Targeting integrins αvβ3 and α5β1 with new β-lactam derivatives

Galletti, Paola; Soldati, Roberto; Pori, Matteo; Durso, Margherita; Tolomelli, Alessandra; Gentilucci, Luca; Dattoli, Samantha Deianira; Baiula, Monica; Spampinato, Santi; Giacomini, Daria

doi:10.1016/j.ejmech.2014.06.041

Cited by 40 publications

(69 citation statements)

References 42 publications

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“…The solid tumors formed from epithelial cells are found to be with higher level of α 6 β 4 , α 6 β 1 , α v β 5 , α 2 β 1 and α 3 β 1 integrins and retained with different expression levels during tumor cell survival, proliferation, progression and migration. The higher expression levels of integrins α v β 3 , α5β1 and α v β 6 in some tumors acts as the marker proteins, while they are under expressed in normal epithelial cells [6]. Integrins in association with oncogenes or receptor tyrosine kinases can result in enhanced tumorigenesis.…”

Section: Introduction Integrinsmentioning

confidence: 99%

“…It adheres to the extracellular matrix proteins using an amino acid sequence of arginine-glycine-aspartic acid [6,10,11]. The α v β 3 integrin, vitronectin receptor is a member in the family of αv integrins, a group of 5 members: α v β 1 , α v β 3 , α v β 5 , α v β 6 and α v β 8 whose prime function is regulation of cell adhesion to ECM, proliferation and migration. It adheres to vitronectin, an extracellular matrix protein with the help of RGD sequence [6,10,11].…”

Section: Introduction Integrinsmentioning

confidence: 99%

“…A group of membrane proteins called Tetraspanins are responsible for regulating the integrin function in the tumor cells by recruiting integrins to the membrane microdomains. The extent of cell adhesion and migration on ECM is controlled by the recruitment specific integrins and other Focal adhesion proteins, which in turn became potential candidates for cancer therapy [3][4][5][6].…”

Section: Introduction Integrinsmentioning

confidence: 99%

“…The α v β 3 integrin, vitronectin receptor is a member in the family of αv integrins, a group of 5 members: α v β 1 , α v β 3 , α v β 5 , α v β 6 and α v β 8 whose prime function is regulation of cell adhesion to ECM, proliferation and migration. It adheres to vitronectin, an extracellular matrix protein with the help of RGD sequence [6,10,11]. These are the prime type of integrins that are present in the endothelial cells and helps in angiogenesis via the basic fibroblast growth factor (bFGF) and tumor necrosis factor-α and also contribute to the malignant spread of various tumor cells such as breast carcinoma, prostrate carcinoma and melanoma [12][13][14].…”

Section: Introduction Integrinsmentioning

confidence: 99%

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Pharmacological and Clinical Importance of Integrin Antagonists in Treatment of Cancer

Santhosh¹

2014

J Cell Sci Ther

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Integrins are heterodimeric molecules that are composed of 18 α-subunits and 8 β-subunits. They exist in 24 distinctive shapes based on combination of these sub-units and are mainly responsible for the adhesion of extracellular matrix (ECM) and immunoglobulin family molecules. Integrins mediate adhesion of epithelial cells to the basement membrane and also help in the migration, proliferation and survival of tumor cells. Studies also reveal that certain integrins act as markers for tumor cells and they also assist in both tumor progression and apoptosis. Studies reveal that unligated integrins in association with caspase 8 result in inhibition of ECM adhesion might result and integrin mediated death (IMD) on the other hand integrins in association with oncogenes or receptor tyrosine kinases can result in enhanced tumorigenesis. Among several types of integrins, αvβ3 and α 5 β 1 have gained importance in anti-angiogenesis studies.Hence the role of antiangiogenesis antagonists has come into light. These include a variety of monoclonal antibodies and peptides. Each one of them has their own mechanism of action and antiangiogenesis activity. Current review aims at studying the phase 1 and 2 trails of these antagonists for anti-angiogenic function.

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Section: Introduction Integrinsmentioning

confidence: 99%

Section: Introduction Integrinsmentioning

confidence: 99%

Section: Introduction Integrinsmentioning

confidence: 99%

Section: Introduction Integrinsmentioning

confidence: 99%

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Pharmacological and Clinical Importance of Integrin Antagonists in Treatment of Cancer

Santhosh¹

2014

J Cell Sci Ther

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“…Furthermore, the β-lactam ring also serves as a synthon or versatile intermediates for the synthesis of aromatic amino acid derivatives, peptides, polyamines, polyamino alcohols, amino sugars and polyamino ethers, as well as, for many biologically important classes of organic compounds [6][7][8][9][10][11][12][13][14][15][16][17] . Due to this, the investigation into the chemistry of these compounds continues to appeal the synthetic and medicinal organic chemists world over.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2015

IJPSR

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Synthesis of heterocylic compound has always drawn the attention of chemist over the years mainly because of their important biological properties. Particularly, the role of β-lactam which are endowed with unique structure and potent biological activity. The β-lactam heterocycles are considered as an important contribution of science to humanity since they have been constituents of living organisms, natural products, drugs and many more substances useful to mankind and society in all walks of life. Their synthesis and evaluation has always drawn the attention of biologists over the years. β-lactam, a four member heterocyclic compound involved in research aimed to evaluate new products that possess interesting biological activities. Natural and synthetic β-lactam derivatives occupy a central place among medicinally important compounds due to their diverse and interesting antibiotic activities and are still the most prescribed antibiotics used in medicine. The present review article focuses on the pharmacological profile of β-lactam with their potential activities. The ring system exhibits a wide range of activities like antimicrobial, antitubercular, anticancer, antidiabetic, tryptase and chymase inhibitory activity etc. attracting the attention of researchers. The biological profile of β-lactam reported by organic chemist is reviewed here comprehensively with examples under eleven different activities.

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αvβ3‐ oder α5β1‐Integrin‐selektive Peptidmimetika für die Oberflächenbeschichtung

et al. 2016

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Die Entwicklung von Biomaterialien mit Bindungsaffinität für Integrine ist eine ausgezeichnete Methode, die Zelladhäsion zu fördern, zelluläres Verhalten zu regulieren und spezifische biologische Antworten auf der Zelloberfläche zu induzieren. Das Ziel dieses Aufsatzes ist es, die Evolution von Verbindungen für die Beschichtung darzustellen: angefangen von Peptiden und Proteinen mit relativ niedriger Integrinbindungsaffinität und ‐selektivität bis hin zu hochaffinen und subtypselektiven Peptidmimetika. Insbesondere werden wir auf die Herausforderungen eingehen, die auf dem Weg zu einer Selektivität zwischen den strukturell eng verwandten Subtypen αvβ3 und α5β1 zu meistern waren. Die Oberflächenfunktionalisierung mit diesen Peptidmimetika öffnet den Weg für eine neue Generation von spezifisch modifizierten Oberflächen, die das Verhalten von Zellen gezielt beeinflussen können. Diese dienen sowohl zur Aufklärung der biologischen Rolle des jeweiligen Integrins als auch für eine Anwendung im “Tissue‐Engineering” und in der regenerativen Medizin.

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Targeting integrins αvβ3 and α5β1 with new β-lactam derivatives

Cited by 40 publications

References 42 publications

Pharmacological and Clinical Importance of Integrin Antagonists in Treatment of Cancer

Pharmacological and Clinical Importance of Integrin Antagonists in Treatment of Cancer

Untitled

αvβ3‐ oder α5β1‐Integrin‐selektive Peptidmimetika für die Oberflächenbeschichtung

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