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2012 (v1)PublicationUploaded on: April 14, 2023
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2011 (v1)Publication
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Uploaded on: March 31, 2023 -
2009 (v1)Publication
This review will briefly outline the most interesting approaches recently reported for the synthesis of highly functionalized pyrimidine derivs. The pyrimidine scaffold represents an important pharmacophore endowed with a wide range of pharmacol. activities according to the specific decoration of the heterocycle.
Uploaded on: May 11, 2023 -
2008 (v1)Publication
A review. FLT3 is a tyrosine kinase (TK), member of the class III TK receptor family, normally expressed in hematopoietic, immune and neural systems, also playing an important role in the pathogenesis of acute leukemias, particularly acute myeloid leukemia (AML), where it is present in constitutively activated mutated forms, correlated with...
Uploaded on: April 14, 2023 -
2010 (v1)Publication
Abstract Human Pim1 (proviral integration site for Moloney murine leukemia virus) kinase is a 313-amino acid serine-threonine kinase that possesses several biological functions in cell survival, proliferation and differentiation, and its overexpression has been observed in a number of human cancers. Indeed, this kinase is a proto-oncogene that...
Uploaded on: April 14, 2023 -
2007 (v1)Publication
Chronic myelogenous leukemia (CML) is a myeloproliferative disease characterized by the presence of the Philadelphia chromosome that expresses the constitutively activated tyrosine kinase Bcr-Abl; this enzyme causes hyper-proliferation of the stem cells and the consequent pathol. of the disease. Targeted inhibitors of Bcr-Abl have...
Uploaded on: April 14, 2023 -
2010 (v1)Publication
Resistance to the Bcr-Abl inhibitors approved for the treatment of chronic myeloid leukaemia (CML) may arise from different mechanisms, including Bcr-Abl amino acid mutations, gene amplification and mechanisms independent of Bcr-Abl. The T315I mutation at the gatekeeper residue is very frequent in advanced phases of the disease and is one of...
Uploaded on: April 14, 2023 -
2007 (v1)Publication
A review. Protein tyrosine kinases catalyze the transfer of phosphoryl groups from ATP to amino acids on proteins and play a fundamental role in signal transduction pathways in mammalian cells. In particular, Src and Src-family are non-receptor tyrosine kinases that regulate cell growth, differentiation, migration, adhesion and apoptosis. ...
Uploaded on: March 25, 2023 -
2007 (v1)Publication
Angiogenesis is a tightly regulated process that leads to the formation of new blood vessels in limited physiol. conditions, and can also occur under pathol. situations as retinopathies, arthritis, endometriosis and cancer. Enhanced angiogenesis is present in tumors that need new blood capillaries to grow, remove metabolic waste and transport...
Uploaded on: March 25, 2023 -
2007 (v1)Publication
A review. Angiogenesis is a tightly regulated process that leads to the formation of new blood vessels sprouting from pre-existing microvasculature and occurs in limited physiol. conditions or under pathol. situations such as retinopathies, arthritis, endometriosis and cancer. Blockade of angiogenesis is an attractive approach for the...
Uploaded on: March 31, 2023 -
1999 (v1)Publication
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Uploaded on: April 14, 2023 -
2010 (v1)Publication
A review. C-Src and Bcr-Abl are 2 non-receptor or cytoplasmic tyrosine kinases (TKs) that play important roles in the development of solid and hematol. malignancies. Indeed, Src is overexpressed or hyperactivated in a variety of solid tumors, while Bcr-Abl is the causative agent of chronic myeloid leukemia (CML), where Src is also involved. ...
Uploaded on: April 14, 2023 -
2007 (v1)Publication
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Uploaded on: April 14, 2023 -
2009 (v1)Publication
In order to further explore the antiproliferative properties of O-phenoxyethyl and O-adamantyl acylthiocarbamates (ATCs), a series of 14 derivs. was prepd. by a parallel adaptation of a highly convergent one-pot three-step procedure. Ten acylthiocarbamates were selected by the National Cancer Institute drug evaluation program and screened...
Uploaded on: March 25, 2023 -
2009 (v1)Publication
Docking simulations and three-dimensional quant. structure-activity relationship (3D-QSAR) anal. were performed on a wide set of c-Src inhibitors. The study was conducted using a structure-based alignment and by applying the GRID/GOLPE approach. The present 3D-QSAR investigation proved to be of good statistical value, displaying r 2, q 2 and...
Uploaded on: May 11, 2023