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Chapter
Biodegradation of Luteinizing Hormone-Releasing Hormone
The concept that the proteolytic degradation of peptide hormones could be one of the key mechanisms regulating the homeostasis of the hormone, as proposed by Knights et al. (1973), is widely accepted. However, cu...
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Chapter
Tritium Labeling of Brain Peptides
During the past decade, radiolabeling of biologically active peptides has become a widely applied and essential technique for a variety of biochemical and physiological investigations.
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Article
New antitumor leads from a peptidomimetic library
A parallel combinatorial library of over 1600 compounds has been designed and synthesized for the development of new potential peptidomimetic protein tyrosine kinase (PTK) inhibitor leads. These peptidomimetic...
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Article
New antitumor leads from a peptidomimetic library
A parallel combinatorial library of over 1600 compounds has been designed and synthesized for the development of new potential peptidomimetic protein tyrosine kinase (PTK) inhibitor leads. These peptidomimetic...
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Chapter
Further Studies of the Signaling Mechanisms of the Antitumor Somatostatin Analogue TT-232
The somatostatin structural analogue TT-232 is a heptapeptide of a cyclopenta-ring structure: D-Phe-Cys-Tyr-D-Thr-Lys-Cys-Thr-NH2 that was shown to have strong antiproliferative and apoptotic effects on tumor cel...
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Chapter
New Antiproliferative Agents from a Peptidomimetic Library
It is known that chiral ATP analogue quinazolines show selective Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR TK) inhibitory activity depending on the chirality of the molecule [1]. We have developed...
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Chapter
HPLC Analysis, Modeling, and Biological Studies of Antiproliferative Heterocyclic Carboxamides
Reversed phase HPLC and MEKC [1] provide excellent possibilities to measure the hydrophobic properties of compounds, characterizing them directly from the chromatographic retention time. The aim in this respec...
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Chapter
Peptidomimetic tyrosine kinase inhibitors induce non apoptotic, Clarke-III type programmed cell death
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Article
Validation subset selections for extrapolation oriented QSPAR models
One of the most important features of QSPAR models is their predictive ability. The predictive ability of QSPAR models should be checked by external validation. In this work we examined three different types o...
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Article
Open AccessTT-232: An Anti-tumour and Anti-inflammatory Peptide Therapeutic in Clinical Development
TT-232 is a structural derivative of the peptide hormone somatostatin with selective anti-proliferative and anti-inflammatory properties. It has a strong anti-tumour activity both in vitro and in vivo on a wide r...
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Article
Binding specificity of the l-arginine transport systems in mouse macrophages and human cells overexpressing the cationic amino acid transporter hCAT-1
The uptake of l-arginine into mouse peritoneal macrophages can be inhibited by numerous amino acids and derivatives. Kinetic studies showed an almost entirely competitive inhibition for both cationic and neutral ...