Revisiting protein kinase–substrate interactions: Toward therapeutic development

PSL de Oliveira, FAN Ferraz, DA Pena, DT Pramio… - Science …, 2016 - science.org
Despite the efforts of pharmaceutical companies to develop specific kinase modulators, few
drugs targeting kinases have been completely successful in the clinic. This is primarily due …

Computational targeting of allosteric site of MEK1 by quinoline‐based molecules

R Singh, VK Bhardwaj, R Purohit - Cell Biochemistry and …, 2022 - Wiley Online Library
MEK1 is an attractive target due to its role in selective extracellular‐signal‐regulated kinase
phosphorylation, which plays a pivotal role in regulating cell proliferation. Another benefit of …

The cytomegalovirus protein kinase pUL97: host interactions, regulatory mechanisms and antiviral drug targeting

M Steingruber, M Marschall - Microorganisms, 2020 - mdpi.com
Human cytomegalovirus (HCMV) expresses a variety of viral regulatory proteins that
undergo close interaction with host factors including viral-cellular multiprotein complexes …

Novel anticancer fused pyrazole derivatives as EGFR and VEGFR-2 dual TK inhibitors

NM Saleh, MG El-Gazzar, HM Aly, RA Othman - Frontiers in chemistry, 2020 - frontiersin.org
EGFR and VEGFR-2 represent promising targets for cancer treatment as they are very
important in tumor development as well as in angiogenesis and metastasis. In this work, 6 …

Discovery of novel dual mechanism of action Src signaling and tubulin polymerization inhibitors (KX2-391 and KX2-361)

MP Smolinski, Y Bu, J Clements, IH Gelman, T Hegab… - 2018 - ACS Publications
The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an
elusive goal. Herein we describe the discovery of two such clinical candidates that inhibit the …

Design, synthesis, and docking studies of novel pyrazole-based scaffolds and their evaluation as VEGFR2 inhibitors in the treatment of prostate cancer

DH Soliman, MS Nafie - RSC advances, 2023 - pubs.rsc.org
Since VEGFR-2 plays a crucial role in tumor growth, angiogenesis, and metastasis, it is a
prospective target for cancer treatment. In this work, a series of 3-phenyl-4-(2-substituted …

Pyrazolo [3, 4-d] pyrimidine derivatives as EGFRT790M and VEGFR-2 dual TK inhibitors: Design, synthesis, molecular docking, ADMET profile and anticancer …

D Adel, K El-Adl, T Nasr, TM Sakr, W Zaghary - Journal of Molecular …, 2023 - Elsevier
Abstract Seventeen new pyrazolo [3, 4-d] pyrimidine derivatives have been designed,
created and tested as dual VEGFR-2 and EGFR inhibitors for their anticancer special effects …

In vitro and in silico investigation of anti-biofilm activity of Citrus macroptera fruit extract mediated silver nanoparticles

M Majumdar, SA Khan, SC Biswas, DN Roy… - Journal of Molecular …, 2020 - Elsevier
Bacteria produce biofilm not only to infect the host and spread into a new substratum but
also protect themselves against conventional antibiotics. Green silver nanoparticles …

Recent advances of small-molecule c-Src inhibitors for potential therapeutic utilities

XW Dang, JL Duan, E Ye, ND Mao, RR Bai, X Zhou… - Bioorganic …, 2024 - Elsevier
Proto-oncogene tyrosine-protein kinase Src, also known as c-Src, belongs to the family of
non-receptor tyrosine protein kinases (TKs) called Src kinases. It plays a crucial role in cell …

Inherent Efficacies of Pyrazole-Based Derivatives for Cancer Therapy: The Interface Between Experiment and In Silico

ZF Dube, OS Soremekun, T Ntombela… - Future Medicinal …, 2023 - Taylor & Francis
There has been an increasing trend in the design of novel pyrazole derivatives for desired
biological applications. For a cost-effective strategy, scientists have implemented various …