Synthesis of novel 1H-Pyrazolo[3,4-b]pyridine derivatives as DYRK 1A/1B inhibitors

Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133

(2020) Yahu A. Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Modulation of the Wnt pathway through inhibition of CLK2 and DYRK1A by lorecivivint as a novel, potentially disease-modifying approach for knee osteoarthritis treatment

(2019) V. Deshmukh et al.   OSTEOARTHRITIS AND CARTILAGE

LncRNA OIP5-AS1 regulates radioresistance by targeting DYRK1A through miR-369-3p in colorectal cancer cells

(2018) Yanmei Zou et al.   EUROPEAN JOURNAL OF CELL BIOLOGY

Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics

(2018) Dnyandev B. Jarhad et al.   JOURNAL OF MEDICINAL CHEMISTRY

DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives

(2018) Fernanda Neumann et al.   Scientific Reports

Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity

(2018) Kunal Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation

(2018) Kunal Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors

(2018) Anna Czarna et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dyrk1B overexpression is associated with breast cancer growth and a poor prognosis

(2017) Yingying Chen et al.   HUMAN PATHOLOGY

Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma

(2017) Qingqing Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of DYRK1A Stimulates Human β-Cell Proliferation

(2016) Ercument Dirice et al.   DIABETES

Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors To Explore a MEK Resistance Hypothesis

(2015) Jason G. Kettle et al.   JOURNAL OF MEDICINAL CHEMISTRY

A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication

(2015) Peng Wang et al.   NATURE MEDICINE

Inhibition of DYRK1A and GSK3B induces human β-cell proliferation

(2015) Weijun Shen et al.   Nature Communications

Dyrk1A induces pancreatic β cell mass expansion and improves glucose tolerance

(2014) Latif Rachdi et al.   CELL CYCLE

A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr286, not Thr288

(2013) Anne L. Ashford et al.   BIOCHEMICAL JOURNAL

Pyrido[2,3-d]pyrimidines: Discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors

(2013) Kevin Anderson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Mirk/dyrk1B Kinase in Ovarian Cancer

(2013) Eileen Friedman   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Development of DANDYs, New 3,5-Diaryl-7-azaindoles Demonstrating Potent DYRK1A Kinase Inhibitory Activity

(2013) Stéphanie Gourdain et al.   JOURNAL OF MEDICINAL CHEMISTRY

New kinase targets for Alzheimer's disease

(2013) Monica Hoyos Flight   NATURE REVIEWS DRUG DISCOVERY

Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer’s?

(2012) Breland Smith et al.   ACS Chemical Neuroscience

Selectivity, Cocrystal Structures, and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine B

(2012) Tania Tahtouh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)

(2011) Andrew S. Rosenthal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

DYRK family of protein kinases: evolutionary relationships, biochemical properties, and functional roles

(2010) Sergi Aranda et al.   FASEB JOURNAL

The role of DYRK1A in neurodegenerative diseases

(2010) Jerzy Wegiel et al.   FEBS Journal

Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A

(2010) Yasushi Ogawa et al.   Nature Communications

The Kinase Mirk/dyrk1B: A Possible Therapeutic Target in Pancreatic Cancer

(2010) Eileen Friedman   Cancers

Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation

(2009) Nora Göckler et al.   FEBS Journal

Role for DYRK family kinases on regulation of apoptosis

(2008) Kiyotsugu Yoshida   BIOCHEMICAL PHARMACOLOGY

Overexpression of Dyrk1A contributes to neurofibrillary degeneration in Down syndrome

(2008) Fei Liu et al.   FASEB JOURNAL