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Discoidin domain receptor inhibitors as anticancer agents: A systematic review on recent development of DDRs

Ganesh Prasad Shenoy¹, Rohit Pal¹, Gurubasavaraja Swamy Purwarga Matada¹

¹Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.

Bioorganic Chemistry

|November 17, 2022

Abstract:

Discoidin domain receptors (DDRs) are one of the less explored targets for the treatment of cancer which belong to receptor tyrosine kinases family. Discoidin domain receptors (DDRs) are a collagen-activated receptor tyrosine kinase and essential for controlling cellular functions like proliferation, morphogenesis, adhesion, differentiation, invasion, matrix remodeling, and migration. Although there are many targets and their inhibitors are reported which treat cancer. But most of drugs were amalgamated with moderate to severe side effects. This results in untreated cancerous cells. One of the reasons that cancer is considered challenging to treat because the targets were mutating rapidly and the inhibitor become less potent. The target identification is a tedious task for the researchers from the early 1990 s till date. When it comes to cancer, there has not been any magical stick to treat it undisputedly. Therefore, need for discovery of new receptor may helpful to overcome these difficulties. The development of DDR inhibitors has received a lot of attention ever since the target was discovered. In this review we have reported the development of most promising DDR1 and DDR2 small molecule inhibitors from the perspective of medicinal chemistry. We have also discussed about the clinical trials, recent patents, selectivity biological activity, and structure-activity relationship (SAR) of DDR1 and DDR2 inhibitors.

Insights

Discoidin domain receptor (DDR) inhibitors offer a promising new avenue for cancer treatment, addressing limitations of current therapies. This review highlights the development of DDR1 and DDR2 inhibitors, focusing on medicinal chemistry and clinical potential.

Area of Science:

Oncology
Medicinal Chemistry
Molecular Biology

Background:

Discoidin domain receptors (DDRs) are receptor tyrosine kinases activated by collagen.
DDRs regulate crucial cellular processes including proliferation, migration, and matrix remodeling.
Current cancer therapies face challenges due to target mutation and drug side effects.

Purpose of the Study:

To review the development of small molecule inhibitors targeting DDR1 and DDR2.
To explore the medicinal chemistry, biological activity, and clinical potential of these DDR inhibitors.
To provide insights into structure-activity relationships (SAR) for DDR1 and DDR2 inhibitors.

Main Methods:

Literature review of scientific publications and patents.
Analysis of medicinal chemistry approaches for DDR inhibitor development.
Discussion of biological activity, selectivity, and clinical trial data.

Main Results:

Several promising DDR1 and DDR2 small molecule inhibitors have been developed.
These inhibitors show potential for treating cancers with specific DDR pathway involvement.
Structure-activity relationship studies guide the optimization of inhibitor potency and selectivity.

Conclusions:

DDR inhibitors represent a novel therapeutic strategy for cancer treatment.
Further research and clinical trials are warranted to fully realize the potential of DDR inhibitors.
Targeting DDRs may overcome resistance mechanisms associated with conventional cancer therapies.

Read full analysis

Keywords:

Anti-cancer DDR1 DDR2 Mutations SAR Small molecules

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