High impact information on INSL5

• In a saturation binding assay, (125)I-INSL5 binds GPCR142 with a K(d) value of 2.5 nM [1].
• INSL5 inhibits (125)I-relaxin-3 binding to GPCR135 with a low potency (K(i) = 500 nM) [1].
• Overall, INSL5 behaves as an agonist for GPCR142 similar to relaxin-3 [1].
• Insulin-like peptide 5 (INSL5) is a peptide that belongs to the relaxin/insulin family, and its receptor has not been identified [1].
• In addition, INSL5 (up to 1 microm) shows no affinity or activity at LGR7 or LGR8 either in a binding assay or a bio-functional assay [1].

Biological context of INSL5

• By radiation hybrid mapping and the use of surrounding markers, human INSL5 maps to chromosome 1 in the 1p31.1 to 1p22.3 region [2].

Anatomical context of INSL5

• Using quantitative RT-PCR, expression of murine INSL5 was detected in the highest quantity in colon followed by thymus, and minimal expression was seen in testis [2].

Associations of INSL5 with chemical compounds

• In addition, INSL5 stimulates Ca(2+) mobilization in HEK293 cells expressing GPCR142 and G alpha(16) [1].
• In functional guanosine (gamma-thio)-triphosphate binding and cAMP accumulation assays, INSL5 potently activates GPCR142 with EC(50) values of 1.3 and 1.2 nM, respectively [1].
• A new member of the insulin gene superfamily (INSL5) was identified by searching EST databases for the presence of the conserved insulin B-chain cysteine motif [2].

Other interactions of INSL5

• In this report, we demonstrate that INSL5 is a specific agonist for GPCR142 [1].
• A functional assay shows that INSL5 (1 microm) is a weak antagonist for GPCR135 [1].

Analytical, diagnostic and therapeutic context of INSL5

• Northern blot analysis detected expression of human INSL5 in rectal, colon, and uterine tissue and of murine INSL5 only in thymic tissue [2].

References