The development of imatinib as a therapeutic agent for chronic myeloid leukemia

M Deininger, E Buchdunger, BJ Druker - Blood, 2005 - ashpublications.org
Imatinib has revolutionized drug therapy of chronic myeloid leukemia (CML). Preclinical
studies were promising but the results of clinical trials by far exceeded expectations …

The pharmacology and clinical pharmacology of 3, 4-methylenedioxymethamphetamine (MDMA,“ecstasy”)

AR Green, AO Mechan, JM Elliott, E O'Shea… - Pharmacological …, 2003 - Elsevier
Abstract The amphetamine derivative (±)-3, 4-methylenedioxymethamphetamine (MDMA,
ecstasy) is a popular recreational drug among young people, particularly those involved in …

A small molecule–kinase interaction map for clinical kinase inhibitors

MA Fabian, WH Biggs III, DK Treiber, CE Atteridge… - Nature …, 2005 - nature.com
Kinase inhibitors show great promise as a new class of therapeutics. Here we describe an
efficient way to determine kinase inhibitor specificity by measuring binding of small …

Overriding imatinib resistance with a novel ABL kinase inhibitor

NP Shah, C Tran, FY Lee, P Chen, D Norris… - Science, 2004 - science.org
Resistance to the ABL kinase inhibitor imatinib (STI571 or Gleevec) in chronic myeloid
leukemia (CML) occurs through selection for tumor cells harboring BCR-ABL kinase domain …

In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

T O'Hare, DK Walters, EP Stoffregen, T Jia, PW Manley… - Cancer research, 2005 - AACR
Abstract Imatinib, a Bcr-Abl tyrosine kinase inhibitor, is a highly effective therapy for patients
with chronic myelogenous leukemia (CML). Despite durable responses in most chronic …

Mechanisms of disease: oncogene addiction—a rationale for molecular targeting in cancer therapy

IB Weinstein, AK Joe - Nature clinical practice Oncology, 2006 - nature.com
There has been considerable progress in the systemic treatment of cancer because of the
rapid development and clinical application of molecular targeted agents. Although patients …

Translation of the Philadelphia chromosome into therapy for CML

BJ Druker - Blood, The Journal of the American Society of …, 2008 - ashpublications.org
Throughout its history, chronic myeloid leukemia (CML) has set precedents for cancer
research and therapy. These range from the identification of the first specific chromosomal …

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

TA Carter, LM Wodicka, NP Shah… - Proceedings of the …, 2005 - National Acad Sciences
To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it
is important to address the emergence of drug resistance in treated patients. Mutant forms of …

The BCR-ABL story: bench to bedside and back

S Wong, ON Witte - Annu. Rev. Immunol., 2004 - annualreviews.org
The twenty-first century is beginning with a sharp turn in the field of cancer therapy.
Molecular targeted therapies against specific oncogenic events are now possible. The BCR …

N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a Novel, Highly Selective, Orally …

LF Hennequin, J Allen, J Breed, J Curwen… - Journal of medicinal …, 2006 - ACS Publications
Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for
cancer progression. We report here a novel subseries of C-5-substituted anilinoquinazolines …