期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 3, 页码 203-206出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml2002482
关键词
LFA-1/ICAM-1 antagonist; tetrahydroisoquinoline derivative; SAR 1118; ophthalmic solution; dry eye
LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.
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