Target Information

Target General Infomation
Target ID
T42928
Former ID
TTDI02071
Target Name
FGF-21 ligand
Gene Name
FGF21
Synonyms
Fibroblast growth factor 21; FGF21
Target Type
Clinical Trial
Disease Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Stimulates glucose uptake in differentiated adipocytes via the induction of glucose transporter SLC2A1/GLUT1 expression (but not SLC2A4/GLUT4 expression). Activity requires the presence of KLB.
BioChemical Class
Growth factor
UniProt ID
Q9NSA1
Sequence
MDSDETGFEHSGLWVSVLAGLLLGACQAHPIPDSSPLLQFGGQVRQRYLYTDDAQQTEAH
LEIREDGTVGGAADQSPESLLQLKALKPGVIQILGVKTSRFLCQRPDGALYGSLHFDPEA
CSFRELLLEDGYNVYQSEAHGLPLHLPGNKSPHRDPAPRGPARFLPLPGLPPALPEPPGI
LAPQPPDVGSSDPLSMVGPSQGRSPSYAS
Drugs and Mode of Action
Drug(s) PF-05231023 Drug Info Phase 1 Type 2 diabetes [524400]
FGF-21 Drug Info Discontinued in Phase 1/2 Type 2 diabetes [548772]
Agonist FGF-21 Drug Info [548773]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
Ras signaling pathway
Rap1 signaling pathway
PI3K-Akt signaling pathway
Regulation of actin cytoskeleton
Pathways in cancer
Melanoma
Reactome Facilitative Na+-independent glucose transporters
Glucose transport
WikiPathways Regulation of Actin Cytoskeleton
Aryl Hydrocarbon Receptor
SREBP signalling
References
Ref 524400ClinicalTrials.gov (NCT01923389) Multiple Dose Study Of PF-05231023 In Obese Adult Subjects. U.S. National Institutes of Health.
Ref 548772Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028644)
Ref 533190Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Drug Metab Dispos. 2015 Jun;43(6):803-11.
Ref 548773Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028644)

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