Related Experiment Video

Updated: Jul 4, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
08:36

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3

Published on: April 7, 2023

1.2K

Progress with YAP/TAZ-TEAD inhibitors: a patent review (2018-present)

Benjamin Zagiel1, Patricia Melnyk1, Philippe Cotelle1

  • 1Lille Neuroscience and Cognition Research Center, University of Lille, INSERM, CHU Lille, UMR-S 1172, Lille, France.

Expert Opinion on Therapeutic Patents
|June 29, 2022
PubMed
Abstract

Insights

Small-molecule inhibitors targeting the YAP/TAZ-TEAD complex offer new cancer treatment strategies. Recent patents and clinical trials focus on these inhibitors, particularly non-covalent TEAD ligands.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The Hippo pathway, particularly the YAP/TAZ-TEAD transcriptional complex, is implicated in various cancers.
  • Overexpression of YAP/TAZ and TEAD is observed in cancers, with YAP contributing to drug resistance.

Purpose of the Study:

  • To review patent applications disclosing small-molecule inhibitors of the YAP/TAZ-TEAD interaction.
  • To categorize and analyze the landscape of TEAD transcriptional inhibitors in cancer therapy.

Main Methods:

  • Systematic review of international patent applications (2017-2022) using Sci-finder with the query 'TEAD'.
  • Classification of inhibitors based on their mechanism of action and binding site.

Main Results:

  • Approximately 30 international patents disclose TEAD transcriptional inhibitors filed since 2018.
  • Inhibitors are categorized into external TEAD ligands, non-covalent palmitate pocket ligands, and covalent palmitate pocket ligands.
  • The first clinical trial phase 1 drugs are non-covalent TEAD ligands; selective TEAD ligands are also patented.

Conclusions:

  • The YAP/TAZ-TEAD transcriptional complex is a promising therapeutic target for cancer treatment.
  • Development of small-molecule inhibitors, including selective TEAD ligands, is advancing rapidly, with early clinical trials underway.
  • Targeting the YAP/TAZ-TEAD pathway holds potential for personalized cancer medicine.
Keywords:
NF2-deficiencyTranscriptional factors TEADYAP/TAZcancershippo pathwayselectivity

More Related Videos

Y-90 Radioembolization and PD-1 Inhibitor as Neoadjuvant Treatment in Hepatocellular Carcinoma09:11

Y-90 Radioembolization and PD-1 Inhibitor as Neoadjuvant Treatment in Hepatocellular Carcinoma

Published on: May 24, 2024

588
Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors10:29

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

1.5K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Treatment Resistent Cancers02:56

Treatment Resistent Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
Clinical Trials: Overview01:11

Clinical Trials: Overview

Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Drug Administration and Therapy Phases: Overview01:26

Drug Administration and Therapy Phases: Overview

Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
FDA Approved Drugs: Changes to Approved Drugs01:26

FDA Approved Drugs: Changes to Approved Drugs

Post-approval, manufacturers may modify an approved new or generic drug product. Such modifications can encompass alterations in the Active Pharmaceutical Ingredient (API), manufacturing process, formulation, batch size, manufacturing site, and container closure system (FDA Guidance for Industry, April 2004). Often, a drug product may undergo multiple changes.These modifications require careful evaluation to determine their potential impact on the drug product's identity, strength, quality,...