Target intelligence / Profile preview

MicroRNA 221-5p (miR-221-5p)

Target
miR-221-5p
Molecular classification
MicroRNA (miRNA), Non-coding RNA, Regulatory RNA molecule
01

Overview

MicroRNA 221–5p is a short non-coding RNA molecule, part of the microRNA family that regulates gene expression post-transcriptionally by binding complementary sequences on target messenger RNAs. It is transcribed from a cluster with its paralogue miR‑222 on chromosome X. MiR‑221–5p has been extensively studied as an oncogenic microRNA, promoting tumor growth by downregulating tumor suppressors such as CD117 and DIRAS3; it also modulates processes like angiogenesis, epithelial-to-mesenchymal transition (EMT), cell proliferation/migration/invasion across various cancers including liver, prostate, breast, lung, thyroid carcinomas among others. Its dysregulation has diagnostic/prognostic value—e.g., non-invasive colorectal cancer screening—and it represents an emerging therapeutic target using antisense technologies. However, its pleiotropic effects pose safety concerns when considering systemic inhibition.

Other names
miR-221MIR221microRNA 221miR-221/222 cluster
02

Mechanism of action

Antisense inhibition of miR‑221 leads to derepression of its mRNA targets—restoring tumor suppressor gene expression or reducing oncogene activity. Modulation affects cell cycle genes, apoptosis regulators, angiogenesis factors.

03

Biological functions

Regulation of gene expression at the post-transcriptional levelCell proliferation and migration controlAngiogenesis modulation (both antiangiogenic and proangiogenic roles depending on context)Apoptosis regulationEpithelial-to-mesenchymal transition (EMT) promotion in cancer cells
04

Disease associations

Cancer (oncogenic role in multiple cancers including liver, prostate, thyroid, breast, glioblastoma, lung, colorectal)Tumor progression and metastasis facilitatorPrognostic marker for poor survival in renal cell carcinoma and other tumorsDiagnostic/prognostic biomarker for colorectal cancer via non-invasive detection in fecesInvolved in androgenetic alopecia (hair loss disorder)Inflammatory diseases such as acute gouty arthritis by targeting IL‑1β
05

Safety considerations

Off-target effects due to broad regulatory roles across many genes.Delivery issues for nucleic acid-based therapeutics.Context-dependent duality—can act as both oncogene and tumor suppressor depending on tissue/cancer type.
06

Interacting drugs

Antisense oligonucleotides

2 more in the full profile.

07

Biomarkers

Colorectal cancer screening via fecal detectionPrognosis prediction in several cancers including renal cell carcinoma, hepatocellular carcinoma, papillary thyroid carcinoma, etc.

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