CK2 Chemical Probes: Past, Present, and Future

HW Ong, DH Drewry, AD Axtman - Kinases and Phosphatases, 2023 - mdpi.com
Protein kinase casein kinase 2 (CK2/CSNK2) is a pleiotropic kinase involved in many
cellular processes and, accordingly, has been identified as a potential target for therapeutic …

Illuminating function of the understudied druggable kinome

SM Gomez, DH Drewry, TM Willson, MB Major… - Drug Discovery …, 2024 - Elsevier
The human kinome, with more than 500 proteins, is crucial for cell signaling and disease.
Yet, about one-third of kinases lack in-depth study. The Data and Resource Generating …

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication

HW Ong, X Yang, JL Smith… - Journal of Medicinal …, 2024 - ACS Publications
The pyrazolo [1, 5-a] pyrimidine scaffold is a promising scaffold to develop potent and
selective CSNK2 inhibitors with antiviral activity against β-coronaviruses. Herein, we …

Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 …

A Castano, M Silvestre, CI Wells, JL Sanderson… - Elife, 2023 - elifesciences.org
Pathological loss-of-function mutations in cyclin-dependent kinase-like 5 (CDKL5) cause
CDKL5 deficiency disorder (CDD), a rare and severe neurodevelopmental disorder …

Recent Advances in the Discovery of CK2 Inhibitors

MA Al-Qadhi, TAA Yahya, HB El-Nassan - ACS omega, 2024 - ACS Publications
CK2 is a vital enzyme that phosphorylates a large number of substrates and thereby controls
many processes in the body. Its upregulation was reported in many cancer types. Inhibitors …

Naturally Derived Phenethyl Isothiocyanate Modulates Induction of Oxidative Stress via Its N-Acetylated Cysteine Conjugated form in Malignant Melanoma

S Kyriakou, N Demosthenous, T Amery, KJ Stewart… - Antioxidants, 2024 - mdpi.com
Phenethyl isothiocyanate (PEITC) is a secondary metabolic product yielded upon the
hydrolysis of gluconasturtiin and it is highly accumulated in the flowers of watercress. The …

[HTML][HTML] Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2

HW Ong, X Yang, JL Smith, S Taft-Benz, S Howell… - Molecules, 2024 - mdpi.com
The host kinase casein kinase 2 (CSNK2) has been proposed to be an antiviral target
against β-coronaviral infection. To pharmacologically validate CSNK2 as a drug target in …

[HTML][HTML] Targeting Nav1. 7 and Nav1. 8 with a PIKfyve inhibitor to Reverse inflammatory and neuropathic pain

EJ Rodríguez-Palma, S Loya-Lopez, SM Min… - Neurobiology of Pain, 2024 - Elsevier
Abstract PIKfyve (1-phosphatidylinositol 3-phosphate 5-kinase), a lipid kinase, plays an
important role in generating phosphatidylinositol (3, 5)-bisphosphate (PI (3, 5) P 2). SGC …

Identification of 4-(6-((2-methoxyphenyl) amino) pyrazin-2-yl) benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3

KA Galal, A Krämer, BG Strickland, JL Smith… - Bioorganic & Medicinal …, 2024 - Elsevier
We report the synthesis of 2, 6-disubstituted pyrazines as potent cell active CSNK2A
inhibitors. 4′-Carboxyphenyl was found to be the optimal 2-pyrazine substituent for …

Development of a Second-Generation, In Vivo Chemical Probe for PIKfyve

SM Min, FM Bashore, JL Smith, TM Havener, S Howell… - 2024 - chemrxiv.org
We optimized our highly potent and cell-active chemical probe for phosphatidylinositol-3-
phosphate 5-kinase (PIKfyve), SGC-PIKFYVE-1, resulting in compounds with improved …