Related Experiment Video

Updated: Aug 16, 2026

Cell Death Associated with Abnormal Mitosis Observed by Confocal Imaging in Live Cancer Cells
15:53

Cell Death Associated with Abnormal Mitosis Observed by Confocal Imaging in Live Cancer Cells

Published on: August 21, 2013

Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation

Takafumi Uchida1, Mari Takamiya, Morito Takahashi

  • 1Institute of Development, Aging and Cancer, Tohoku University, 4-1 Seiryo, Aoba, Sendai 980-8575, Japan. uchidat@idac.tohoku.ac.jp

Chemistry & Biology
|February 8, 2003
PubMed

Insights

Pin1 inhibitors block cell proliferation by targeting the Pin1 peptidyl prolyl isomerase (PPIase) enzyme. This research identified novel Pin1 inhibitors with potential as anticancer drugs.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The parvulin family peptidyl prolyl isomerase (PPIase) Pin1 plays a crucial role in regulating cell cycle progression.
  • Disruption of the Pin1 gene delays cell cycle reentry in primary mouse embryo fibroblasts.
  • Pin1's role in cell cycle regulation suggests that Pin1 inhibitors could impede cancer cell proliferation.

Purpose of the Study:

  • To identify novel inhibitors of human Pin1 PPIase activity.
  • To evaluate the potential of these inhibitors as anticancer agents.

Main Methods:

  • Screening of a chemical compound library for molecules inhibiting human Pin1 PPIase activity in vitro.
  • Assessing the inhibitory effects of compounds on cancer cell line growth.
  • Evaluating the nonspecific toxicity of identified inhibitors.

Main Results:

  • A set of compounds was identified that inhibit human Pin1 PPIase activity in vitro with low microM IC50 values.
  • These compounds demonstrated inhibition of growth in several cancer cell lines.
  • Diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn] phenanthroline-2,7-diacetate (PiB) exhibited the least nonspecific toxicity among the identified inhibitors.

Conclusions:

  • Pin1 inhibitors can effectively block cell proliferation by targeting Pin1 PPIase activity.
  • The identified Pin1 inhibitors, particularly PiB, show promise as a novel class of anticancer drugs.

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology07:04

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

Published on: May 2, 2025

Related Concept Videos

Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
Phosphoinositides and PIPs01:42

Phosphoinositides and PIPs

Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the daughter...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...