Drug repurposing: progress, challenges and recommendations
Given the high attrition rates, substantial costs and slow pace of new drug discovery and
development, repurposing of'old'drugs to treat both common and rare diseases is …
development, repurposing of'old'drugs to treat both common and rare diseases is …
The resurgence of covalent drugs
J Singh, RC Petter, TA Baillie, A Whitty - Nature reviews Drug discovery, 2011 - nature.com
Covalent drugs haveproved to be successful therapies for various indications, but largely
owing to safety concerns, they are rarely considered when initiating a target-directed drug …
owing to safety concerns, they are rarely considered when initiating a target-directed drug …
Asciminib in chronic myeloid leukemia after ABL kinase inhibitor failure
TP Hughes, MJ Mauro, JE Cortes… - … England Journal of …, 2019 - Mass Medical Soc
Background Asciminib is an allosteric inhibitor that binds a myristoyl site of the BCR-ABL1
protein, locking BCR-ABL1 into an inactive conformation through a mechanism distinct from …
protein, locking BCR-ABL1 into an inactive conformation through a mechanism distinct from …
[HTML][HTML] Dasatinib plus intensive chemotherapy in children, adolescents, and young adults with philadelphia chromosome–positive acute lymphoblastic leukemia …
WB Slayton, KR Schultz, JA Kairalla… - Journal of Clinical …, 2018 - ncbi.nlm.nih.gov
Purpose Addition of imatinib to intensive chemotherapy improved survival for children and
young adults with Philadelphia chromosome–positive acute lymphoblastic leukemia …
young adults with Philadelphia chromosome–positive acute lymphoblastic leukemia …
[HTML][HTML] Ponatinib in refractory Philadelphia chromosome–positive leukemias
JE Cortes, H Kantarjian, NP Shah… - … England Journal of …, 2012 - Mass Medical Soc
Background Resistance to tyrosine kinase inhibitors in patients with chronic myeloid
leukemia (CML) and Philadelphia chromosome–positive acute lymphoblastic leukemia (Ph …
leukemia (CML) and Philadelphia chromosome–positive acute lymphoblastic leukemia (Ph …
Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer
W Pao, J Chmielecki - Nature Reviews Cancer, 2010 - nature.com
Epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC) was
first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The …
first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The …
Targeting cancer with small molecule kinase inhibitors
Deregulation of kinase activity has emerged as a major mechanism by which cancer cells
evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors …
evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors …
[HTML][HTML] EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors
YL Choi, M Soda, Y Yamashita, T Ueno… - … England Journal of …, 2010 - Mass Medical Soc
The EML4 (echinoderm microtubule-associated protein-like 4)–ALK (anaplastic lymphoma
kinase) fusion-type tyrosine kinase is an oncoprotein found in 4 to 5% of non–small-cell lung …
kinase) fusion-type tyrosine kinase is an oncoprotein found in 4 to 5% of non–small-cell lung …
Epidermal growth factor receptor mutations in lung cancer
SV Sharma, DW Bell, J Settleman, DA Haber - Nature Reviews Cancer, 2007 - nature.com
The development and clinical application of inhibitors that target the epidermal growth factor
receptor (EGFR) provide important insights for new lung cancer therapies, as well as for the …
receptor (EGFR) provide important insights for new lung cancer therapies, as well as for the …
[PDF][PDF] A collection of breast cancer cell lines for the study of functionally distinct cancer subtypes
RM Neve, K Chin, J Fridlyand, J Yeh, FL Baehner… - Cancer cell, 2006 - cell.com
Recent studies suggest that thousands of genes may contribute to breast cancer
pathophysiologies when deregulated by genomic or epigenomic events. Here, we describe …
pathophysiologies when deregulated by genomic or epigenomic events. Here, we describe …