Browsing Cancer Therapeutics by issue date
Now showing items 1-20 of 641
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Dominant negative knockout of p53 abolishes ErbB2-dependent apoptosis and permits growth acceleration in human breast cancer cells
(Springer Science and Business Media LLC, 2002-04-01)Dominant negative knockout of p53 abolishes ErbB2-dependent apoptosis and permits growth acceleration in human breast cancer cells. We previously reported that the FrbB2 oncoprotein prolongs and amplifies growth factor ... -
(2-carboxamido)(3-amino)thiophene compounds
(2005-09-27)Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C 0-4 alkyl, are useful in the treatment of cancer. -
Synthesis of trisubstituted pyrimidines by regioselective S<sub>N</sub>Ar and Suzuki reactions of polyhalopyrimidines
(GEORG THIEME VERLAG KG, 2006-04-04)An efficient, regioselective approach to the synthesis of trisubstituted pyrimidines was developed. Sequential functionalization of com. available polyhalopyrimidines provided the target compds. in moderate to good overall ... -
A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days.
(NATURE PUBLISHING GROUP, 2007-01-15)Seliciclib (CYC202; R-roscovitine) is the first selective, orally bioavailable inhibitor of cyclin-dependent kinases 1, 2, 7 and 9 to enter clinical trial. Preclinical studies showed antitumour activity in a broad range ... -
MoKCa database--mutations of kinases in cancer.
(OXFORD UNIV PRESS, 2009-01-01)Members of the protein kinase family are amongst the most commonly mutated genes in human cancer, and both mutated and activated protein kinases have proved to be tractable targets for the development of new anticancer ... -
Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design
(2010-01-01)The production of selective protein kinase inhibitors is often frustrated by the similarity of the enzyme active sites. For this reason, it is challenging to design inhibitors that discriminate between the three Aurora ... -
The epidermal growth factor receptor/Erb-B/HER family in normal and malignant breast biology.
(UPV/EHU Press, 2011-01-01)The EGFR/Erb-B receptor tyrosine kinases each play distinct and complementary roles in normal breast development. The four receptors form both homodimers and heterodimers in response to binding by ligands which show ... -
Protein coalitions in a core mammalian biochemical network linked by rapidly evolving proteins
(Springer Science and Business Media LLC, 2011-05-25)<jats:title>Abstract</jats:title> <jats:sec> <jats:title>Background</jats:title> <jats:p>Cellular ATP levels are generated by glucose-stimulated mitochondrial metabolism and determine ... -
PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
(2011-07-28)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), ... -
canSAR: an integrated cancer public translational research and drug discovery resource.
(OXFORD UNIV PRESS, 2012-01-01)canSAR is a fully integrated cancer research and drug discovery resource developed to utilize the growing publicly available biological annotation, chemical screening, RNA interference screening, expression, amplification ... -
ChEMBL: a large-scale bioactivity database for drug discovery.
(OXFORD UNIV PRESS, 2012-01-01)ChEMBL is an Open Data database containing binding, functional and ADMET information for a large number of drug-like bioactive compounds. These data are manually abstracted from the primary published literature on a regular ... -
ALDEHYDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
(2012-01-12)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aldehyde compounds of the following formula (A) (for convenience, collectively referred to herein as "ALD ... -
PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(2012-01-26)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKe and/or TBK-1 : in which: R1 represents an aliphatic heterocyclyl ... -
miRNA Profiles as a Predictor of Chemoresponsiveness in Wilms' Tumor Blastema
(2013-01-01)The current SIOP treatment protocol for Wilms' tumor involves pre-operative chemotherapy followed by nephrectomy. Not all patients benefit equally from such chemotherapy. The aim of this study was to generate a miRNA profile ... -
COMPOUNDS AND THEIR USES
(2013-02-21)The invention provides a compound that is an inhibitor of one or both of TBK1 and IKKe, or a down-regulator of the expression of one or both of TBK1 and IKKe, for use in a method of treating a cancer that is dependent on ... -
Identification of nine new susceptibility loci for testicular cancer, including variants near DAZL and PRDM14.
(NATURE PUBLISHING GROUP, 2013-06-01)Testicular germ cell tumor (TGCT) is the most common cancer in young men and is notable for its high familial risks. So far, six loci associated with TGCT have been reported. From genome-wide association study (GWAS) ... -
GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors.
(AMER ASSOC CANCER RESEARCH, 2013-06-15)Most breast cancers at diagnosis are estrogen receptor-positive (ER(+)) and depend on estrogen for growth and survival. Blocking estrogen biosynthesis by aromatase inhibitors has therefore become a first-line endocrine ... -
Dual blockade of the PI3K/AKT/mTOR (AZD8055) and RAS/MEK/ERK (AZD6244) pathways synergistically inhibits rhabdomyosarcoma cell growth in vitro and in vivo.
(AMER ASSOC CANCER RESEARCH, 2013-08-05)PURPOSE: To provide rationale for using phosphoinositide 3-kinase (PI3K) and/or mitogen-activated protein kinase (MAPK) pathway inhibitors to treat rhabdomyosarcomas, a major cause of pediatric and adolescent cancer deaths. ... -
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.
(IMPACT JOURNALS LLC, 2013-08-25)The ribosomal P70 S6 kinases play a crucial role in PI3K/mTOR regulated signalling pathways and are therefore potential targets for the treatment of a variety of diseases including diabetes and cancer. In this study we ... -
Individualized 131I-mIBG therapy in the management of refractory and relapsed neuroblastoma.
(SPRINGER, 2013-10-01)OBJECTIVE: Iodine-131-labelled meta-iodobenzylguanidine (I-mIBG) therapy is an established treatment modality for relapsed/refractory neuroblastoma, most frequently administered according to fixed or weight-based criteria. ...