Targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 with a highly selective inhibitor for the treatment of prostate cancer

K Yuan, Z Li, W Kuang, X Wang, M Ji, W Chen… - Nature …, 2022 - nature.com
Prostate cancer (PCa) is one of the most prevalent cancers in men worldwide, and hormonal
therapy plays a key role in the treatment of PCa. However, the drug resistance of hormonal …

Discovery of Potent, Selective, and Orally Bioavailable DYRK2 Inhibitors for the Treatment of Prostate Cancer

K Yuan, F Xia, Q Li, M Zheng, H Shen… - Journal of Medicinal …, 2023 - ACS Publications
Prostate cancer (PCa) seriously threatens male health, and targeting dual-specificity
tyrosine phosphorylation-regulated kinase 2 (DYRK2) has been verified to reduce PCa …

Discovery of potent DYRK2 inhibitors with high selectivity, great solubility, and excellent safety properties for the treatment of prostate cancer

K Yuan, H Shen, M Zheng, F Xia, Q Li… - Journal of Medicinal …, 2023 - ACS Publications
Prostate cancer (PCa) is a common male cancer with high incidence and mortality, and
hormonal therapy as the major treatment for PCa patients is troubled by the inevitable …

The tumor suppressor NKX3. 1 is targeted for degradation by DYRK1B kinase

LN Song, J Silva, A Koller, A Rosenthal, EI Chen… - Molecular Cancer …, 2015 - AACR
Abstract NKX3. 1 is a prostate-specific homeodomain protein and tumor suppressor whose
expression is reduced in the earliest phases of prostatic neoplasia. NKX3. 1 expression is …

Targeting the DYRK1A kinase prevents cancer progression and metastasis and promotes cancer cells response to G1/S targeting chemotherapy drugs

AJ Laham, R El-Awady, M Saber-Ayad, N Wang… - NPJ Precision …, 2024 - nature.com
Metastatic cancer remains incurable as patients eventually loose sensitivity to targeted
therapies and chemotherapies, further leading to poor clinical outcome. Thus, there is a …

Structure-guided discovery of potent and selective DYRK1A inhibitors

C Weber, M Sipos, A Paczal, B Balint… - Journal of medicinal …, 2021 - ACS Publications
The kinase DYRK1A is an attractive target for drug discovery programs due to its implication
in multiple diseases. Through a fragment screen, we identified a simple biaryl compound …

Function and inhibition of DYRK1A: emerging roles of treating multiple human diseases

Y Yang, X Fan, Y Liu, D Ye, C Liu, H Yang, Z Su… - Biochemical …, 2023 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is an evolutionarily
conserved protein kinase and the most studied member of the Dual-specificity tyrosine …

DYRK1A modulates c-MET in pancreatic ductal adenocarcinoma to drive tumour growth

J Luna, J Boni, M Cuatrecasas, X Bofill-De Ros… - Gut, 2019 - gut.bmj.com
Background and aims Pancreatic ductal adenocarcinoma (PDAC) is a very aggressive
tumour with a poor prognosis using current treatments. Targeted therapies may offer a new …

Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry

T Wei, J Wang, R Liang, W Chen, Y Chen, M Ma, A He… - Elife, 2022 - elifesciences.org
The dual-specificity tyrosine phosphorylation-regulated kinase DYRK2 has emerged as a
critical regulator of cellular processes. We took a chemical biology approach to gain further …

Updating dual-specificity tyrosine-phosphorylation-regulated kinase 2 (DYRK2): molecular basis, functions and role in diseases

A Correa-Sáez, R Jiménez-Izquierdo… - Cellular and Molecular …, 2020 - Springer
Members of the dual-specificity tyrosine-regulated kinase (DYRKs) subfamily possess a
distinctive capacity to phosphorylate tyrosine, serine, and threonine residues. Among the …