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Discoidin Domain Receptors: A Promising Target in Melanoma

Coralie Reger de Moura, Maxime Battistella, Anjum Sohail, Anne Caudron, Jean Paul Feugeas, Marie-Pierre Podgorniak, Cecile Pages, Sarra Mazouz Dorval, Oren Marco, Suzanne Menashi, Rafael Fridman, Celeste Lebbé, etc.

Pigment Cell Melanoma Res. 2019 Sep;32(5):697-707.

PMID: 31271515

Abstract:

The discoidin domain receptor 1 (DDR1) is a member of the receptor tyrosine kinase family that signals in response to collagen and that has been implicated in cancer progression. In the present study, we investigated the expression and role of DDR1 in human melanoma progression. Immunohistochemical staining of human melanoma specimens (n = 52) shows high DDR1 expression in melanoma lesions that correlates with poor prognosis. DDR1 expression was associated with the clinical characteristics of Clark level and ulceration and with BRAF mutations. Downregulation of DDR1 by small interfering RNA (siRNA) in vitro inhibited melanoma cells malignant properties, migration, invasion, and survival in several human melanoma cell lines. A DDR tyrosine kinase inhibitor (DDR1-IN-1) significantly inhibited melanoma cell proliferation in vitro, and ex vivo and in tumor xenografts, underlining the promising potential of DDR1 inhibition in melanoma.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1449685964 DDR1-IN-1 DDR1-IN-1 1449685-96-4 Price
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