Related Experiment Video

Updated: Sep 11, 2025

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

8.0K

Traf2- and Nck-interacting kinase inhibitors: a patent review (2008-2024)

Luoheng Qin1, Vladimir Aladinskiy2, David Gennert3

  • 1Insilico Medicine Shanghai Ltd, Shanghai, China.

Expert Opinion on Therapeutic Patents
|August 18, 2025
PubMed
Abstract

Insights

Small molecule Traf2- and Nck-interacting kinase (TNIK) inhibitors show promise, with one advancing to clinical trials for idiopathic pulmonary fibrosis. Challenges remain for oncology applications due to pathway complexity and drug-like properties.

Area of Science:

  • Biochemistry
  • Drug Discovery
  • Molecular Biology

Background:

  • Traf2- and Nck-interacting kinase (TNIK) is a key kinase involved in Wnt/β-catenin signaling, cytoskeleton organization, and immune responses.
  • TNIK is expressed across various tissues and implicated in oncology, neurological diseases, and fibrosis.
  • Small molecule inhibitors targeting TNIK are of significant therapeutic interest.

Purpose of the Study:

  • To review recent advancements in small molecule TNIK inhibitors disclosed in patents from 2008 to 2024.
  • To analyze the progress and challenges in developing TNIK inhibitors for various disease indications.

Main Methods:

  • Patent literature review focusing on small molecule TNIK inhibitors.
  • Analysis of inhibitor scaffolds, clinical trial progression, and reasons for advancement or attrition.

Main Results:

  • Over 10 patents describe multiple TNIK inhibitor scaffolds.
  • Only one inhibitor, INS018_055, has reached clinical trials for idiopathic pulmonary fibrosis.
  • Development for oncology is hindered by TNIK's role in oncogenic pathways and molecule-specific properties.

Conclusions:

  • Despite numerous patented scaffolds, clinical translation of TNIK inhibitors remains limited.
  • Kinase selectivity, physicochemical properties, and pharmacokinetics are critical for advancing TNIK inhibitors.
  • Further research is needed to overcome challenges in developing TNIK inhibitors for oncology and other diseases.
Keywords:
IPFPatent reviewTNIKclinical trial

More Related Videos

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

9.2K
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.4K

Related Concept Videos

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...
4.9K
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
5.7K
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...
7.8K
MAPK Signaling Cascades01:07

MAPK Signaling Cascades

Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
6.0K
NF-κB-dependent Signaling Pathway02:26

NF-κB-dependent Signaling Pathway

The transcription factor NF-κB was discovered in 1986 in the lab of Nobel laureate Professor David Baltimore, for its interaction with the immunoglobulin light chain enhancer in B-cells. After more than three decades of study, it is now evident that NF-κB regulates the expression of over 100 genes. Most of these genes play an essential role in the innate and adaptive immune responses as well as the inflammatory responses of animals.
NF-κB-dependent Signaling Mechanism
The...
7.8K
Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
5.7K