Therapeutic Target Details
| Target ID: | T01 |
| Target Name: | Insulin receptor |
| Synonyms: | Insulin receptor; Insulin receptor subunit alpha; Insulin receptor subunit beta; CD_antigen=CD220; 2.7.10.1 |
| GENE: | INSR |
| Action: | AGONIST; INHIBITOR |
| Class: | Target is a single protein chain |
| UniProtKB ID: | P06213 |
| Entry Name: | INSR_HUMAN |
| Related Drugs: | Bms-754807; Kw-2450; Linsitinib |
| Mechanism: | Insulin receptor agonist; Insulin receptor inhibitor |
| Reference (PMIDs): | 17671083; 19996272; 21425998; 21875414; 25208878; 26988411; 27723227; 31436533 |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B000148 | CHEMBL6246 | Small molecule | ELLAGIC ACID | 302.19 | C14H6O8 | ACID | Details |
| B000250 | CHEMBL10 | Small molecule | SB-203580 | 377.44 | C21H16FN3OS | NEUTRAL | Details |
| B000273 | CHEMBL440084 | Small molecule | SB-431542 | 384.4 | C22H16N4O3 | NEUTRAL | Details |
| B000923 | CHEMBL413 | Small molecule | SIROLIMUS | 914.19 | C51H79NO13 | NEUTRAL | Details |
| B012922 | CHEMBL274654 | Small molecule | ORANTINIB | 310.35 | C18H18N2O3 | ACID | Details |
| B013048 | CHEMBL535 | Small molecule | SUNITINIB | 398.48 | C22H27FN4O2 | BASE | Details |
| B013629 | CHEMBL274064 | Small molecule | SB-220025 | 338.39 | C18H19FN6 | BASE | Details |
| B014221 | CHEMBL14762 | Small molecule | SELICICLIB | 354.46 | C19H26N6O | NEUTRAL | Details |
| B014366 | CHEMBL428690 | Small molecule | ALVOCIDIB | 401.85 | C21H20ClNO5 | NEUTRAL | Details |
| B014785 | CHEMBL553 | Small molecule | ERLOTINIB | 393.44 | C22H23N3O4 | NEUTRAL | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00005 | 10480624 | Diabetes | A polymorphism (K121Q) of the human glycoprotein PC-1 gene coding region is strongly associated with insulin resistance. | Details |
| A00006 | 10525667 | Diabetologia | Search for variants of the gene-promoter and the potential phosphotyrosine encoding sequence of the insulin receptor substrate-2 gene: evaluation of their relation with alterations in insulin secretion and insulin sensitivity. | Details |
| A00019 | 11030756 | Hum Mol Genet | Interaction between the G1057D variant of IRS-2 and overweight in the pathogenesis of type 2 diabetes. | Details |
| A00026 | 11473060 | Diabetes | New amino acid substitutions in the IRS-2 gene in Finnish and Chinese subjects with late-onset type 2 diabetes. | Details |
| A00029 | 11600548 | J Clin Endocrinol Metab | The prevalent Gly1057Asp polymorphism in the insulin receptor substrate-2 gene is not associated with impaired insulin secretion. | Details |
| A00031 | 11739459 | J Clin Endocrinol Metab | The Q121 PC-1 variant and obesity have additive and independent effects in causing insulin resistance. | Details |
| A00044 | 12679424 | J Clin Endocrinol Metab | A novel T608R missense mutation in insulin receptor substrate-1 identified in a subject with type 2 diabetes impairs metabolic insulin signaling. | Details |
| A00053 | 1314826 | J Biol Chem | Substitution of isoleucine for methionine at position 1153 in the beta-subunit of the human insulin receptor. A mutation that impairs receptor tyrosine kinase activity, receptor endocytosis, and insulin action. | Details |
| A00057 | 14671192 | J Clin Endocrinol Metab | Genetic polymorphism PC-1 K121Q and ethnic susceptibility to insulin resistance. | Details |
| A00064 | 15126519 | J Clin Endocrinol Metab | The association of the K121Q polymorphism of the plasma cell glycoprotein-1 gene with type 2 diabetes and hypertension depends on size at birth. | Details |
| A00065 | 15166380 | Science | A family with severe insulin resistance and diabetes due to a mutation in AKT2. | Details |
| A00070 | 15924147 | Nat Med | Lack of the architectural factor HMGA1 causes insulin resistance and diabetes in humans and mice. | Details |
| A00075 | 1607076 | Diabetes | NIDDM associated with mutation in tyrosine kinase domain of insulin receptor gene. | Details |
| A00105 | 17906635 | Nat Med | Crucial role of a long-chain fatty acid elongase, Elovl6, in obesity-induced insulin resistance. | Details |
| A00117 | 1890161 | J Clin Endocrinol Metab | A mutation in the tyrosine kinase domain of the insulin receptor associated with insulin resistance in an obese woman. | Details |
| A00121 | 19164855 | J Clin Invest | Postreceptor insulin resistance contributes to human dyslipidemia and hepatic steatosis. | Details |
| A00123 | 1963473 | Mol Endocrinol | Functional properties of a naturally occurring Trp1200----Ser1200 mutation of the insulin receptor. | Details |
| A00138 | 21364139 | JAMA | Functional variants of the HMGA1 gene and type 2 diabetes mellitus. | Details |
| A00158 | 26150605 | J Am Soc Nephrol | The PROPKD Score: A New Algorithm to Predict Renal Survival in Autosomal Dominant Polycystic Kidney Disease. | Details |
| A00186 | 32939031 | Genet Med | Clinical impact of genomic testing in patients with suspected monogenic kidney disease. | Details |