Taavi K Neklesa
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Explore the profile of Taavi K Neklesa including associated specialties, affiliations and a list of published articles.
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12
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889
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Recent Articles
1.
Snyder L, Neklesa T, Willard R, Gordon D, Pizzano J, Vitale N, et al.
Mol Cancer Ther
. 2024 Dec;
PMID: 39670468
Androgen receptor (AR) signaling is the principal driver of prostate cancer, and drugs that target this pathway (e.g., abiraterone and enzalutamide) are standard treatments for metastatic hormone-sensitive prostate cancer and...
2.
Flanagan J, Neklesa T
Mol Cell Endocrinol
. 2019 May;
493:110452.
PMID: 31125586
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....
3.
Salami J, Alabi S, Willard R, Vitale N, Wang J, Dong H, et al.
Commun Biol
. 2018 Oct;
1:100.
PMID: 30271980
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....
4.
Crew A, Raina K, Dong H, Qian Y, Wang J, Vigil D, et al.
J Med Chem
. 2017 Jul;
61(2):583-598.
PMID: 28692295
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...
5.
Neklesa T, Winkler J, Crews C
Pharmacol Ther
. 2017 Feb;
174:138-144.
PMID: 28223226
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...
6.
Gustafson J, Neklesa T, Cox C, Roth A, Buckley D, Tae H, et al.
Angew Chem Int Ed Engl
. 2015 Jun;
54(33):9659-62.
PMID: 26083457
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...
7.
Neklesa T, Noblin D, Kuzin A, Lew S, Seetharaman J, Acton T, et al.
ACS Chem Biol
. 2013 Aug;
8(10):2293-2300.
PMID: 23978068
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...
8.
9.
Tae H, Sundberg T, Neklesa T, Noblin D, Gustafson J, Roth A, et al.
Chembiochem
. 2012 Jan;
13(4):538-41.
PMID: 22271667
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,...
10.
Neklesa T, Tae H, Schneekloth A, Stulberg M, Corson T, Sundberg T, et al.
Nat Chem Biol
. 2011 Jul;
7(8):538-43.
PMID: 21725302
The ability to regulate any protein of interest in living systems with small molecules remains a challenge. We hypothesized that appending a hydrophobic moiety to the surface of a protein...