High levels of adenosine known to stimulate tumor immunoevasion are formed by the ecto-5’-nucleotidase enzyme (CD73) conversion of adenosine monophosphate to adenosine. CD73 is a cell surface enzyme that is overexpressed in many cancer types where this overexpression has been correlated with a poor prognosis.
Neuroblastoma is among the deadliest cancers in infants, with frequent relapse and long-term survival being <10%. Recently, it has been found that protein RD3 is constitutively expressed in healthy adult and fetal tissues beyond the retina, and it follows a gradient expression from high to low levels in ganglioneuroma and neuroblastoma.
Triple-negative breast cancer (TNBC) constitutes the most aggressive form of breast cancer and presents a high frequency of relapse. The available treatment options are limited and accompanied by resistance and significant treatment side effects.
Researchers from Jacobio Pharmaceuticals Co. Ltd. have reported preclinical data for JAB-X1800, an immunostimulatory antibody-drug conjugate (iADC) targeting CD73. JAB-X1800 was developed using an anti-CD73 monoclonal antibody (MAb) for targeted delivery of a highly potent noncyclic dinucleotide STING agonist payload, JAB-27670.
The infiltration of regulatory T cells (Tregs) into the tumor microenvironment and a low ratio of effector T cells to Tregs is usually tied to tumor progression and poor prognosis. On the other hand, interleukin-2 receptor subunit α (IL-2-RA) is highly expressed on Tregs.
Researchers from Flare Therapeutics Inc. presented the discovery of a first-in-class covalent peroxisome proliferator-activated receptor γ (PPARγ) inverse agonist, FX-909, being developed for the treatment of urothelial cancer (UC). Synthesis and optimization of covalent lead series of agonists of the PPARγ lineage transcription factor led to the discovery of FX-909 as the lead covalent PPARγ inverse agonist with powerful repressive conformational biasing activity.
New and updated preclinical data presented at the American Association for Cancer Research annual meeting in Orlando, Fla., by: Fusion Pharmaceuticals, Ose Immunotherapeutics, Salarius Pharmaceuticals.
PHI-501 is a novel pan-RAF inhibitor being developed for acute myeloid leukemia. Big data, an artificial intelligence (AI)-based drug discovery platform and cell-based investigation identified PHI-501 as potentially useful against melanoma, and researchers from Pharos Ibio Co. Ltd. presented preclinical evaluation of the drug for this new indication.
Cyclin-dependent kinases (CDK) are serine/threonine kinases that act as regulatory enzymes involved in cell proliferation. The dysregulation of CDK activity occurs through overexpression of cyclin E1, a binding partner of CDK2, which is observed in several cancers such as high-grade serous ovarian cancer (HGSOC), bladder cancer, gastric cancer and estrogen receptor-positive breast cancer, among others. Selective inhibition of CDK2 may thus be considered a therapeutic approach to regaining cell cycle control.
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