved heptad repeat sequence in which two key positions are occupied by leucines. The leucine zipper of the cell cycle-regulated Ne

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e2f98a5eb209ffcf6f076e3eee6b6547
https://pubmed.ncbi.nlm.nih.gov/21669869

Assessing the Lesbian Victim

Autor: Tara Hardy

Publikováno v: Same-Sex Domestic Violence: Strategies for Change

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::06d37d887037d0bc35a590c808147e86
https://doi.org/10.4135/9781452231914.n18