Revisiting the halogen bonding between phosphodiesterase type 5 and its inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Modeling"
DOI: 10.1007/s00894-018-3897-z
Abstract: Halogenated ligands are nowadays commonly designed in order to increase their potency against protein targets. Although novel computational methods of evaluating the affinity of such halogenated inhibitors have emerged, they still lack the sufficient accuracy,… read more here.
Keywords: phosphodiesterase type; halogen bonding; bonding phosphodiesterase; type inhibitors ... See more keywords
The use of antimuscarinics, phosphodiesterase type V inhibitors and phytotherapy for lower urinary tract symptoms in men
Sign Up to like & getrecommendations! Published in 2017 at "Asian Journal of Urology"
DOI: 10.1016/j.ajur.2017.05.002
Abstract: Besides the mainstay of α-blockers and 5α-reductase inhibitors, other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms (LUTS) in men. These treatments can target specific symptoms as well… read more here.
Keywords: urinary tract; phosphodiesterase type; tract symptoms; type inhibitors ... See more keywords
Design, 3D QSAR modeling and docking of TGF-β type I inhibitors to target cancer
Sign Up to like & getrecommendations! Published in 2018 at "Computational biology and chemistry"
DOI: 10.1016/j.compbiolchem.2018.07.011
Abstract: Transforming growth factor-β (TGF-β) family members plays a vital role in regulating hormonal function, bone formation, tissue remodeling, and erythropoiesis, cell growth and apoptosis. TGF-β super-family members mediate signal transduction via serine/threonine kinase receptors located… read more here.
Keywords: tgf type; type inhibitors; qsar; cancer ... See more keywords
EDEUS, a Real-Life Study on the Users of Phosphodiesterase Type 5 Inhibitors: Prevalence, Perceptions, and Health Care-Seeking Behavior Among European Men With a Focus on 2nd-Generation Avanafil
Sign Up to like & getrecommendations! Published in 2018 at "Sexual Medicine"
DOI: 10.1016/j.esxm.2017.10.003
Abstract: Introduction Erectile dysfunction (ED) is a multidimensional disorder with an estimated prevalence of 1% to 10% in men younger than 40 years and up to 100% in men in their 70s and 80s. Aim To… read more here.
Keywords: phosphodiesterase type; generation; type inhibitors; real life ... See more keywords
PERSISTENCE AND ADHERENCE WITH PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 INHIBITORS IN CLINICAL PRACTICE
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the American College of Cardiology"
DOI: 10.1016/s0735-1097(17)33548-9
Abstract: Background: Elevated low-density lipoprotein cholesterol (LDL-C) is associated with premature atherosclerotic cardiovascular disease. Proprotein convertase subtilisin/kexin type 9 inhibitors (PCSK9i) have shown reductions in LDL-C levels in patients uncontrolled by statin and/or ezetimibe therapy. read more here.
Keywords: proprotein convertase; subtilisin kexin; kexin type; type inhibitors ... See more keywords
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01568
Abstract: For the first time, the in silico design, screening, and in vitro validation of potent GSK-3β type-II inhibitors are presented. In the absence of crystallographic evidence for a DFG-out GSK-3β activation loop conformation, computational models… read more here.
Keywords: type inhibitors; structure based; gsk; design ... See more keywords
NTRK kinase domain mutations in cancer variably impact sensitivity to type I and type II inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Communications Biology"
DOI: 10.1038/s42003-020-01508-w
Abstract: Tyrosine kinase domains dynamically fluctuate between two main structural forms that are referred to as type I (DFG-in) or type II (DFG-out) conformations. Comprehensive data comparing type I and type II inhibitors are currently lacking… read more here.
Keywords: type inhibitors; sensitivity; type; type type ... See more keywords
Impact of Type II LRRK2 inhibitors on signaling and mitophagy
Sign Up to like & getrecommendations! Published in 2021 at "Biochemical Journal"
DOI: 10.1042/bcj20210375
Abstract: Much effort has been devoted to the development of selective inhibitors of the LRRK2 as a potential treatment for LRRK2 driven Parkinson's disease. In this study, we first compare the properties of Type I (GSK3357679A… read more here.
Keywords: type lrrk2; impact type; type inhibitors; lrrk2 inhibitors ... See more keywords
Risk of nonarteritic ischaemic optic neuropathy with phosphodiesterase type 5 inhibitors: a systematic review and meta‐analysis
Sign Up to like & getrecommendations! Published in 2019 at "Acta Ophthalmologica"
DOI: 10.1111/aos.14253
Abstract: The development of nonarteritic anterior ischaemic optic neuropathy has been described to phosphodiesterase type 5 inhibitors. The aim of this systematic review and meta‐analysis was to assess the risk of nonarteritic anterior ischaemic optic neuropathy… read more here.
Keywords: type inhibitors; optic neuropathy; phosphodiesterase type; ischaemic optic ... See more keywords
Resistance Profile and Structural Modeling of Next-Generation ROS1 Tyrosine Kinase Inhibitors
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DOI: 10.1158/1535-7163.mct-21-0395
Abstract: ROS1 fusion proteins resulting from chromosomal rearrangements of the ROS1 gene are targetable oncogenic drivers in diverse cancers. Acquired resistance to targeted inhibitors curtails clinical benefit and response durability. Entrectinib, a NTRK/ROS1/ALK targeted tyrosine kinase… read more here.
Keywords: tyrosine kinase; type inhibitors; ros1; inhibitor ... See more keywords
Elephant in the Room: Cost of Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Circulation. Cardiovascular quality and outcomes"
DOI: 10.1161/circoutcomes.117.004425
Abstract: See Article by Doshi et al In this issue of Circulation: Cardiovascular Quality and Outcomes , Doshi et al1 raise the issue of whether the prior authorization (PA) program requirements are particularly excessive for the… read more here.
Keywords: proprotein convertase; subtilisin kexin; kexin type; type inhibitors ... See more keywords