Conservation of coactivator engagement mechanism enables small-molecule allosteric modulators

Autor: Matthew J. Henley, James A. Wells, Tomasz Cierpicki, Brian M. Linhares, Amanda L. Peiffer, Z.B. Hill, Nicholas J. Foster, Steven M. Sturlis, Kevon D. Stanford, Anna K. Mapp, Matthew S. Beyersdorf, Charles L. Brooks, Carol A. Fierke, Andrew R. Henderson

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America

Significance Transcriptional coactivators and their partner transcription factors have been labeled as intrinsically disordered, fuzzy, and undruggable. We propose that the identification of conserved mechanisms of engagement between coactivators and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa43e1514af79802656ce43777b2fdae
http://europepmc.org/articles/PMC6130367

An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering

Autor: E. Kang, Justin T Biel, Z.B. Hill, José Brandão-Neto, Frank von Delft, James A. Wells, Daniel A. Keedy, James S. Fraser, Nicholas M Pearce, T. Justin Rettenmaier

Publikováno v: eLife, Vol 7 (2018)
ELIFE, vol 7
Keedy, DA; Hill, ZB; Biel, JT; Kang, E; Rettenmaier, TJ; Brandão-Neto, J; et al.(2018). An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering. eLife, 7. doi: 10.7554/eLife.36307. UCSF: Retrieved from: http://www.escholarship.org/uc/item/4tk2c02t
Keedy, DA; Hill, ZB; Biel, JT; Kang, E; Rettenmaier, TJ; Brandao-Neto, J; et al.(2018). An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering. ELIFE, 7. doi: 10.7554/eLife.36307.001. UCSF: Retrieved from: http://www.escholarship.org/uc/item/6w5970b7
eLife

Allostery is an inherent feature of proteins, but it remains challenging to reveal the mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic circuitry would afford new opportunities to modulate protein function.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8dd86c17f8f80e5ecc812260f93d5cd
https://elifesciences.org/articles/36307

Human antibody-based chemically induced dimerizers for cell therapeutic applications

Autor: Alexander J. Martinko, Z.B. Hill, Duy P. Nguyen, James A. Wells

Publikováno v: Nature chemical biology, vol 14, iss 2
Nature chemical biology

Chemically induced dimerizers (CIDs) have emerged as one of the most powerful tools for artificially regulating signaling pathways in cells; however, currently available CID systems lack the properties desired for use in regulating cellular therapies

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c24235346f45474d49a0f4ddcf778f20
https://escholarship.org/uc/item/53s4f07s

Art Festivals & Galleries: The Art of Selling Art

Autor: Z.B. Hill

While many people dream of being an artist, there is an art behind art that is just as important as what artists create with paint or cameras. Selling art—often at festivals and galleries—is an important part of many artists'careers. Discover the

Bivalent inhibitors of the tyrosine kinases ABL and SRC: determinants of potency and selectivity

Autor: Dustin J. Maly, Z.B. Hill, B. Gayani K. Perera

Publikováno v: Mol. BioSyst.. 7:447-456

We recently reported a chemical genetic method for generating bivalent inhibitors of protein kinases. This method relies on the use of the DNA repair enzyme O(6)-alkylguanine-DNA alkyltransferase (AGT) to display an ATP-competitive inhibitor and a li

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32524cf4f874f0a9c5e300869ca2f6f3
https://doi.org/10.1039/c0mb00108b