Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

10.9K
Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
10.9K
Drug Discovery: Overview01:26

Drug Discovery: Overview

11.3K
Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
11.3K
DNA Microarrays02:34

DNA Microarrays

20.8K
Microarrays are high-throughput and relatively inexpensive assays that can be automated to analyze large quantities of data at a time. They are used in genome-wide studies to compare gene or protein expression under two varied conditions, such as healthy and diseased states. Microarrays consist of glass or silica slides on which probe molecules are covalently attached through surface functionalization. Most commonly, the slides are prepared through the chemisorption of silanes to silica...
20.8K
Molecules and Compounds02:38

Molecules and Compounds

68.4K
Atoms and Molecules
68.4K
Negative Regulator Molecules01:23

Negative Regulator Molecules

38.3K
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.
38.3K
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

618
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
618

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Correction to "A Focused DNA-Encoded Chemical Library for the Discovery of Inhibitors of NAD<sup>+</sup>-Dependent Enzymes".

Journal of the American Chemical Society·2021
Same author

System-wide identification and prioritization of enzyme substrates by thermal analysis.

Nature communications·2021
Same author

Engineering Af1521 improves ADP-ribose binding and identification of ADP-ribosylated proteins.

Nature communications·2020
Same author

Correction to "Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors".

Journal of medicinal chemistry·2019
Same author

A Focused DNA-Encoded Chemical Library for the Discovery of Inhibitors of NAD<sup>+</sup>-Dependent Enzymes.

Journal of the American Chemical Society·2019
Same author

A Potent and Selective PARP11 Inhibitor Suggests Coupling between Cellular Localization and Catalytic Activity.

Cell chemical biology·2018
Same journal

Selective Degradation of Polyurethanes in Mixed Plastic Wastes via Ir-Catalyzed Hydrogenolysis.

Angewandte Chemie (International ed. in English)·2026
Same journal

Covalent Organic Framework Photocatalysts: Decoding Linkage Chemistry in Hydrogen Peroxide Synthesis From Air and Water.

Angewandte Chemie (International ed. in English)·2026
Same journal

Anomeric Amide Enabled Divergent Synthesis of Unsymmetrical Ureas, Carbamates, Thioesters, and Amides From Aldehydes.

Angewandte Chemie (International ed. in English)·2026
Same journal

Anisotropic Magneto-Chiral Dichroism in Lanthanide Complexes.

Angewandte Chemie (International ed. in English)·2026
Same journal

Engineering LE-CT State Synergy in Aminoboranes for Single Molecule White Light Emission and Dual-Mode Chiroptical/Phosphorescence Output.

Angewandte Chemie (International ed. in English)·2026
Same journal

Editable Hydrogen Bond Network Within the Electric Double Layer for CO<sub>2</sub> Reduction.

Angewandte Chemie (International ed. in English)·2026
See all related articles

Related Experiment Video

Updated: Jan 25, 2026

Fluorescence-Based Detection of FEN1 Nuclease Activity and Screening of Small-Molecule Inhibitors
05:46

Fluorescence-Based Detection of FEN1 Nuclease Activity and Screening of Small-Molecule Inhibitors

Published on: June 27, 2025

553

Small Molecule Microarray Based Discovery of PARP14 Inhibitors.

Bo Peng1, Ann-Gerd Thorsell2, Tobias Karlberg2

  • 1Department of Chemistry, National University of Singapore, 3 Science Drive, Singapore, 117543, Singapore.

Angewandte Chemie (International Ed. in English)
|December 6, 2016
PubMed
Summary
This summary is machine-generated.

Researchers developed a new method to screen over 1000 potential inhibitors, discovering a potent PARP14 inhibitor (H10) selective over PARP1. This compound effectively reduced PARP14 activity in tumor cells.

Keywords:
PARP inhibitorsX-ray crystallographyclick chemistryhigh-throughput screeningmicroarrays

More Related Videos

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

8.3K
Microarray-based Identification of Individual HERV Loci Expression: Application to Biomarker Discovery in Prostate Cancer
13:19

Microarray-based Identification of Individual HERV Loci Expression: Application to Biomarker Discovery in Prostate Cancer

Published on: November 2, 2013

17.1K

Related Experiment Videos

Last Updated: Jan 25, 2026

Fluorescence-Based Detection of FEN1 Nuclease Activity and Screening of Small-Molecule Inhibitors
05:46

Fluorescence-Based Detection of FEN1 Nuclease Activity and Screening of Small-Molecule Inhibitors

Published on: June 27, 2025

553
Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

8.3K
Microarray-based Identification of Individual HERV Loci Expression: Application to Biomarker Discovery in Prostate Cancer
13:19

Microarray-based Identification of Individual HERV Loci Expression: Application to Biomarker Discovery in Prostate Cancer

Published on: November 2, 2013

17.1K

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Poly(ADP-ribose) polymerases (PARPs) are crucial enzymes involved in DNA repair and other cellular functions.
  • Existing small-molecule inhibitors primarily target PARP1, often lacking selectivity.
  • PARP14 is an emerging therapeutic target, but inhibitor development is less advanced.

Purpose of the Study:

  • To develop a high-throughput screening strategy for identifying novel PARP inhibitors.
  • To discover potent and selective inhibitors targeting PARP14.
  • To characterize the binding mode and structure-activity relationships of identified inhibitors.

Main Methods:

  • Utilized a small molecule microarray-based strategy for parallel synthesis and screening.
  • Screened over 1000 potential bidentate inhibitors against PARPs.
  • Employed co-crystallization to determine the binding complex structure.
  • Conducted structure-activity relationship studies.

Main Results:

  • Successfully discovered a potent PARP14 inhibitor, designated H10.
  • H10 demonstrated >20-fold selectivity for PARP14 over PARP1.
  • Co-crystallization revealed H10 binds to both nicotinamide and adenine subsites of PARP14.
  • Structure-activity relationship studies elucidated key binding elements in the adenine subsite.
  • H10 effectively reduced endogenous PARP14 activity in tumor cells.

Conclusions:

  • The developed microarray strategy is effective for high-throughput inhibitor discovery.
  • H10 represents a promising lead compound for PARP14-targeted therapeutics.
  • Understanding the binding interactions facilitates the design of more selective PARP inhibitors.