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.
Researchers from Peking University Cancer Hospital presented the discovery and preclinical evaluation of [124I]IMMU-132, a trophoblast cell surface antigen 2 (Trop2)-targeting molecular probe for micro-PET imaging.
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.
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.
Carbonic anhydrase IX (CAIX) is a transmembrane protein involved in cell proliferation and transformation that is expressed in clear-cell renal cell carcinoma (ccRCC), colorectal cancer (CRC), and other hypoxic tumor types, but has low expression in healthy tissues.
Lipids are “very diverse, but also vastly understudied,” Anne Brunet told the audience at the recent meeting on Aging Research and Drug Discovery. Advances in the ability to predict protein structures have fueled a much better understanding of the human proteome and its estimated 20,000 members. The lipidome is much larger, numbering maybe 100,000 total. And what those lipids do remains much more fuzzy. “Very little is known about their function, and especially their function during aging,” Brunet said. Slowly, however, technological advances are enabling researchers to understand the roles of lipids as well.
Pancreatic ductal adenocarcinoma (PDAC) is an exocrine pancreatic cancer with a poor prognosis and limited treatment options. There is a strong demand for new treatment strategies to overcome these challenges.
At the recent ERS meeting, researchers from Hilung Inc. and Ube Corp. presented preclinical data for the novel lysophospholipid LPA1 receptor antagonist, HL-001, being developed for the treatment of idiopathic pulmonary fibrosis (IPF).
Senescence of lung epithelial tissue translates into fibrinolysis reduction and loss of tissue repair, both drivers of pulmonary fibrotic diseases. Researchers from Tokushima University reported on the effect of ARV-825, a BRD4 degrader, as an antifibrotic agent in lung fibrosis.
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