Researchers from Jinggangshan University reported on the synthesis of a series of novel celastrol derivatives that led to the identification of [I] as the main compound with water solubility of 11.8 mg/mL and antiproliferative effects accounting for IC50 values of 0.58, 0.32, 0.32, 0.75, 0.29 and 4.30 µM against BEL-7402, AGS, HCT 116, HepG-2, MGC-803 and A549 human cancer cell lines, respectively.
Harbour Biomed Ltd. has received FDA clearance of its IND application to commence a phase I trial of HBM-9033 in advanced solid tumors. Developed in collaboration with Medilink Therapeutics (Suzhou) Co. Ltd., HBM-9033 is an antibody-drug conjugate that specifically targets human mesothelin (MSLN), an upregulated tumor-associated antigen in various solid tumors, including mesothelioma, ovarian cancer, lung cancer, breast cancer and pancreatic cancers. The fully human monoclonal antibody in HBM-9033, generated from the Harbour Mice platform, binds preferably to membrane bond MSLN over soluble MSLN, which minimizes the interference of the shedding MSLN on the binding and internalization of the membrane bond MSLN.
Researchers from China Pharmaceutical University have reported the discovery of novel spleen tyrosine kinase (SYK) inhibitors as potential candidates for the treatment of hematological malignancies.
One of the key advances in regenerative medicine has been the engraftment of external epithelial stem cells to supplement or replace damaged native cells. However, the difficulty in engrafting internal tissues has hindered the long-term rescue of diseased internal epithelia, such as those in the respiratory airways.
Both oxidative stress and inflammation are the main hallmarks in the development of heart failure. Researchers from the Hefei University of Technology have reported on the discovery and optimization of a series of pterostilbene derivatives intended to be used in heart failure.
Chengdu Easton Biopharmaceuticals Co. Ltd. has described lysine-specific histone demethylase 1A (KDM1A, LSD1) inhibitors reported to be useful for the treatment of cancer.
Merck KGaA has divulged proteolysis targeting chimeras (PROTACs) compounds comprising an E3 ubiquitin ligase binding agent coupled to methionine aminopeptidase-2 (MNPEP; MetAP2) targeting moiety via a linker reported to be useful for the treatment of cancer, rheumatoid arthritis, psoriasis, osteoporosis, diabetes, obesity, malaria and benign prostatic hyperplasia, among others.
Gilead Sciences Inc. has identified protein mono-ADP-ribosyltransferase TIPARP (PARP-7; ARTD14) inhibitors reported to be useful for the treatment of cancer.
Wuhan LL Science & Technology Development Co. Ltd. has synthesized mannan-binding lectin serine protease 2 (MASP2) inhibitors reported to be useful for the treatment of lupus nephritis and IgA nephropathy, among others.
Adlai Nortye Pharmaceutical Co. Ltd. has disclosed Wnt signaling inhibitors reported to be useful for the treatment of cancer, immunological and inflammatory disorders.