Rohitukine is a chromone alkaloid with antiproliferative, anti-inflammatory, and immunomodulatory activities. Although several rohitukine derivatives are being investigated as potent anticancer leads, the potential antitumor activity of the naturally occurring rohitukine-N-oxide has yet to be evaluated.
Transforming growth factor β1 (TGF-β1) is a key mediator of the fibrotic response, and its dysregulation drives the formation of the fibrotic niche, which impairs the capacity of tissue repair, regeneration and homeostasis.
Integrin alphavbeta3 and aminopeptidase N (CD13) are important biomarkers involved in tumor angiogenesis, tumor growth and metastasis. Peptides RGD (Arg-Gly-Asp) and NGR (Asn-Gly-Arg) are the most studied peptides for targeting integrin alphavbeta3 and CD13, respectively.
Retinoic acid (RA) is fundamental to maintain immune homeostasis. In this process, RA induces regulatory T cells and promotes tolerance, but depending on the conditions, RA may also promote inflammation and tissue damage.
Ephrin type-A receptor 2 (EphA2) is a type I transmembrane glycoprotein highly expressed in a wide range of tumors such as bladder, pancreatic, esophageal, colorectal, or non-small-cell lung cancer, among others. Furthermore, in most normal tissues, EphA2 is found at low levels and plays a relevant role in carcinogenesis control and tumor progression modulation.
Bicycle radionuclide conjugates (BRCs) have been developed as a unique radiotheranostic modality for imaging and targeting of proteins overexpressed by tumors, and they possess favorable drug-like properties allowing for effective delivery of radioisotopes. Researchers from Bicycletx Ltd. recently presented a new BRC that targets ephrin type-A receptor 2 (EphA2), named BCY-18469.
Molecular glue degraders are compounds intended to prompt the degradation of E3 ubiquitin ligases by engaging and modifying their surface. Molecular glue-induced protein degradation is considered an emerging strategy in drug discovery.
Researchers from Ashvattha Therapeutics LLC recently reported on ASH-41020, a new dendranib compound acting as a CSF-1R inhibitor with anti-inflammatory and immunomodulatory effects.
Researchers from Sichuan University synthesized new pyrazole amides based on the previously described NADH-ubiquinone oxidoreductase (complex I, CI) inhibitor IACS-010759. Subsequent optimization resulted in the identification of SCAL-255 and SCAL-266 as lead candidates with potent CI inhibitory activity.
A different class of antibiotics could ease the increasing resistance triggered by some gram-negative bacteria. LpxC inhibitors are not new, but all attempts to develop them have failed due to cardiovascular toxicity or ineffectiveness. A modification of the structure of these compounds may have solved the problem. Duke University scientists demonstrated the preclinical safety and efficacy of an LpxC inhibitor candidate against a wide selection of these pathogens.
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