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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Structural Insight into Anaphase Promoting Complex 3 Structure and Docking with a Natural Inhibitory Compound

Hamzeh Rahimi1, Mohammad Ali Shokrgozar2, Armin Madadkar-Sobhani3

  • 1Department of Molecular Medicine, Biotechnology Research Center, Pasteur Institute of Iran, Tehran, Iran.

Advanced Biomedical Research
|April 13, 2017
PubMed
Abstract

Insights

Researchers modeled the APC3 subunit, revealing its superhelical TPR domain structure. They identified a binding pocket for a natural APC inhibitor, aiding anti-cancer drug design targeting the anaphase-promoting complex (APC).

Area of Science:

  • Biochemistry
  • Structural Biology
  • Cell Biology

Background:

  • The anaphase-promoting complex (APC) is a crucial Cullin-RING E3 ligase regulating cell cycle control.
  • APC targets include anti-cancer agents due to its role in chromosome separation and mitotic exit.
  • The APC3 subunit is key for identifying APC activators Cdh1 and Cdc20.

Purpose of the Study:

  • To computationally model the structure of the APC3 subunit.
  • To investigate the binding of a natural inhibitory compound to APC3.

Main Methods:

  • Computational techniques were employed to develop the structural model of APC3.
  • The interaction between APC3 and a natural inhibitory compound was analyzed.

Main Results:

  • The APC3 structure exhibits numerous anti-parallel helices, forming a superhelical arrangement of tetratrico-peptide repeat (TPR) domains.
  • A specific binding pocket for a natural APC3 inhibitor was identified.

Conclusions:

  • The study provides insights into the mechanism of APC activation.
  • Findings facilitate the design of novel APC inhibitory compounds for therapeutic applications.
Keywords:
Anaphase promoting complexbioinformaticstetratrico-peptide repeat domain

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