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Specific Inhibition of Mammalian Oocyte Meiosis by Small Molecule Inhibitors targeting Polo-like Kinase 1

첫 페이지 보기
  • 발행기관
    한국동물생명공학회(구 한국동물번식학회) 바로가기
  • 간행물
    Reproductive & Developmental Biology(Supplement) 바로가기
  • 통권
    Volume 41 No 2 Supplement (2017.06)바로가기
  • 페이지
    pp.19-19
  • 저자
    Sung-Min Jeong, In-Won Lee, Yu-Jin Jo, Jeong-Kyu Bang, Suk Namgoong, Nam-Hyung Kim
  • 언어
    영어(ENG)
  • URL
    https://www.earticle.net/Article/A347527

원문정보

초록

영어
Polo-like kinase 1 (Plk1) plays crucial roles in various stages of oocyte maturation. Recently, we demonstrated that synthesized peptidomimetics AB103-8, targeting the polo- box domain (PBD) of Plk1 disrupted oocyte meiotic maturation and meiosis resumption. However, as a peptidic character of AB103-8 appeared to be defective due to poor membrane permeability and protease stability. To overcome the drawbacks, we designed and synthesized a series of pyrrole-based small-molecule inhibitors and screened against porcine oocyte maturation rates. Among the synthesized compounds, the macrocyclic inhibitor compound 4 displayed the highest inhibition potential against the oocyte meiotic maturation and embryos blastocyst formation. Furthermore, the addition of this compound to culture medium efficiently blocked the maturation of porcine and mouse oocytes, indicating that the lead compound could penetrate zona pellucida and cell membrane. We also investigated the Plk1 inhibiting ability of this compound. Treated mouse oocytes confirmed the Plk1 inhibition by showing abnormal spindle formation. Collectively, these results suggest that the novel Pyrrole-based compounds could be used for the basis of developing contraceptive agents.

키워드

Oocyte maturation Plk1 Inhibitor Contraceptive agents

저자

  • Sung-Min Jeong [ Molecular Embryology Laboratory, Department of Animal Sciences, Chungbuk National University, Chung-Buk 361-763, Republic of Korea ]
  • In-Won Lee [ Molecular Embryology Laboratory, Department of Animal Sciences, Chungbuk National University, Chung-Buk 361-763, Republic of Korea ]
  • Yu-Jin Jo [ Molecular Embryology Laboratory, Department of Animal Sciences, Chungbuk National University, Chung-Buk 361-763, Republic of Korea ]
  • Jeong-Kyu Bang [ Division of Magnetic Resonance, Korea Basic Science Institute, Ochang, 363-883, Republic of Korea ]
  • Suk Namgoong [ Molecular Embryology Laboratory, Department of Animal Sciences, Chungbuk National University, Chung-Buk 361-763, Republic of Korea ]
  • Nam-Hyung Kim [ Molecular Embryology Laboratory, Department of Animal Sciences, Chungbuk National University, Chung-Buk 361-763, Republic of Korea ]

참고문헌

자료제공 : 네이버학술정보

간행물 정보

발행기관

  • 발행기관명
    한국동물생명공학회(구 한국동물번식학회) [The Korean Society of Animal Reproduction and Biotechnology]
  • 설립연도
    1976
  • 분야
    농수해양>축산학
  • 소개
    동물번식생리학, 동물생명공학, 수의학, 인공수정 및 수정란이식을 이용한 동물개량에 관한 이론과 기술의 발전을 통해 학계, 연구계, 산업계 및 양축가 상호간의 협력을 도모함으로써 동물과학발전 및 사회일반의 이익에 기여 한다는 목적을 위해 노력해 나가겠습니다.

간행물

  • 간행물명
    Reproductive & Developmental Biology(Supplement)
  • 간기
    연간
  • 수록기간
    2001~2017
  • 십진분류
    KDC 527 DDC 636

이 권호 내 다른 논문 / Reproductive & Developmental Biology(Supplement) Volume 41 No 2 Supplement

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