Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTOVWYL9)

• DOT Name: Keratin-associated protein 5-2 (KRTAP5-2)
• Synonyms: Keratin-associated protein 5-8; Keratin-associated protein 5.2; Keratin-associated protein 5.8; Ultrahigh sulfur keratin-associated protein 5.2
• Gene Name: KRTAP5-2
• UniProt ID: KRA52_HUMAN
• Sequence:
  MGCCGCSRGCGSGCGGCGSSCGGCGSGCGGCGSGRGGCGSGCGGCSSSCGGCGSRCYVPV
  CCCKPVCSWVPACSCTSCGSCGGSKGGCGSCGGSKGGCGSCGGSKGGCGSCGCSQSSCCK
  PCCCSSGCGSSCCQSSCCKPCCCQSSCCVPVCCQSSCCKPCCCQSNCCVPVCCQCKI
• Function: In the hair cortex, hair keratin intermediate filaments are embedded in an interfilamentous matrix, consisting of hair keratin-associated protein (KRTAP), which are essential for the formation of a rigid and resistant hair shaft through their extensive disulfide bond cross-linking with abundant cysteine residues of hair keratins. The matrix proteins include the high-sulfur and high-glycine-tyrosine keratins.
• Tissue Specificity: Restricted to hair root, not detected in any other tissues.
• Reactome Pathway: Keratinization (R-HSA-6805567)

Molecular Interaction Atlas (MIA) of This DOT

2 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Keratin-associated protein 5-2 (KRTAP5-2).	[1]
Milchsaure	DM462BT	Investigative	Milchsaure decreases the expression of Keratin-associated protein 5-2 (KRTAP5-2).	[2]

References

• [1] Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
• [2] Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.