Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Taavi K. Neklesa"'
Autor:
Taavi K Neklesa, Ronald W Davis
Publikováno v:
PLoS Genetics, Vol 5, Iss 6, p e1000515 (2009)
TORC1 is a central regulator of cell growth in response to amino acid availability, yet little is known about how it is regulated. Here, we performed a reverse genetic screen in yeast for genes necessary to inactivate TORC1. The screen consisted of m
Externí odkaz:
https://doaj.org/article/292fe920a0a24e08a489dc56b8deebfe
Autor:
Andrew P. Crew, Ron Peck, Xin Chen, Deborah A. Gordon, Hanqing Dong, Jennifer Pizzano, John Houston, Jennifer Macaluso, Taavi K. Neklesa, Craig M. Crews, Nicholas Vitale, Ian Taylor, Caterina Ferraro, Lawrence Snyder, Jing Wang, Ryan R. Willard, Marcia Dougan Moore
Publikováno v:
Cancer Research. 81:43-43
Prostate cancer is the second leading cause of cancer death in men in the United States. The androgen receptor (AR) plays critical roles in both early disease and advanced prostate cancer. Current therapeutic approaches targeting the androgen/AR axis
Autor:
Andrew P. Crew, Taavi K. Neklesa, Donald P. McDonnell, Craig M. Crews, Shanique B. Alabi, Jemilat Salami, Hanqing Dong, Meizhong Jin, Nick J. Vitale, Jing Wang, Ryan R. Willard
Publikováno v:
Communications Biology, Vol 1, Iss 1, Pp 1-9 (2018)
The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management. However, the majority of patient
Autor:
Jeffrey L. Gustafson, Taavi K. Neklesa, D. Blake Stagg, Anke G. Roth, John Hines, Thomas B. Sundberg, John D. Norris, Carly S. Cox, Donald P. McDonnell, Hyun Seop Tae, Craig M. Crews, Dennis L. Buckley
Publikováno v:
Angewandte Chemie International Edition. 54:9659-9662
Androgen Receptor (AR)-dependent transcription is a major driver of prostate tumor cell proliferation. Consequently, it is the target of several antitumor chemotherapeutic agents, including the AR antagonist MDV3100/enzalutamide. Recent studies have
Autor:
Alicia Morgan, Kevin Coleman, Dominico Vigil, Caterina Ferraro, Andrew P. Crew, Kam W. Siu, Brian D. Hamman, James D. Winkler, Jing Wang, Yevgeniy V. Serebrenik, Craig M. Crews, Yimin Qian, Taavi K. Neklesa, Kanak Raina, Hanqing Dong
Publikováno v:
Journal of medicinal chemistry. 61(2)
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young
Publikováno v:
Pharmacologytherapeutics. 174
Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases driven by the aberrant expression of a disease-causing protein. PROTAC molecules are bifunctional small molecules that simultaneous
Autor:
Taavi K. Neklesa, John J. Flanagan
Publikováno v:
Molecular and Cellular Endocrinology. 493:110452
Nuclear receptors comprise a class of intracellular transcription factors whose major role is to act as sensors of various stimuli and to convert the external signal into a transcriptional output. Nuclear receptors (NRs) achieve this by possessing a
Autor:
Caterina Ferraro, Jing Wang, Ryan R. Willard, Taavi K. Neklesa, Jennifer Pizzano, John Houston, Ian Taylor, Gan Wang, Nicholas Vitale, Andrew P. Crew, Deborah A. Gordon, Hanqing Dong, Mark Bookbinder, Jennifer Macaluso, Craig M. Crews, Lawrence Snyder
Publikováno v:
Journal of Clinical Oncology. 37:259-259
259 Background: The Androgen Receptor (AR) remains the principal driver of castration-resistant prostate cancer during the transition from a localized to metastatic disease. Most patients initially respond to inhibitors of the AR pathway, but the res
Autor:
Alexander P. Kuzin, Devin J. Noblin, Thomas Acton, Craig M. Crews, Liang Tong, G. Kornhaber, Gaetano T. Montelione, Scott Lew, Jayaraman Seetharaman, Taavi K. Neklesa, Rong Xiao
Publikováno v:
ACS Chemical Biology. 8:2293-2300
Small molecule control of intracellular protein levels allows temporal and dose-dependent regulation of protein function. Recently, we developed a method to degrade proteins fused to a mutant dehalogenase (HaloTag2) using small molecule hydrophobic t
Autor:
Craig M. Crews, Thomas B. Sundberg, Taavi K. Neklesa, Devin J. Noblin, Kanak Raina, Hyun Seop Tae, Anke G. Roth, Jeffrey L. Gustafson
Publikováno v:
ChemBioChem. 13:538-541
New HyTs are a knockout: we previously reported that labeling HaloTag proteins with low molecular weight hydrophobic tags (HyTs) leads to targeted degradation of HaloTag fusion proteins. In this report, we employed a chemical approach to extend this