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Concept

Renin inhibitor

Publications associées (30)

Exploring the role of cGAS-STING-mediated inflammation in age-associated neurodegeneration and antitumor immunity

Natasha Ella Samson

Inflammation stands as a dynamic and intricate biological process, promoting vital defence mechanisms against harmful stimuli, including infections and injuries, to drive pathogen clearance and healing. On one hand, these responses can manifest acutely and ...

EPFL2024

Altered heart cytokine profile and action potential modulation in cardiomyocytes from Mas-deficient mice

Analina Raquel Hausin

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 SCIENCE2022

Rational design of protein switches: applications in synthetic biology and cancer immunotherapy

Sailan Shui

Synthetic biology aims to engineer cells as miniature biological devices to sense, process, and respond to exogenous stimuli. Protein switches are designed to sense and respond to various molecular queues in a fast and specific manner, which fits the requi ...

EPFL2022

Investigation of the specificity and mechanism of action of the ULK1/AMPK inhibitor SBI-0206965

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 ...

2021

Can Precision Electrophile Signaling Make a Meaningful and Lasting Impression in Drug Design?

Yimon Aye, Amogh Kulkarni

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 GMBH2022

Structures 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 Research2021

Characterization of the Renin-Angiotensin System in Aged Cavernosal Tissue and its Role in Penile Fibrosis

Nikolaos Stergiopoulos, Mikaël Nils Sturny, Maiia Bragina

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 LTD2020

Zinc complexation improves angiotensin II receptor type 1 blockade and in vivo antihypertensive activity of telmisartan

Nikolaos Stergiopoulos, Augusto Martins Lima

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 LTD2021

Human proteinase 3 resistance to inhibition extends to alpha-2 macroglobulin

Marc Moniatte

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 ...

2020

De novo development of proteolytically resistant therapeutic peptides for oral administration

Christian Heinis, Florence Pojer, Luciano Andres Abriata, Xudong Kong, Kaycie Marie Butler, Vanessa Carle

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...

2020

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Kaycie Marie Butler, Jeremy Touati, Maola Khan Mohammad Golam, Michal Sabisz

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 ...

2019

Can 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

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor

John McKinney, Neeraj Dhar, François Signorino-Gelo

Despite being one of the first antitubercular agents identified, isoniazid (INH) is still the most prescribed drug for prophylaxis and tuberculosis (TB) treatment and, together with rifampicin, the pillars of current chemotherapy. A high percentage of ison ...

Elsevier Science Bv2016

Arene Osmium Complexes with Ethacrynic Acid-Modified Ligands: Synthesis, Characterization, and Evaluation of Intracellular Glutathione S-Transferase Inhibition and Antiproliferative Activity

Paul Joseph Dyson, Tina Riedel, Emilia Paunescu

Four arene osmium complexes were prepared containing derivatives of ethacrynic acid, a potent inhibitor of glutathione Stransferases, either by direct coordination or via N- or P-donor ligands. The complexes were characterized by spectroscopic and analytic ...

American Chemical Society2016

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening

Pierre Gönczy, Sachin Kotak, Maria Josefina Marcaida Lopez

Here we report the discovery of a selective inhibitor of Aurora A, a key regulator of cell division and potential anticancer target. We used the atom category extended ligand overlap score (xLOS), a 3D ligand-based virtual screening method recently develop ...

2016

Development of potent and selective S. aureus sortase A inhibitors Based on Peptide Macrocycles

Christian Heinis, Inmaculada Rentero Rebollo, Davide Bertoldo

Sortases are transpeptidase enzymes that anchor surface proteins, including virulence factors, to the cell wall of Gram-positive bacteria, and they are potential targets for the development of anti-infective agents. While several large compound libraries w ...

2016

Update on the role of angiotensin in the pathophysiology of coronary atherothrombosis

Nikolaos Stergiopoulos, Rodrigo Araujo Fraga Da Silva

BackgroundCoronary atherothrombosis due to atherosclerotic plaque rupture or erosion is frequently associated with acute coronary syndromes (ACS). Significant efforts have been made to elucidate the pathophysiological mechanisms underlying acute coronary e ...

Wiley-Blackwell2015

Diminazene Protects Corpus Cavernosum Against Hypercholesterolemia-Induced Injury

Nikolaos Stergiopoulos, Rafaela Fernandes Da Silva, Mikaël Nils Sturny, Younouss Faye

IntroductionAngiotensin-converting enzyme 2 (ACE2) is a key enzyme of the renin angiotensin system, which breaks down angiotensin II and forms angiotensin-(1-7). In erectile tissues, it has been documented that angiotensin II contributes to the development ...

Wiley-Blackwell2015

Antihypertensive drugs metabolism: an update to pharmacokinetic profiles and computational approaches

Vassily Hatzimanikatis, Ljubisa Miskovic, Aikaterini Zisaki

Drug discovery and development is a high-risk enterprise that requires significant investments in capital, time and scientific expertise. The studies of xenobiotic metabolism remain as one of the main topics in the research and development of drugs, cosmet ...

Bentham Science Publishers2015

The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-beta peptides

Patrick Fraering

Known gamma-secretase inhibitors or modulators display an undesirable pharmacokinetic profile and toxicity and have therefore not been successful in clinical trials for Alzheimer's disease (AD). So far, no compounds from natural products have been identifi ...

Nature Publishing Group2015