One nucleotide substitution in pseudoexon 5 of HLA-DQB1*06:02:01:01 results in a novel allele, HLA-DQB1*06:02:01:32.
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http://dx.doi.org/10.1111/tan.15032 | DOI Listing |
J Med Chem
January 2025
Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic v.v.i., Prague 160 00, Czech Republic.
Itaconate, an endogenous immunomodulator from the tricarboxylic acid (TCA) cycle, shows therapeutic effects in various disease models, but is highly polar with poor cellular permeability. We previously reported a novel, topical itaconate derivative, SCD-153, for the treatment of alopecia areata. Here, we present the discovery of orally available itaconate derivatives for systemic and skin disorders.
View Article and Find Full Text PDFJ Med Chem
January 2025
State Key Laboratory of Advanced Drug Delivery and Release Systems, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
The ligand-binding pocket of the androgen receptor (AR) is the targeting site of all clinically used AR antagonists. However, various drug-resistant mutations emerged in the pocket. We previously reported a new targeting site at the dimer interface of AR (dimer interface pocket) and identified a novel antagonist M17-B15 that failed in oral administration.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Université de Caen Normandie, Normandie Univ., CERMN, 14000, Caen, France. Electronic address:
Alzheimer's disease (AD) remains a significant healthcare challenge, necessitating innovative therapeutic approaches to address its complex and multifactorial nature. Traditional drug discovery strategies targeting single molecular targets are not sufficient for the effective treatment of AD. In recent years, MTDLs have emerged as promising candidates for AD therapy, aiming to simultaneously modulate multiple pathological targets.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education and School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, 450001, China. Electronic address:
Gastric cancer remains one of the global health threats for human beings. However, the therapeutic efficacy of the widely-used chemotherapy is usually limited due to the lack of specificity and the related toxicity. Only limited therapeutic agents were demonstrated to show selective and potent inhibitory activity to gastric cancer cells.
View Article and Find Full Text PDFDrug Metab Pharmacokinet
December 2024
Graduate School of Pharmaceutical Sciences, Nagoya City University, Japan. Electronic address:
The intestines are an important organ with a variety of functions. For drug discovery research, experimental animals and Caco-2 cells derived from a human colon carcinoma may be used to evaluate the absorption and safety of orally administered drugs. These systems have issues, such as species differences with humans in experimental animals, variations in gene expression patterns, very low drug-metabolizing activities in Caco-2 cells, and the recent trend toward reduced animal testing.
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