Browsing Cancer Therapeutics by issue date
Now showing items 1-20 of 263
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Molecular cytogenetic analysis consistently identifies translocations involving chromosomes 1, 2 and 15 in five embryonal rhabdomyosarcoma cell lines and a PAX-FOXO1A fusion gene negative alveolar rhabdomyosarcoma cell line.
(2001-01)Rhabdomyosarcoma in children is a "small round blue cell tumour" that displays skeletal muscle differentiation. Two main histological variants are recognised, alveolar (ARMS) and embryonal (ERMS) rhabdomyosarcoma. Whereas ... -
Dominant negative knockout of p53 abolishes ErbB2-dependent apoptosis and permits growth acceleration in human breast cancer cells
(2002)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 ... -
A rationale for the clinical development of the thymidylate synthase inhibitor ZD9331 in ovarian and other solid tumours
(2002-07-18)A rationale for the clinical development of the thymidylate synthase inhibitor ZD9331 in ovarian and other solid tumours. ZD9331 is an antifolate drug that potently and specifically inhibits thymidylate synthase (TS). In ... -
Viral delivery of P450 reductase recapitulates the ability of constitutive overexpression of reductase enzymes to potentiate the activity of mitomycin C in human breast cancer xenografts
(2003)Viral delivery of P450 reductase recapitulates the ability of constitutive overexpression of reductase enzymes to potentiate the activity of mitomycin C in human breast cancer xenografts. Indolequinones such as mitomycin ... -
Technology evaluation: EMD-273063, EMD Lexigen
(2004)Technology evaluation: EMD-273063, EMD Lexigen EMD-273063 is an antibody/cytokine fusion protein comprised of a humanized version of the murine anti-GD2 antibody 14.18 coupled to two molecules of IL-2. It is being developed ... -
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF.
(2004-03)Over 30 mutations of the B-RAF gene associated with human cancers have been identified, the majority of which are located within the kinase domain. Here we show that of 22 B-RAF mutants analyzed, 18 have elevated kinase ... -
Significant differences in biological parameters between prodrugs cleavable by carboxypeptidase G2 that generate 3,5-difluoro-phenol and -aniline nitrogen mustards in gene-directed enzyme prodrug therapy systems.
(2004-05)Nine new nitrogen mustard compounds derived from 2,6-difluoro-4-hydroxy- (3a-e) and 2,6-difluoro-4-amino- (4a-d) aniline were synthesized as potential prodrugs. They were designed to be activated to their corresponding ... -
Discovery of small molecules as anticancer agents: the role of the medicinal chemist in the discovery of new cancer therapeutics
(2005)Discovery of small molecules as anticancer agents: the role of the medicinal chemist in the discovery of new cancer therapeutics -
PLCgamma1 is essential for early events in integrin signalling required for cell motility.
(2005-06)Cell motility is a critical event in many processes and is underlined by complex signalling interactions. Although many components have been implicated in different forms of cell migration, identification of early key ... -
Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models.
(2005-10)PURPOSE: To establish the pharmacokinetic and pharmacodynamic profile of the heat shock protein 90 (HSP90) inhibitor 17-allylamino, 17-demethoxygeldanamycin (17-AAG) in ovarian cancer xenograft models. EXPERIMENTAL DESIGN: ... -
Targeting of multiple signalling pathways by heat shock protein 90 molecular chaperone inhibitors.
(2006-12)The last decade has seen the molecular chaperone heat shock protein 90 (HSP90) emerge as an exciting target for cancer therapy. This is because HSP90 is involved in maintaining the conformation, stability, activity and ... -
Calmodulin-independent, agonistic properties of a peptide containing the calmodulin binding site of estrogen receptor alpha
(2007-03-30)Calmodulin (CaM) contributes to estrogen receptor alpha (ER)-mediated transcription. In order to study the underlying mechanisms, we synthesized a peptide including the CaM binding site: ERalpha17p (P(295)-T(311)). This ... -
Multifaceted dysregulation of the epidermal growth factor receptor pathway in clear cell sarcoma of the kidney.
(2007-08)PURPOSE: Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase overexpressed in a variety of human malignancies, against which targeted therapies have shown efficacy in lung and brain tumors. Clinical ... -
Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity.
(2007-12)The Aurora family of serine/threonine kinases is important for the regulation of centrosome maturation, chromosome segregation, and cytokinesis during mitosis. Overexpression of Aurora kinases in mammalian cells leads to ... -
Mechanisms of acquired resistance to 2-(4-Amino-3-methylphenyl)benzothiazole in breast cancer cell lines
(2008)Compounds within the 2-(4-aminophenyl)benzothiazole class represent extremely potent and selective experimental antitumour agents. The lysylamide prodrug of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole is undergoing ... -
Benchmarking the reliability of QikProp. Correlation between experimental and predicted values
(2008)The theoretical prediction power of the software package QikProp was tested. This was achieved by comparing experimentally known results to predicted values. First, simple molecular descriptors for physicochemical properties: ... -
Known drug space as a metric in exploring the boundaries of drug-like chemical space
(2009)In this work, marketed drug compounds (or known drug space) were used as a metric to test the principles of eliminating parent structures of the nitrenium ion (aryl-amine/nitro compounds) as well as sulphur and halogen ... -
Trastuzumab emtansine, an antibody-drug conjugate for the treatment of HER2+metastatic breast cancer
(2010)Roche Holding AG, and its subsidiaries Genentech Inc and Chugai Pharmaceutical Co Ltd, are developing trastuzumab emtansine (trastuzumab-DM1) for the treatment of HER2+ metastatic breast cancer. Trastuzumab emtansine is a ... -
Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design
(2010)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 ...
