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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-436 |
| Subject |
Novel urotensin-II antagonist |
| Authors |
임채조*, 김대근1, 이규양2
한국화학연구원 의약화학연구센터, Korea
1과학기술연합대학원대학교(UST) 한국화학연구원, Korea
2한국화학연구원 대사증후군치료제연구센터, Korea
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| Abstract |
Among many targets, urotensin-II receptor (UT) has attracted considerable recent attention as a therapeutic target for treatment of heart failure. Urotensin-II (U-II), a cysteine-linked cyclic peptide, is mainly expressed in a variety of tissues, including blood vessels, heart, liver, kidney, skeletal muscle and lung. It is known to be the most potent vasoconstrictor, displaying a 10 times greater potency than that of endothelin. The effects of this peptide are mediated through its interaction with a G protein-coupled receptor known as a GPR14 or the urotensin-II receptor. Activation of UT by binding with U-II results in several cardiovascular responses including vasoconstriction, vasodilation, cell proliferation and hypertrophy. These findings suggest that U-II and its receptor system are involved in the pathogenesis of cardiovascular disease. Furthermore, the results of previous studies demonstrate that the expression of UT is low or undetectable in normal myocardium, whereas elevated U-II plasma levels and increased levels of UT expression are associated with numerous cardiorenal and metabolic diseases, including hypertension, heart failure, atherosclerosis, diabetes and renal failure. Therefore, UT has emerged as one of the most promising therapeutic target for treatment of heart failure as well as a broad range of other cardiovascular maladies. As part of a continuing program aimed at the development of novel and potent UT antagonists, we recently identified and optimized a series of aminopiperidine derivatives. The details of synthesis, biological evaluation and structure-activity relationships(SAR) results will be discussed. |
| E-mail |
giant387@krict.re.kr |
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119th General Meeting of the KCS