Harnessing acylhydrazone-oxime exchange reaction to achieve diverse synthesis of glycosite-specific antibody-drug conjugates.

Glycosite-specific antibody-drug conjugates (gsADCs), which carry cytotoxic payloads at the conserved -glycosylation site, N297, of an IgG, have emerged as a promising ADC format with better therapeutic index. Conjugating the payloads aldehyde-based chemistry is more friendly to IgGs, and has been widely investigated. However, the efficiency of introducing an aldehyde tag at the N297 site is poor due to the complicated procedures required, such as the multiple-enzyme-catalyzed IgG glycoengineering process and the successive oxidation step, which always results in heterogeneous products and poor stability.

Transcriptome-wide association identifies as a regulator of mitophagy in non-syndromic cleft lip with or without palate.

This study investigated pathogenic genes associated with non-syndromic cleft lip with or without cleft palate (NSCL/P) through transcriptome-wide association studies (TWAS). By integrating expression quantitative trait loci (eQTL) data with genome-wide association study (GWAS) data, we identified key susceptibility genes, including . Notably, the variant rs12884809 G>A was associated with an increased risk of NSCL/P by enhancing the binding of the transcription factor ELK1 to the promoter, thereby activating its expression.

Sesquiterpene Monomers and Dimers from The Flower of Inula japonica Thunb. With Selective Antiproliferation Against Breast Cancer Cells.

A total of 34 sesquiterpene derivates were obtained from the flower of Inula japonica Thunb. Compounds 2, 14-34 were identified as sesquiterpene monomers, while the other 12 isolates (1, 3-13) were characterized as sesquiterpene dimers. Among them, japonicone Z (1), an present undescribed sesquiterpene dimer, and another undescribed monomer, japonicol A (2), were discovered.