Prolonging duration of action of inhaled drugs is a challenging endeavor and guidance for medicinal chemistry teams is very limited, particularly if the site of action is intracellular. Herein, we identified recent literature reports of newly designed inhaled compounds with intracellular targets and summarized learnings from different approaches and strategies undertaken by medicinal chemistry teams. We highlight key properties that have shown to lead to longer duration of action and provide guidance on the best strategy to follow while designing a new inhaled drug with an intracellular target.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2022.128627 | DOI Listing |
Breast Cancer Res
January 2025
College of Pharmacy, Seoul National University, Seoul, 08826, South Korea.
Background: Patients with estrogen receptor (ER)-positive breast cancer (BC) can be treated with endocrine therapy targeting ER, however, metastatic recurrence occurs in 25% of the patients who have initially been treated. Secreted proteins from tumors play important roles in cancer metastasis but previous methods for isolating secretory proteins had limitations in identifying novel targets.
Methods: We applied an in situ secretory protein labeling technique using TurboID to analyze secretome from tamoxifen-resistant (TAMR) BC.
BMC Chem
January 2025
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nile Valley University (NVU), El Fayoum, 63518, Egypt.
Coronavirus disease 2019 (COVID-19), an extremely contagious illness, has posed enormous challenges to healthcare systems around the world. Although the evidence on COVID-19 management is growing, antiviral medication is still the first line of treatment. Therefore, it is critical that effective, safe, and tolerable antivirals be available to treat early COVID-19 and stop its progression.
View Article and Find Full Text PDFBMC Complement Med Ther
January 2025
School of Pharmaceutical Sciences, University Sains Malaysia, Gelugor, Malaysia.
Background: Nonalcoholic steatohepatitis (NASH) is a severe form of nonalcoholic fatty liver disease (NAFLD) characterized by damage and inflammation of hepatocytes. Some medicinal plants have shown antioxidant and anti-inflammatory effects on liver cells. We aimed to investigate the hepatoprotective effect of Heptex® capsules containing 200 mg of Dukung Anak (a powdered extract from aerial parts of Phyllanthus niruri) and 100 mg of Milk Thistle (a powdered extract from fruits of Silybum marianum) in patients with an apparent risk factor for NASH.
View Article and Find Full Text PDFNat Struct Mol Biol
January 2025
Institute of Biophysical Chemistry and Center for Biomolecular Magnetic Resonance, Goethe University, Frankfurt, Germany.
Infection of cells with high-risk strains of the human papillomavirus (HPV) causes cancer in various types of epithelial tissue. HPV infections are responsible for ~4.5% of all cancers worldwide.
View Article and Find Full Text PDFNat Commun
January 2025
NCI RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, Frederick, MD, USA.
Mutations in RAS and PI3Kα are major drivers of human cancer. Their interaction plays a crucial role in activating PI3Kα and amplifying the PI3K-AKT-mTOR pathway. Disrupting RAS-PI3Kα interaction enhances survival in lung and skin cancer models and reduces tumor growth and angiogenesis, although the structural details of this interaction remain unclear.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!