Publications by authors named "G L Araldi"
Article Synopsis
- Researchers developed a new small molecule, ABI-171, targeting specific kinases related to idiopathic pulmonary fibrosis (IPF) to combat its progression and high mortality rates.
- In a mouse model, ABI-171 showed significant improvements in lung health, reducing fibrosis and inflammation, as well as weight loss in treated mice, whether given before or after disease onset.
- The treatment led to lower mortality rates and better overall lung function compared to current treatments like pirfenidone and EGCG, indicating ABI-171's potential as a promising therapy for IPF.
Article Synopsis
- Non-muscle myosin II (NMII) plays a crucial role in biological processes, but current therapeutic options are limited due to non-selective inhibitors like blebbistatin that affect both NMII and cardiac myosin II (CMII).
- Researchers developed a series of selective NMII inhibitors, notably MT-228, which demonstrates high brain penetration and effectiveness in preclinical models for stimulant use disorder, a condition lacking FDA-approved treatments.
- The structure of MT-228 binding to myosin II reveals its 17-fold selectivity for NMII over CMII, providing insights for future drug development and potential applications in various medical fields, including cancer and nerve regeneration.
Natural polyphenol derivatives such as those found in green tea have been known for a long time for their useful therapeutic activity. Starting from EGCG, we have discovered a new fluorinated polyphenol derivative () characterized by improved inhibitory activity against DYRK1A/B enzymes and by considerably improved bioavailability and selectivity. DYRK1A is an enzyme that has been implicated as an important drug target in various therapeutic areas, including neurological disorders (Down syndrome and Alzheimer's disease), oncology, and type 2 diabetes (pancreatic β-cell expansion).
View Article and Find Full Text PDFGreen tea and its natural components are known for their usefulness against a variety of diseases. In particular, the activity of main catechin Epigallocatechin gallate (EGCG) against Dual-specificity tyrosine-(Y)-phosphorylation Regulated Kinase-1A (DYRK1A) has been reported; here we are showing a structure-activity relationship (SAR) for EGCG against this molecular target. We have studied the influence of all four rings on the activity and the nature of its absolute geometry.
View Article and Find Full Text PDFIntroduction: Despite the widespread use of prostaglandin E(1) as an efficacious treatment for male erectile dysfunction for more than two decades, research on prostanoid function in penile physiology has been limited.
Aim: To characterize the pharmacological and physiological activity of novel subtype-selective EP and DP receptor agonists.
Methods: Radioligand binding and second messenger assays were used to define receptor subtype specificity of the EP and DP agonists.