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Robert G Dullea

Explore the profile of Robert G Dullea including associated specialties, affiliations and a list of published articles. Areas
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Articles 7
Citations 126
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Recent Articles
1.
Aspnes G, Coffey S, Darout E, Dechert-Schmitt A, Dullea R, Kamlet A, et al.
Bioorg Med Chem Lett . 2023 Jun; 92:129394. PMID: 37379958
Our previous work on the optimization of a new class of small molecule PCSK9 mRNA translation inhibitors focused on empirical optimization of the amide tail region of the lead PF-06446846...
2.
Li W, Ward F, McClure K, Chang S, Montabana E, Liras S, et al.
Nat Struct Mol Biol . 2019 Jun; 26(6):501-509. PMID: 31160784
The drug-like molecule PF-06446846 (PF846) binds the human ribosome and selectively blocks the translation of a small number of proteins by an unknown mechanism. In structures of PF846-stalled human ribosome...
3.
Londregan A, Wei L, Xiao J, Lintner N, Petersen D, Dullea R, et al.
J Med Chem . 2018 Jun; 61(13):5704-5718. PMID: 29878763
The optimization of a new class of small molecule PCSK9 mRNA translation inhibitors is described. The potency, physicochemical properties, and off-target pharmacology associated with the hit compound (1) were improved...
4.
Lintner N, McClure K, Petersen D, Londregan A, Piotrowski D, Wei L, et al.
PLoS Biol . 2018 Apr; 16(4):e1002628. PMID: 29664898
[This corrects the article DOI: 10.1371/journal.pbio.2001882.].
5.
McClure K, Piotrowski D, Petersen D, Wei L, Xiao J, Londregan A, et al.
Angew Chem Int Ed Engl . 2017 Oct; 56(51):16218-16222. PMID: 29073340
Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. A liver-targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9, a lipid regulator...
6.
Lintner N, McClure K, Petersen D, Londregan A, Piotrowski D, Wei L, et al.
PLoS Biol . 2017 Mar; 15(3):e2001882. PMID: 28323820
Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the compound PF-06446846 inhibits translation of...
7.
Chen C, Stock J, Liu X, Shi J, Van Deusen J, DiMattia D, et al.
Drug Metab Dispos . 2008 Jun; 36(9):1840-5. PMID: 18556442
We generated the organic anion transporting polypeptide (Oatp) 1b2 knockout (KO) mouse model and assessed its utility to study hepatic uptake using model compounds: cerivastatin, lovastatin acid, pravastatin, simvastatin acid,...