Cyclin-dependent kinase 2 inhibitors in cancer therapy: an update

S Tadesse, EC Caldon, W Tilley… - Journal of medicinal …, 2018 - ACS Publications
Cyclin-dependent kinase 2 (CDK2) drives the progression of cells into the S-and M-phases
of the cell cycle. CDK2 activity is largely dispensable for normal development, but it is …

GSK-3 inhibitors: preclinical and clinical focus on CNS

H Eldar-Finkelman, A Martinez - Frontiers in molecular neuroscience, 2011 - frontiersin.org
Inhibiting glycogen synthase kinase-3 (GSK-3) activity via pharmacological intervention has
become an important strategy for treating neurodegenerative and psychiatric disorders. The …

Marine natural products

JW Blunt, BR Copp, MHG Munro, PT Northcote… - Natural product …, 2010 - pubs.rsc.org
Covering: 2008. Previous review: Nat. Prod. Rep., 2009, 26, 170This review covers the
literature published in 2008 for marine natural products, with 829 citations (613 for the …

DYRK1A, a Dosage-Sensitive Gene Involved in Neurodevelopmental Disorders, Is a Target for Drug Development in Down Syndrome

A Duchon, Y Herault - Frontiers in behavioral neuroscience, 2016 - frontiersin.org
Down syndrome (DS) is one of the leading causes of intellectual disability, and patients with
DS face various health issues, including learning and memory deficits, congenital heart …

Variolins and related alkaloids

SR Walker, EJ Carter, BC Huff, JC Morris - Chemical reviews, 2009 - ACS Publications
The phosphorylation of proteins on serine, threonine, and tyrosine residues by the 518
protein kinases encoded in the human genome constitutes one of the major mechanisms …

Recent developments in the biology and medicinal chemistry of CDK9 inhibitors: an update

T Wu, Z Qin, Y Tian, J Wang, C Xu, Z Li… - Journal of medicinal …, 2020 - ACS Publications
Cyclin-dependent kinase 9 (CDK9), which regulates transcriptional elongation, is an
attractive therapeutic target for many cancers, especially for cancers driven by transcriptional …

The azaindole framework in the design of kinase inhibitors

JY Mérour, F Buron, K Plé, P Bonnet, S Routier - Molecules, 2014 - mdpi.com
This review article illustrates the growing use of azaindole derivatives as kinase inhibitors
and their contribution to drug discovery and innovation. The different protein kinases which …

Cyclin dependent kinase 9 inhibitors for cancer therapy: miniperspective

YA Sonawane, MA Taylor, JV Napoleon… - Journal of medicinal …, 2016 - ACS Publications
Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly
2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has …

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors as potential therapeutics

DB Jarhad, KK Mashelkar, HR Kim… - Journal of medicinal …, 2018 - ACS Publications
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a member of an
evolutionarily conserved family of protein kinases that belongs to the CMGC group of …

Selective DYRK1A inhibitor for the treatment of Type 1 Diabetes: Discovery of 6-azaindole derivative GNF2133

YA Liu, Q Jin, Y Zou, Q Ding, S Yan… - Journal of medicinal …, 2020 - ACS Publications
Autoimmune deficiency and destruction in either β-cell mass or function can cause
insufficient insulin levels and, as a result, hyperglycemia and diabetes. Thus, promoting β …