University of Florida researchers have synthesized proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)- and apoptosis regulator Bcl-2-targeting moiety.
To address the dual bottlenecks of immunosuppressive cell infiltration and impaired T-cell function in the tumor microenvironment (TME), researchers from the School of Pharmaceutical Sciences of Sun Yat-sen University (China) aimed to develop an engineered bispecific peptide-nanozyme conjugate (BsPNEC) targeting PD-L1 and CXCR1/2.
In a recent paper, researchers from the University of Perugia and University of Naples Federico II have shown how the use of leukemia inhibitory factor receptor (LIFR) antagonists dismantles the pro-CAF programs in pancreatic ductal adenocarcinoma (PDAC) to avoid its progression.
Bone metastasis represents a challenge in cancer therapy because of the independency of immunosuppression, neuropathic pain and osteolytic destruction. Recent evidence has suggested the tumor microenvironment can be reshaped through the activation of stimulator of interferon genes protein (STING) and pyroptosis induction.
Beijing Avistone Pharmaceuticals Biotechnology Co. Ltd. has patented HER2 (erbB2) Ex20Ins mutant inhibitors. They are reported to be useful for the treatment of cancer, atherosclerosis and pulmonary fibrosis.
Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have divulged new isoindoline proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)-targeting moiety. They are reported to be useful for the treatment of cancer.
Work at Apertor Pharmaceuticals Inc. has led to the preparation of new hetero-bifunctional compounds acting as mTOR complex 1 (mTORC1) inhibitors potentially useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to an estrogen receptor-α (ERα)-targeting moiety. They are reported to be useful for the treatment of breast cancer.
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