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SUMMARY:Selective integrin inhibitors for application as drugs\, for coati
 ng biomaterials and for molecular imaging
DTSTART:20131106T171500
DTEND:20131106T183000
DTSTAMP:20260407T011313Z
UID:c89c954ee0e03cc94f81b27e5a9813690e52a321f5a48947501155e7
CATEGORIES:Conferences - Seminars
DESCRIPTION:Prof. Dr. Horst Kessler\, Institute for Advanced Study\, Techn
 ische Universität München\, Garching Technische Universität München (T
 UM)\, Department Chemistry\, Garching/Munich\, Germany\nCell adhesion is m
 ediated via cellular bidirectional receptors\, so-called integrins. The tr
 ipeptidic sequence RGD is recognized by several integrin subtypes (v
 3\, v5\, v6\, v8\, 51\, IIb3). The different
  integrins recognize different extracellular matrix proteins and the integ
 rin pattern on cells strongly depend on many factors. Superactivity and re
 ceptor subtype selectivity has been achieved by the “spatial screening
 ” procedure which yielded the cyclic peptides c(RGDfX)  as the first se
 lective and superactive ligand for αvβ3. This lead structure was optimiz
 ed by development of peptidomimetics to achieve subtype selectivity\, espe
 cially between the integrins αvβ3 and α5β1. Different functionalizatio
 n under retention of their activity and selectivity profiles allow biophys
 ical studies regarding the function of different integrin subtypes and coa
 ting of implant materials to stimulate osteoblast adhesion in bone implant
 s or to prevent restenosis in artery stents. Labelling with 18F or 68Ga al
 lows molecular imaging using positron emission tomography (PET) in animals
  and man. Thus\, the varying integrin patterns of different cancers can be
  elucidated\, a prerequisite for personalized medicine. \nA similar proce
 dure as described for the RGD peptides was applied to the chemokine recept
 or CXCR4 leading to a superpotent ligand for anti-HIV therapy and to the f
 irst imaging of cancer by targeting this receptor.\nRecent publications:\n
 S. Neubauer\, F. Rechenmacher\, A. J. Beer\, F. Curnis\, K. Pohle\, C. D´
 Alessandria\, H.-J. Wester\, U. Reuning\, A. Corti\, M. Schwaiger\, H. Kes
 sler\, Selective imaging of the angiogenic relevant integrins α5β1 and 
 αvβ3\, Angew Chem.Int. Ed. 2013\, in press.\nF. Rechenmacher\, S. Neubau
 er\, J. Polleux\, C. Mas-Moruno\, M. De Simone\, E. A. Cavalcanti-Adam\, J
 . P. Spatz\, R. Fässler\, H. Kessler\, Functionalizing αvβ3- or α5β1-
 Selective Integrin Antagonists for Surface Coating: A Method to Discrimina
 te Integrin Subtypes In Vitro\, Angew. Chem. Int. Ed. 2013\, 52\, 1572-157
 5.\nO. Demmer\, A.O. Frank\, F. Hagn\, M. Schottelius\, L. Marinelli\, S. 
 Cosconati\, R. Brack-Werner\, S. Kremb\, H.-J. Wester\, H. Kessler\; A Con
 formationally Frozen Peptoid Boosts CXCR4 Affinity and Anti-HIV Activity\,
  Angew Chem. Int. Ed. 2012\, 51\, 8114-8117.
LOCATION:BCH 2218 https://plan.epfl.ch/?room==BCH%202218
STATUS:CONFIRMED
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