Abstract
The discoidin domain receptors (DDRs) play crucial roles in the regulation of fundamental cellular processes, such as proliferation, survival, differentiation, adhesion, and matrix remodeling. Dysregulation of DDRs has been linked to many human diseases, including fibrotic disorders, atherosclerosis, and cancer. Thus, DDRs have been considered as emerging potential molecular targets for new drug discovery. Several classes of DDR small molecular inhibitors have been discovered in recent years. This chapter will provide an updated overview on the chemical structures, mechanism of action (MOA), and potential medical implications of the newly identified DDR small molecule inhibitors.
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Abbreviations
- DDRs:
-
Discoidin domain receptors
- 2D:
-
Two dimensional
- DS:
-
Discoidin domain
- ECM:
-
Extracellular matrix
- EJXM:
-
Extracellular juxtamembrane
- FDA:
-
Food and Drug Administration
- FLiK:
-
Fluorescent labels in kinases
- FUSION:
-
Functional Signature-Based Ontology
- IJXM:
-
Intracellular juxtamembrane
- IR:
-
Insulin receptor
- KD:
-
Kinase domain
- MOA:
-
Mechanism of action
- NMR:
-
Nuclear magnetic resonance
- NSCLC:
-
Non-small cell lung cancer
- PK:
-
Pharmacokinetics
- PMBCl:
-
para-Methoxybenzyl chloride
- QSAR:
-
Quantitative structure-activity relationship
- RTKs:
-
Receptor tyrosine kinases
- SQCC:
-
Squamous lung cancer
- S768R:
-
Serine 768 to arginine 768
- TMT:
-
Transmembrane
- VEGFR:
-
Vascular endothelial growth factor receptor
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Lu, X., Ding, K. (2016). Small Molecule Inhibitors of Discoidin Domain Receptors (DDRs). In: Fridman, R., Huang, P. (eds) Discoidin Domain Receptors in Health and Disease. Springer, New York, NY. https://doi.org/10.1007/978-1-4939-6383-6_10
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