Abstract:
:It is well established that the Eph/ephrin system plays a central role in the embryonic development, with minor implications in the physiology of the adult. However, it is overexpressed and deregulated in a variety of tumors, with a primary involvement in tumorigenesis, tumor angiogenesis, metastasis development, and cancer stem cell regeneration. Targeting the Eph/ephrin system with biologicals, including antibodies and recombinant proteins, reduces tumor growth in animal models of hematological malignancies, breast, prostate, colon, head and neck cancers and glioblastoma. Currently, some of these biopharmaceutical agents are under investigations in phase I or phase II clinical trials. Peptides and small molecules targeting protein-protein-interaction (PPI) are in the late preclinical phase where they are showing promising activity in models of glioblastoma, ovarian and lung cancer. The present review summarizes the most critical findings proposing the Eph/ephrin signaling system as a new target in molecularly targeted oncology.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Lodola A,Giorgio C,Incerti M,Zanotti I,Tognolini Mdoi
10.1016/j.ejmech.2017.07.029subject
Has Abstractpub_date
2017-12-15 00:00:00pages
152-162eissn
0223-5234issn
1768-3254pii
S0223-5234(17)30551-2journal_volume
142pub_type
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