Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy

R Du, C Huang, K Liu, X Li, Z Dong - Molecular cancer, 2021 - Springer
Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose
activation is necessary for cell division processes via regulation of mitosis. AURKA shows …

Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

F Rossari, F Minutolo, E Orciuolo - Journal of hematology & oncology, 2018 - Springer
Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine
kinase inhibitor to be discovered with high specificity for Bcr-Abl protein resulting from t (9 …

Tau phosphorylation: the therapeutic challenge for neurodegenerative disease

DP Hanger, BH Anderton, W Noble - Trends in molecular medicine, 2009 - cell.com
The microtubule-associated protein tau is integral to the pathogenesis of Alzheimer's
disease (AD), as well as several related disorders, termed tauopathies, in which tau is …

Aurora‐A kinase: a potent oncogene and target for cancer therapy

M Yan, C Wang, B He, M Yang, M Tong… - Medicinal research …, 2016 - Wiley Online Library
The Aurora kinase family is comprised of three serine/threonine kinases, Aurora‐A, Aurora‐
B, and Aurora‐C. Among these, Aurora‐A and Aurora‐B play central roles in mitosis …

Targeting the cancer kinome through polypharmacology

ZA Knight, H Lin, KM Shokat - Nature Reviews Cancer, 2010 - nature.com
Kinase inhibitors are the largest class of new cancer drugs. However, it is already apparent
that most tumours can escape from the inhibition of any single kinase. If it is necessary to …

Axitinib effectively inhibits BCR-ABL1 (T315I) with a distinct binding conformation

T Pemovska, E Johnson, M Kontro, GA Repasky… - Nature, 2015 - nature.com
The BCR-ABL1 fusion gene is a driver oncogene in chronic myeloid leukaemia and 30–50%
of cases of adult acute lymphoblastic leukaemia. Introduction of ABL1 kinase inhibitors (for …

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent …

WS Huang, CA Metcalf, R Sundaramoorthi… - Journal of medicinal …, 2010 - ACS Publications
In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the
T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This …

A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies

AC Borisa, HG Bhatt - European journal of medicinal chemistry, 2017 - Elsevier
Aurora kinase belongs to serine/threonine kinase family which controls cell division.
Therapeutic inhibition of Aurora kinase showed great promise as probable anticancer …

Inhibition of NEDD8-activating enzyme: a novel approach for the treatment of acute myeloid leukemia

RT Swords, KR Kelly, PG Smith… - Blood, The Journal …, 2010 - ashpublications.org
NEDD8 activating enzyme (NAE) has been identified as an essential regulator of the
NEDD8 conjugation pathway, which controls the degradation of many proteins with …

Aurora kinase inhibitors-rising stars in cancer therapeutics?

AA Dar, LW Goff, S Majid, J Berlin, W El-Rifai - Molecular cancer therapeutics, 2010 - AACR
Standard therapeutic approaches of cytotoxics and radiation in cancer are not only highly
toxic, but also of limited efficacy in treatment of a significant number of cancer patients. The …