Dotinurad: a clinical pharmacokinetic study of a novel, selective urate reabsorption inhibitor in subjects with hepatic impairment
Sign Up to like & getrecommendations! Published in 2019 at "Clinical and Experimental Nephrology"
DOI: 10.1007/s10157-019-01816-4
Abstract: Background Dotinurad is a novel, selective urate reabsorption inhibitor, which reduces serum uric acid levels by inhibiting the urate transporter 1 (URAT1). We compared the pharmacokinetics (PK), pharmacodynamics (PD), and safety of dotinurad in subjects… read more here.
Keywords: hepatic impairment; group; study; novel selective ... See more keywords
Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.12.028
Abstract: The sphingomyelin synthase 2 (SMS2) is a potential target for pharmacological intervention in atherosclerosis. However, so far, few selective SMS2 inhibitors and their pharmacological activities were reported. In this study, a class of 2-benzyloxybenzamides were… read more here.
Keywords: inhibitor; novel selective; anti atherosclerotic; atherosclerotic activities ... See more keywords
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111769
Abstract: Polo-like kinase 1 (Plk1) is a validated target for the treatment of cancer. In this report, by analyzing amino acid residue differences among the ATP-binding pockets of Plk1, Plk2 and Plk3, novel selective Plk1 inhibitors… read more here.
Keywords: plk1; like kinase; plk1 inhibitors; polo like ... See more keywords
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113394
Abstract: Herein, we describe the design, synthesis, and structure-activity relationships of a series of imidazopyrrolopyridines derivatives that selectively inhibit Janus kinase 2 (JAK2). These screening cascades revealed that 6k was a preferred compound, with IC50 values… read more here.
Keywords: imidazopyrrolopyridines derivatives; derivatives novel; discovery imidazopyrrolopyridines; novel selective ... See more keywords
Novel Selective Galectin-3 Antagonists Are Cytotoxic to Acute Lymphoblastic Leukemia.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01296
Abstract: Galectin-3 is a β-galactoside-specific, carbohydrate-recognizing protein (lectin) that is strongly implicated in cancer development, metastasis, and drug resistance. Galectin-3 promotes migration and ability to withstand drug treatment of B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells.… read more here.
Keywords: acute lymphoblastic; novel selective; galectin; lymphoblastic leukemia ... See more keywords
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00149
Abstract: A series of biaryl chromans exhibiting potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM) were discovered as potential therapeutics for the treatment of type II diabetes. Optimization… read more here.
Keywords: biaryl; relationship novel; novel selective; activity relationship ... See more keywords
Identification of a novel selective PPARγ ligand with a unique binding mode and improved therapeutic profile in vitro
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/srep41487
Abstract: Thiazolidinediones (TZD) function as potent anti-diabetic drugs through their direct action on the nuclear receptor peroxisome proliferator-activated receptor γ (PPARγ), but their therapeutic benefits are compromised by severe side effects. To address this concern, here… read more here.
Keywords: ppar; vsp; selective ppar; novel selective ... See more keywords
Identifying novel selective PPO inhibitors through structure-based virtual screening and bio-evaluation
Sign Up to like & getrecommendations! Published in 2023 at "RSC Advances"
DOI: 10.1039/d2ra08006k
Abstract: Protoporphyrinogen oxidase (PPO) is a key enzyme in chlorophyll and heme biosynthesis, and the development of its inhibitors is of great importance both in the pharmaceutical and pesticide industries. However, the currently developed PPO inhibitors… read more here.
Keywords: ppo; novel selective; virtual screening; ppo inhibitors ... See more keywords
Therapeutic efficacy of the novel selective RNA polymerase I inhibitor CX‐5461 on pulmonary arterial hypertension and associated vascular remodelling
Sign Up to like & getrecommendations! Published in 2021 at "British Journal of Pharmacology"
DOI: 10.1111/bph.15385
Abstract: CX‐5461 is a novel selective RNA polymerase I (Pol I) inhibitor. Previously, we found that CX‐5461 could inhibit pathological arterial remodelling caused by angioplasty and transplantation. In the present study, we explored the pharmacological effects… read more here.
Keywords: arterial hypertension; rna polymerase; pulmonary arterial; novel selective ... See more keywords
Marked effects of novel selective peroxisome proliferator-activated receptor α modulator, pemafibrate in severe hypertriglyceridemia: preliminary report
Sign Up to like & getrecommendations! Published in 2020 at "Cardiovascular Diabetology"
DOI: 10.1186/s12933-020-01172-8
Abstract: Background Currently available treatments have only been partly successful in patients with severe hypertriglyceridemia, including those with high serum triglycerides above 1,000 mg/dL (11.3 mmol/L), who often suffer from acute pancreatitis. Pemafibrate is a novel selective peroxisome… read more here.
Keywords: mmol; severe hypertriglyceridemia; selective peroxisome; pemafibrate ... See more keywords
Antifibrotic Effect of a Novel Selective 11β-HSD2 Inhibitor (WZ51) in a rat Model of Myocardial Fibrosis
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2021.629818
Abstract: Myocardial fibrosis (MF) is one of the leading causes of end-stage heart disease. Many studies have confirmed that inflammation caused by aldosterone may play an important role in the process of MF. A selective 11β-hydroxysteroid… read more here.
Keywords: selective hsd2; inhibitor; effect novel; hsd2 ... See more keywords