ACC inhibitor alone or co-administered with a DGAT2 inhibitor in patients with non-alcoholic fatty liver disease: two parallel, placebo-controlled, randomized phase 2a …
…, TA Tuthill, K Kou, M Boucher, G Tesz, R Dullea… - Nature Medicine, 2021 - nature.com
… Data in a represent median (Q1, Q3), and, in b and d–r, data represent LSM (80% CI) from
an MMRM … There was no relationship between any of these parameters (r 2 ≤ 0.093 at all PF-…
an MMRM … There was no relationship between any of these parameters (r 2 ≤ 0.093 at all PF-…
[HTML][HTML] Inhibition of diacylglycerol acyltransferase 2 versus diacylglycerol acyltransferase 1: potential therapeutic implications of pharmacology
NB Amin, AR Saxena, V Somayaji, R Dullea - Clinical Therapeutics, 2023 - Elsevier
Purpose Hepatic steatosis due to altered lipid metabolism and accumulation of hepatic
triglycerides is a hallmark of nonalcoholic fatty liver disease (NAFLD). Diacylglycerol …
triglycerides is a hallmark of nonalcoholic fatty liver disease (NAFLD). Diacylglycerol …
Receptor-mediated delivery of CRISPR-Cas9 endonuclease for cell-type-specific gene editing
CRISPR-Cas RNA-guided endonucleases hold great promise for disrupting or correcting
genomic sequences through site-specific DNA cleavage and repair. However, the lack of …
genomic sequences through site-specific DNA cleavage and repair. However, the lack of …
Chemical modification study of antisense gapmers
…, T Clark, M Liu, J Qian, M Roy, R Dullea - Nucleic acid …, 2012 - liebertpub.com
… KOLE R.Effects of base modifications on antisense properties of 2′-O-methoxyethyl and
PNA oligonucleotidesAntisense Nucleic Acid Drug Dev.13119128. SAZANI, P., ASTRIAB-…
PNA oligonucleotidesAntisense Nucleic Acid Drug Dev.13119128. SAZANI, P., ASTRIAB-…
[HTML][HTML] Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain
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 …
levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the …
Efficient liver targeting by polyvalent display of a compact ligand for the asialoglycoprotein receptor
…, BA Chrunyk, K Beaumont, R Dullea… - Journal of the …, 2017 - ACS Publications
A compact and stable bicyclic bridged ketal was developed as a ligand for the asialoglycoprotein
receptor (ASGPR). This compound showed excellent ligand efficiency, and the …
receptor (ASGPR). This compound showed excellent ligand efficiency, and the …
Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule
…, E Montabana, S Liras, RG Dullea… - Nature structural & …, 2019 - nature.com
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 …
blocks the translation of a small number of proteins by an unknown mechanism. In structures of …
Pharmacological inhibition of CETP (cholesteryl ester transfer protein) increases HDL (high-density lipoprotein) that contains ApoC3 and other HDL subspecies …
…, G Ruotolo, SJ Nicholls, R Dullea… - … and Vascular Biology, 2022 - Am Heart Assoc
Objective: Plasma total HDL (high-density lipoprotein) is a heterogeneous mix of many
protein-based subspecies whose functions and associations with coronary heart disease vary. …
protein-based subspecies whose functions and associations with coronary heart disease vary. …
Discovery of ervogastat (PF-06865571): a potent and selective inhibitor of diacylglycerol acyltransferase 2 for the treatment of non-alcoholic steatohepatitis
…, MS Dowling, R Dullea… - Journal of Medicinal …, 2022 - ACS Publications
Discovery efforts leading to the identification of ervogastat (PF-06865571), a systemically
acting diacylglycerol acyltransferase (DGAT2) inhibitor that has advanced into clinical trials for …
acting diacylglycerol acyltransferase (DGAT2) inhibitor that has advanced into clinical trials for …
[PDF][PDF] Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro
…, P Walsh, P Sunderland, A Reyes, R Dullea… - Chemistry & biology, 2014 - cell.com
Disrupting the binding interaction between proprotein convertase (PCSK9) and the epidermal
growth factor-like domain A (EGF-A domain) in the low-density lipoprotein receptor (LDL-R…
growth factor-like domain A (EGF-A domain) in the low-density lipoprotein receptor (LDL-R…