Year: 2025
Type: article
Abstract: Dual‐specificity tyrosine phosphorylation‐regulated kinase 1A (DYRK1A) is a protein kinase that is ubiquitously expressed in human tissues and acts as a master regulator of cell proliferation and differentiation. DYRK1A might be associated with Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes and other neurodegenerative diseases. In search of novel and selective DYRK1A inhibitor scaffold, KTD‐092 are validated as a hit for DYRK1A inhibition. KTD‐092 shows good stability under various liver microsomes, and markedly reduces tau phosphorylation in a human neuroblastoma cell in a concentration‐dependent manner. Molecular binding mode of KTD‐092 to DYRK1A is also proposed.
DOI: 10.1002/bkcs.70018
Authors: Sujeong Hong, Subin Hwang, Rajath Cyriac, Hyunha Choi, Gahyeon Choi, Eun Hye Kim, Chaemi Lee, Seong Hwan Kim, Sunjoo Ahn, Chong Hak Chae, Jin Sook Song, Kwangho Lee
Language: English
Subfield: Physiology
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $3,470
Awards: G2369249591, G6321257798
OpenAlex ID: W4410780555