Current Medicinal Chemistry

ISSN: 0929-8673

Current Medicinal Chemistry
Volume 12 , Number 1 , 2005

Contents


Protein Tyrosine Phosphatases and their Inhibitors Pp. 1-22
Purushottam M. Dewang, Nai-Mu Hsu, Shao-Zheng Peng and Wen-Ren Li
[Abstract] [Full text article]


Bioisosterism: A Useful Strategy for Molecular Modification and Drug Design Pp. 23-49
Lidia Moreira Lima and Eliezer J. Barreiro
[Abstract] [Full text article]


Non Peptidic α_vβ₃ Antagonists: Recent Developments Pp. 51-70
Barbara Cacciari and Giampiero Spalluto
[Abstract] [Full text article]


Oligonucleotides and Oligonucleotide Conjugates: A New Approach for Cancer Treatment Pp. 71-88

Tatiana Da Ros, Giampiero Spalluto, Maurizio Prato, Tula Saison-Behmoaras, Alexandre Boutorine and Barbara Cacciari
[Abstract] [Full text article]




Abstracts

[Back to top]
Protein Tyrosine Phosphatases and their Inhibitors
Purushottam M. Dewang, Nai-Mu Hsu, Shao-Zheng Peng and Wen-Ren Li
[Full text article]

Protein tyrosine phosphatase (PTP) is the family of enzymes that are key players in cellular signal transduction system and perturbation in their functioning is implicated in many disease-states. Diverse chemical compounds are being synthesized and evaluated as PTP inhibitors. This review presents a brief account of various enzymes of the PTP family and their inhibitors. Peculiar features of these enzymes and their roles in various diseases are summarized along with important inhibitors developed in recent years.


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Bioisosterism: A Useful Strategy for Molecular Modification and Drug Design
Lidia Moreira Lima and Eliezer J. Barreiro
[Full text article]

This review aim to demonstrate the role of bioisosterism in rational drug design as well as in the molecular modification and optimization process aiming to improve pharmacodynamic and pharmacokinetic properties of lead compounds.


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Non Peptidic α_vβ₃ Antagonists: Recent Developments
Barbara Cacciari and Giampiero Spalluto
[Full text article]

The α_vβ₃ receptor, which are members of the group of the cellular adhesion molecules (CAM), are heterodimeric transmembrane glycoprotein receptors involved in processes such as cell-cell and cell-matrix adhesion, cell migration and signaling. Integrin α_vβ₃ receptor is expressed on almost all cells originating from the mesenchyme and seem to mediate several biological processes, including adhesion of osteoblasts to the bone matrix, migration of vascular smooth muscle cells, and angiogenesis.

Many efforts were done in the last 10 years to individuate inhibitors for α_vβ₃ receptors, due to their involvement in important pathophysiological functions. In fact, selective α_vβ₃ antagonists offer new therapeutic opportunities for the treatment of several human pathologies like osteoporosis, restenosis and diseases involving neovascularization such as rheumatoid arthritis, tumor induced angiogenesis and metastasis. Purpose of this account is to summarize the recent developments in the field of non-peptidic α_vβ₃ antagonists.


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Oligonucleotides and Oligonucleotide Conjugates: A New Approach for Cancer Treatment
Tatiana Da Ros, Giampiero Spalluto, Maurizio Prato, Tula Saison-Behmoaras, Alexandre Boutorine and Barbara Cacciari
[Full text article]

In this account we summarise recent studies on oligonucleotides and oligonucleotide derivatives and their utilisation in antigene, antisense and decoy approaches, with particular attention to peptide nucleic acids, locked nucleic acids and oligonucleotide conjugates, the most promising compounds in this field.