National Taiwan University

National Cheng-kung University

Temple University

National Science Council of Republic of China

Dcb-usa LLC

Tur-Fu Huang

Woei-Jer Chuang

Chien-Hsin Chang

Ching-Hu Chung

Shwu-Jen Wu

Che-Ming Teng

Feng-Nien Ko

Wen-Mei Fu

Wenya Huang

Chih-Hsin Tang

Stefan Niewiarowski

Yu-Ju Kuo

Chiu-Yueh Chen

John C Holt

Hanna Lukasiewicz

Ih-Sheng Chen

Disclosed herein are disintegrin variants, and methods for suppressing or inhibiting platelet aggregation in a subject in need thereof. The method includes administering to the subject in need thereof an effective amount of the present disintegrin variant to alleviate or ameliorate symptoms associated with diseases, disorders, and/or conditions resulted from platelet aggregation. According to preferred embodiments, the present disintegrin variant is applied as a coating on an implantable device, such as a stent or a catheter.

Disintegrin variants and uses thereof

The invention relates to a peptide compound and its pharmaceutical composition for inhibiting platelet aggregation and preventing/treating thrombogenic diseases. The invention develops pentapeptides and hexapeptides derived from snake venom C-type lectin-like proteins (CLPs) fragments, which can inhibit platelet aggregation and have antithrombotic activity without hemorrhagic tendency. Accordingly, they can be used as potential agents for the prevention and therapy of thrombogenic diseases.

Peptide compounds for inhibitions of platelet aggregation

Peptide compounds for inhibition of platelet aggregation

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

This invention refer to chelerythrine, a considerably effective drug in the prevention and therapy of the thrombosis, which is a quaternary amine derivative and a major component of the organic solvent soluble extract of Zanthoxylum simulans. The effects of chelerythrine on the thromboembolism and the constriction of the blood vessel are also examined.

Chelerythrine inhibits platelet aggregation--a potential

Trigramin, a 72-amino acid polypeptide, has the following amino acid sequence: EAGEDCDCGSPANPCCDAATCKLIPGAQCGEGLCCDQCSFIEEGTVCRIARGDDLDDYCNGRSAGCPRNPFH. The molecule is a potent inhibitor of fibrinogen binding to receptors expressed on the glycoprotein IIb/IIIa complex in the membrane of platelets. Trigramin is thus a potent inhibitor of fibrinogen-induced human platelet aggregation. It is useful in inhibiting the formation of hemostatic platelet plugs.

Trigramin - a platelet aggregation inhibiting polypeptide

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Taipei, Taiwan

Tur-Fu Huang