Results 61 to 70 of about 12,487 (241)

Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Identification of highly selective type II kinase inhibitors is described. Two different chiral peptidomimetic scaffolds were introduced on the tail region of non-selective type II kinase inhibitor GNF-7 to enhance the selectivity.
Seo-Jung Han, Jae Eun Jung, Do Hee Oh, Minsup Kim, Jae-Min Kim, Kyung-Sook Chung, Hee-Soo Han, Jeong-Hun Lee, Kyung-Tae Lee, Hee Jin Jeong, In Ho Park, Eunkyeong Jeon, Jeon-Soo Shin, Dongkeun Hwang, Art E. Cho, Duck-Hyung Lee, Taebo Sim   +16 more
doaj   +1 more source

Targeting Lipopolysaccharide Transport Induces Membrane Lipid Remodeling and Sensitizes Acinetobacter baumannii to Colistin Treatment

Advanced Science, EarlyView.
This study identifies C4 as a lead inhibitor of the Lpt system. Notably, C4 potentiates colistin activity by disrupting LPS transport and remodeling phospholipid homeostasis, revealing a functional interplay between the Lpt and Mla systems. These findings establish a mechanistic link between Lpt inhibition and membrane lipid remodeling, positioning Lpt–
Jianya Luo, Hetianzi Zhang, Jinju Cai, Shuang Zhou, Haijie Zhang, Zhiqiang Wang, Yuan Liu   +6 more
wiley   +1 more source

Late‐Stage Functionalization of Peptides on the Solid Phase

Angewandte Chemie International Edition, EarlyView.
Peptide modifications are essential to control pharmacodynamic and pharmacokinetic properties of peptide drugs. Consequently, strategies that allow for efficient and rapid incorporation of non‐canonical modifications into peptides in parallel formats are highly sought after.
Marius Werner, Truc Lam Pham, Franziska Thomas   +2 more
wiley   +1 more source

Antiviral Activity of Anthranilamide Peptidomimetics against Herpes Simplex Virus 1 and a Coronavirus

Antibiotics, 2023
The development of potent antiviral agents is of utmost importance to combat the global burden of viral infections. Traditional antiviral drug development involves targeting specific viral proteins, which may lead to the emergence of resistant strains ...
Umme Laila Urmi, Samuel Attard, Ajay Kumar Vijay, Mark D. P. Willcox, Naresh Kumar, Salequl Islam, Rajesh Kuppusamy   +6 more
doaj   +1 more source

Peptidomimetic Thrombin Inhibitors [PDF]

Pathophysiology of Haemostasis and Thrombosis, 2003
The central position of thrombin in the coagulation cascade has made it a popular target for discovery of novel antithrombotic agents. Starting with hirudin, a natural peptide isolated from the medicinal leech, its shorter synthetic analogue hirulog, and argatroban,the first therapeutically used synthetic small-molecule thrombin active site inhibitor ...
openaire   +2 more sources

Pd(II)‐Catalyzed Strategies for the β‐Arylation of α‐Amino Acids: An Overview

Chemistry – A European Journal, EarlyView.
The graphical abstract summarizes the review “Pd(II)‐Catalyzed Strategies for the β‐Arylation of α‐Amino Acids: An Overview”, highlighting representative Pd(II)‐catalyzed methods for the β‐arylation of α‐amino acids. Key mechanistic features, substrate diversity, and synthetic relevance of these transformations are showcased. Abstract Metal‐catalyzed C─
Davide Illuminati, Claudio Trapella, Vinicio Zanirato, Virginia Cristofori, Anna Fantinati   +4 more
wiley   +1 more source

Phosphorescent Iridium Hydrazinonicotinic Acid (HYNIC) Complexes That Bind to Prostate Specific Membrane Antigen: Potential Photodynamic Therapy of Prostate Cancer

Chemistry – A European Journal, EarlyView.
A phosphorescent iridium(III) complex has been prepared with a 6‐hydrazinonicotinic acid (HYNIC) ligand tethered to a lysine‐ureido‐glutamatic acid pharmacophore, which binds to an enzyme, called prostate‐specific membrane antigen (PSMA), which is overexpressed in prostate cancer.
La'El Kimchi, Emily R. McGowan, Katherine A. Morgan, Jonathan M. White, Trevor A. Smith, Stacey E. Rudd, Paul S. Donnelly   +6 more
wiley   +1 more source

Peptidomimetic toolbox for drug discovery

Chemical Society Reviews, 2020
Local modifications, secondary structure mimetics and global restrictions are useful synthetic tools for peptidomimetic design.
Lenci, Elena, Trabocchi, Andrea
openaire   +2 more sources

Development of Peptidomimetics Targeting IAPs [PDF]

International Journal of Peptide Research and Therapeutics, 2006
Inhibitor of apoptosis proteins (IAPs) such as XIAP subvert apoptosis by binding and inhibiting caspases. Because occupation of the XIAP BIR3 peptide binding pocket by Smac abolishes the XIAP-caspase 9 interaction, it is a proapoptotic event of great therapeutic interest. An assay for pocket binding was developed based on the displacement of Smac 7-mer
Sharma, Sushil K., Straub, Christopher, Zawel, Leigh   +2 more
openaire   +2 more sources

Dynamic Control of Nucleic Acids Self‐Assembly and Expression Using Photoswitches

Chemistry – A European Journal, EarlyView.
We review here the recent progress made in the design of molecular photoswitches, and highlight their implementation for the dynamic control over nucleic acids self‐assembly and expression. ABSTRACT Synthetic nucleic acids have become readily available and now constitute versatile building blocks in materials science—where they can be used to engineer ...
Noemí Nogal, Hugo Laigle, Maxime Mansy, Sébastien Ulrich, Mathieu Surin   +4 more
wiley   +1 more source