Results 161 to 170 of about 2,846 (197)

A phase I study of continuous infusion cilengitide in patients with solid tumors [PDF]

Investigational New Drugs, 2010
Cilengitide (EMD121974) is a cyclized pentapeptide that is a potent and selective integrin antagonist which has shown activity in malignant gliomas. In all previous studies, cilengitide has been administered in an intermittent fashion. However, cilengitide has a short half-life of 3-5 h with no evidence of drug accumulation.
Mark J Ratain, Peter H O'Donnell
exaly   +3 more sources

Receptor-Bound Conformation of Cilengitide Better Represented by Its Solution-State Structure than the Solid-State Structure

Chemistry - A European Journal, 2014
The X-ray crystal and NMR spectroscopic structures of the peptide drug candidate Cilengitide (cyclo(RGDf(NMe)Val)) in various solvents are obtained and compared in addition to the integrin receptor bound conformation.
Valeria la Pietra, Michael Groll, Ettore Novellino   +2 more
exaly   +2 more sources

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Iceni to repurpose Merck’s cilengitide

C&EN Global Enterprise, 2016
Scottish DNA vaccines developer BigDNA has renamed itself Iceni Pharmaceuticals and relaunched to focus on repurposed cancer therapies. The firm’s lead candidate is cilengitide, a cyclic peptide. Cilengitide was initially developed by the Technical University of Munich and Merck KGaA, but it failed late-stage clinical trials for treating glioblastoma ...
openaire   +1 more source

Protective effects of cilengitide on inflammation in chondrocytes under excessive mechanical stress

Cell Biology International, 2020
AbstractChondrocytes constantly receive external stimuli, which regulates remodeling. An optimal level of mechanical stress is essential for maintaining chondrocyte homeostasis, however, excessive mechanical stress induces inflammatory cytokines and protease, such as matrix metalloproteinases (MMPs). Therefore, excessive mechanical stress is considered
Naoto Hirose, Yuki Okamoto, Makoto Yanoshita, Yuki Asakawa, Chikako Sumi, Mami Takano, Sayuri Nishiyama, Shao‐Ching Su, Tomomi Mitsuyoshi, Ryo Kunimatsu, Kazuo Tanne, Kotaro Tanimoto   +11 more
openaire   +2 more sources

Inhibition of cytochrome P450 3A4 by cilengitide

2014
Questions Cilengitide is a stable cyclic pentapeptide containing the Arg- Gly-Asp (RGD) motif that selectively binds to αvβ3 and αvβ5 integrins, but did not meet its primary endpoint of significantly increasing overall survival when added to the current standard chemoradiotherapy regimen for brain tumors, i.e temozolomide and radiotherapy.
Bojic, Mirza, Barbero, Luca M., Riva, Simona, Dolgos, Hugues, Fluck, Marcus, Freisleben, Achim, Gallemann, Dieter, Guengerich, F. Peter   +7 more
openaire   +2 more sources

Increasing αvβ3 Selectivity of the Anti‐Angiogenic Drug Cilengitide by N‐Methylation

Angewandte Chemie International Edition, 2011
Thumbnail image of graphical abstract A subtle change: Structural changes upon amide bond methylation improve the selectivity of the anti-angiogenic drug Cilengitide, which after N-methylation at distinct positions discriminates between the closely related pro-angiogenic integrins avß3 and avß5 (see scheme).
Mas Moruno C, Beck JG, Doedens L, Frank AO, Marinelli L, COSCONATI, Sandro, Novellino E, Kessler H.   +7 more
openaire   +6 more sources

Cilengitide Merck.

Current opinion in investigational drugs (London, England : 2000), 2003
Merck KGaA is developing cilengitide, the lead in a series of integrin antagonists with anti-angiogenic activities, for the potential treatment of a variety of cancer types. The National Cancer Institute is conducting clinical trials of cilengitide. In October 1999, phase II trials in non-small-cell lung cancer (as a monotherapy) and pancreatic cancer (
openaire   +1 more source

Cilengitide inhibits proliferation and differentiation of human endothelial progenitor cells in vitro

Biochemical and Biophysical Research Communications, 2007
Bone marrow derived hematopoietic stem cells can function as endothelial progenitor cells. They are recruited to malignant tumors and differentiate into endothelial cells. This mechanism of neovascularization termed vasculogenesis is distinct from proliferation of pre-existing vessels.
Sonja, Loges, Martin, Butzal, Jasmin, Otten, Michaela, Schweizer, Uta, Fischer, Carsten, Bokemeyer, Dieter K, Hossfeld, Gunter, Schuch, Walter, Fiedler   +8 more
openaire   +2 more sources

Cilengitide

Drugs of the Future, 2000
null Sorbera, L.A., null Graul, A., null Castaner, J.   +2 more
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Does cilengitide deserve another chance?

The Lancet Oncology, 2014
TUCCI, MARCO GAETANO, Stucci S, SILVESTRIS, Francesco   +2 more
openaire   +2 more sources