National Taiwan University

National Cheng-Kung University

Dcb-usa LLC

Chiu-Yueh Chen

Woei-Jer Chuang

Tur-Fu Huang

Wen-Mei Fu

Wenya Huang

Chih-Hsin Tang

Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin &#x3b1;v&#x3b2;3 receptor-antagonist activity and substantially reduced integrin &#x3b1;llb&#x3b2;3 and/or &#x3b1;5&#x3b2;1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin &#x3b1;llb&#x3b2;3 and/or &#x3b1;5&#x3b2;1 as compared to a wild-type disintegrin. The variant is useful for treatment and/or prevention of &#x3b1;v&#x3b2;3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.

Disintegrin variants and their use in treating osteoporosis-induced bone loss and angiogenesis-related diseases

Growing community of inventors

Tainan, Taiwan

Chiu-Yueh Chen