[HTML][HTML] A new oxadiazole-based topsentin derivative modulates cyclin-dependent kinase 1 expression and exerts cytotoxic effects on pancreatic cancer cells

C Pecoraro, B Parrino, S Cascioferro, A Puerta, A Avan… - Molecules, 2021 - mdpi.com
Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal form of cancer characterized by
drug resistance, urging new therapeutic strategies. In recent years, protein kinases have …

[HTML][HTML] Defining the sensitivity landscape of EGFR variants to tyrosine kinase inhibitors

LEI An, Y Wang, G Wu, Z Wang, Z Shi, C Liu… - Translational …, 2023 - Elsevier
Tyrosine kinase inhibitor (TKI) is a standard treatment for patients with NSCLC harboring
constitutively active epidermal growth factor receptor (EGFR) mutations. However, most rare …

Bruton's tyrosine kinase inhibitors: a promising emerging treatment option for multiple sclerosis

E Carnero Contentti, J Correale - Expert opinion on emerging drugs, 2020 - Taylor & Francis
Multiple Sclerosis (MS) is a chronic inflammatory disease of the central nervous system
(CNS) leading to demyelination and neurodegeneration. Although its etiology is not fully …

Synthesis of novel pyrido [2, 3-d] pyrimidine-thiazolidine-1, 2, 3-triazoles: Potent EGFR targeting anticancer agents

SR Bandi, R Kapavarapu, R Palabindela… - Journal of Molecular …, 2023 - Elsevier
In this study, we designed and synthesized a number of novel pyrido [2, 3-d] pyrimidine-
thiazolidine-1, 2, 3-triazole derivatives and investigated them in vitro for their inhibitory …

[HTML][HTML] Epidermal growth factor receptor: key to selective intracellular delivery

AA Rosenkranz, TA Slastnikova - Biochemistry (Moscow), 2020 - Springer
Epidermal growth factor receptor (EGFR) is an integral surface protein mediating cellular
response to a number of growth factors. Its overexpression and increased activation due to …

[HTML][HTML] Recent developments in anticancer kinase inhibitors based on the pyrazolo [3, 4-d] pyrimidine scaffold

DJ Baillache, A Unciti-Broceta - RSC medicinal chemistry, 2020 - pubs.rsc.org
Pyrazolo [3, 4-d] pyrimidines have become of significant interest for the medicinal chemistry
community as a privileged scaffold for the development of kinase inhibitors to treat a range …

[HTML][HTML] Anti-fibrotic activity of a rho-kinase inhibitor restores outflow function and intraocular pressure homeostasis

G Li, C Lee, AT Read, K Wang, J Ha, M Kuhn, I Navarro… - Elife, 2021 - elifesciences.org
Glucocorticoids are widely used as an ophthalmic medication. A common, sight-threatening
adverse event of glucocorticoid usage is ocular hypertension, caused by dysfunction of the …

An updated patent review of VEGFR-2 inhibitors (2017-present)

TA Farghaly, WA Al-Hasani… - Expert opinion on …, 2021 - Taylor & Francis
Introduction: Angiogenesis is a vital process for cellular functions in both physiological and
pathophysiological conditions and is one of the hallmarks of cancer progression and …

Protein kinase inhibitors for amyotrophic lateral sclerosis therapy

V Palomo, V Nozal, E Rojas‐Prats… - British Journal of …, 2021 - Wiley Online Library
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disorder that causes the
progressive loss of motoneurons and, unfortunately, there is no effective treatment for this …

PRM-LIVE with trapped ion mobility spectrometry and its application in selectivity profiling of kinase inhibitors

H Zhu, SB Ficarro, WM Alexander, LE Fleming… - Analytical …, 2021 - ACS Publications
Parallel reaction monitoring (PRM) has emerged as a popular approach for targeted protein
quantification. With high ion utilization efficiency and first-in-class acquisition speed, the …