Concept
Renin inhibitor
Related publications (49)
Altered heart cytokine profile and action potential modulation in cardiomyocytes from Mas-deficient mice
The renin-angiotensin system (RAS) is a key hormonal system. In recent years, the functional analysis of the novel axis of the RAS (ACE2/Ang-(1-7)/Mas receptor) revealed that its activation can become pro-tective against several pathologies, including card ...
ACADEMIC PRESS INC ELSEVIER SCIENCE2022Investigation of the specificity and mechanism of action of the ULK1/AMPK inhibitor SBI-0206965
Kei Sakamoto, Katyayanee Neopane
SBI-0206965, originally identified as an inhibitor of the autophagy initiator kinase ULK1, has recently been reported as a more potent and selective AMP-activated protein kinase (AMPK) inhibitor relative to the widely used, but promiscuous inhibitor Compou ...
2021Can Precision Electrophile Signaling Make a Meaningful and Lasting Impression in Drug Design?
For several years, drugs with reactive electrophilic appendages have been developed. These units typically confer prolonged residence time of the drugs on their protein targets, and may assist targeting shallow binding sites and/or improving the drug-prote ...
WILEY-V C H VERLAG GMBH2021Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism
Henning Paul-Julius Stahlberg, Dongchun Ni
ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...
NATURE RESEARCH2021Characterization of the Renin-Angiotensin System in Aged Cavernosal Tissue and its Role in Penile Fibrosis
Nikolaos Stergiopoulos, Mikaël Nils Sturny, Fabiana Pereira Da Costa Fraga, Maiia Bragina, Babak Ebadi Shirmard
Background: The renin-angiotensin system (RAS) plays an important role in erectile function. The RAS contains 2 major axes: one deleterious, composed of ACE-Ang II-AT1 receptor, and another protective, composed of ACE2-Ang-(1-7)-Mas receptor. While aging i ...
ELSEVIER SCI LTD2020Zinc complexation improves angiotensin II receptor type 1 blockade and in vivo antihypertensive activity of telmisartan
Nikolaos Stergiopoulos, Augusto Martins Lima, Valeria Romina Martinez
Background: Angiotensin II receptor blockers were designed as therapeutic agents to block the binding site of the angiotensin II receptor type 1 (AT1R). Methodology: The structure of telmisartan was modified by coordination to the biometal Zn(II), resultin ...
FUTURE SCI LTD2020Human proteinase 3 resistance to inhibition extends to alpha-2 macroglobulin
Polymorphonuclear neutrophils contain at least four serine endopeptidases, namely neutrophil elastase (NE), proteinase 3 (PR3), cathepsin G (CatG), and NSP4, which contribute to the regulation of infection and of inflammatory processes. In physiological co ...
2020Optimized antiangiogenic reprogramming of the tumor microenvironment potentiates CD40 immunotherapy
Michele De Palma, Alan Nicolas Thierry Guichard, Nicolo Rigamonti, Daniela Pais Ferreira
Cancer immunotherapies are increasingly combined with targeted therapies to improve therapeutic outcomes. We show that combination of agonistic anti-CD40 with antiangiogenic antibodies targeting 2 proangiogenic factors, vascular endothelial growth factor A ...
2020Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity
Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Jeremy Touati, Michal Sabisz, Alice Baumann
Matrix metalloproteinases (MMPs) are zinc‐dependent endopeptidases at the intersection of health and disease due to their involvement in processes such as tissue repair and immunity as well as cancer and inflammation. Because of the high structural conserv ...
2019Can Biomimetic Zinc Compounds Assist a (3 + 2) Cycloaddition Reaction? A Theoretical Perspective
Ursula Röthlisberger, Esra Bozkurt
Compounds bearing tetrazole rings are valuable facets in numerous branches of chemistry including metabolic imaging and the production of drugs and high-energy materials. Synthesis of tetrazoles with the help of organocatalysts has intensively been explore ...
2017