Researchers from University Hospital Basel and Universitätsklinikum Ulm presented the discovery of novel radiotheragnostic candidates targeting C-X-C chemokine receptor 4 (CXCR4), which is highly expressed in various cancers and has been linked to poor prognosis.
Researchers from Huazhong University of Science and Technology presented the discovery and preclinical evaluation of a novel peptide PET tracer targeting LAG-3, [68Ga]NOTA-XH05, being developed as a candidate for evaluating the efficacy of cancer immunotherapy.
The discovery of new 68Ga-labeled CD38-targeted peptides for PET imaging was recently discussed by researchers from Peking University First Hospital and China National Center For Nanoscience & Technology.
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.
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