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Review

Synthetic ligands for PPARγ - review of patent literature 1994 - 1999

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Pages 623-634 | Published online: 25 Feb 2005

Bibliography

  • OLEFSKY JM: Insulin resistance in non-insulin dependent diabetes mellitus. Curr. Opin. Endocrinol. & Diabetes (1995) 2(4):290–299.
  • LEAHY JL: 6-cell dysfunction in Type II diabetes mellitus. Curr. Opin. Endocrinol. & Diabetes (1995) 2(4) :300–306.
  • GROOP LC: Sulfonylureas in NIDDM. Diabetes Care (1993) 15:737–754.
  • PETERS AL, DAVIDSON MB: Sulfonylureas in the treatment of Type II diabetes. Curr. Opin. Endocrinol & Diabetes (1995) 2(4):325–332.
  • UK PROSPECTIVE DIABETES STUDY (UKPDS) GROUP: Effect of intensive blood-glucose control with metformin in overweight patients with Type 2 diabetes (UKPDS 34). Lancet (1998) 352:854–865.
  • DUNN CJ, PETERS DH: Metformin - a review of its pharmacological properties and therapeutic use in non-insulin dependent diabetes mellitus. Drugs (1995) 49 (5):721–749.
  • HULIN B, MCCARTHY PA, GIBBS ME: The glitazone family of antidiabetic agents. Curr. Pharm. Design (1996) 2:85–102.
  • JOHNSON MD, CAMPBELL LK, CAMPBELL RK: Troglita-zone: Review and assessment of its role in the treatment of patients with impaired glucose tolerance and diabetes mellitus. Ann. Pharmacol. (1998) 32:337–348.
  • AULT A: US FDA issues new troglitazone labelling. Lancet (1999) 353:2221.
  • SCRIP (28 May 1999) 2441:20.
  • SCRIP (21 July 1999) 2456:18.
  • MANGELSDORF DF, THUMMEL C, BEATO M et al: The nuclear receptor superfamily: the second decade. Cell (1995) 83:835–839.
  • FORMAN BM, CHEN J, EVANS RM: Hypolipidemic drugs, polyunsaturated fatty acids and eicosanoids are ligands for peroxisome proliferator-activated receptors a and S. Proc. Natl. Acad. Sci. USA (1997) 94:4312–4317.
  • KLIEWER SA, SUNDSETH SS, JONES SA: Fatty acids andeicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors a and ö. Proc Natl. Acad. Sci. USA (1997) 94:4318–4323.
  • ISSEMANN I, GREEN S: Activation of a member of thesteroid hormone receptor superfamily by peroxisome proliferators. Nature (1990) 347:645–650.
  • KLIEWER SA, FORMAN BM, BLUMBERG B et al.: Differen-tial expression and activation of a family of murine peroxisome proliferator-activated receptors. Proc. Natl. Acad. Sci. USA (1994) 91:7355–7359.
  • SOHDA T, MIZUNO K, IMAMIYA E et al.: Studies onantidiabetic agents II. Synthesis of 54441- methylcy-clohexylmethoxy)benzylithiazolidine-2,4-dione (ADD-3878) and its derivatives. Chem. Pharm. (1982) 30:3580–3600.
  • CHANG AY, WYSE BM, GILCHRIST et al: Ciglitazone, a new hypoglycemic agent. 1 Studies in ob/ob and db/db mice, diabetic chinese hamsters and normal and streptozotocin-diabetic rats. Diabetes (1983) 32:830–838.
  • ••First disclosure relating to insulin sensitising properties ofthiazolidinediones.
  • KLETZIEN RF, CLARK SD, ULRICH RG: Enhancement of adipocyte differentiation by an insulin-sensitizing agent. Mol Pharmacol (1992) 41:393–398.
  • TAFURI SR: Troglitazone enhances differentiation, basal glucose uptake and GLUT-1 protein levels in 3T3-L1 adipocytes. Endocrinol. (1996) 137:4706–4712.
  • TONTONEZ P, HU E, SPIEGELMAN BM: Stimulation ofadipogenesis in fibroblasts by PPARy2, a lipid-activated transcription factor. Cell (1994) 79:1147–1156.
  • LEHMANN JM, MOORE LB, SMITH OLIVER TA et al.: An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator activated receptor gamma. J. Biol. Chem. (1995) 270:12953–12956.
  • ••Discloses PPARy as the molecular target forthiazolidinediones.
  • WILLSON TM, COBB JE, COWAN DJ et al.: The structure- activity, relationship between peroxisome-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J. Med. Chem. (1996) 39:665–668.
  • ELBRECHT A, CHEN Y, CULLINAN CA et al: Molecular cloning, expression and characterisation of human peroxisome proliferator activated receptors yi and y2. Biochem. Biophys. Res. Commun. (1996) 224:431–437.
  • HULIN B NEWTON LS, LEWIS DM et al: Hypoglycaemic activity of a series of a-alkylthio and a-alkoxy carbox-ylic acids related to ciglitazone. J. Med. Chem. (1996) 39:3897–3907.
  • •First report of non thiazolidinedione insulin sensitiser before discovery of PPARy.
  • BUCKLE DR, CANTELLO BCC, CAWTHORNE MA et al.:Non thiazolidinedione antihyperglycaemic agents. 1: a-Heteroatom substituted p-phenylpropanoic acids. Bioorg. Med. Chem. Letts. (1996) 6:2121–2126.
  • BUCKLE DR, CANTELLO BCC, CAWTHORNE MA et al.:Non thiazolidinedione antihyperglycaemic agents. 2: a-carbon substituted p-phenylpropanoic acids. Bioorg. Med. Chem. Letts. (1996) 6:2127–2130.
  • HENCKE BR, BLANCHARD SG, FRACKEEN MF et al: N-(2-Benzoylpheny1)-t-tyrosine PPARy agonists. 1. Discovery of a novel series of potent antihypergly-caemic and antihyperlipidemic agents. J. Med. Chem. (1998) 41:5020–5036.
  • •Disclosure of tyrosine derivatives using recombinant PPAR for screening.
  • COLLINS JL, BLANCHARD SG, VAN BOSEWELL G et al: N,-(2-Benzoylpheny1)-t-tyrosine PPARy agonists. 2. Structure-activity relationship and optimisation of the phenyl alkyl ether moiety. J. Med. Chem. (1998) 41:5037–5054.
  • COBB JE, BLANCHARD SG, EVAN BOSEWELL1 G et al: N-(2-Benzoylpheny1)-t-tyrosine PPARy agonists. 3. Structure-activity relationship and optimisation of the N-aryl substituent. J. Med. Chem. (1998) 41:5055–5069.
  • WILLSON TM, BROWN PJ, STERNBACH DD et al.: The PPARs: From orphan receptors to drug discovery. J. Med. Chem. (2000) 43:527–550.
  • •Succinct review on PPAR ligands and pharmacology.
  • YOUNG PW, BUCKLE DR, CANTELLO BCC et al.: Identifi-cation of high affinity binding sites for the insulin sensitiser rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand. J. Pharmacol. Exp. Ther. (1998) 284:751–759.
  • PARKS DJ, TOMKINSON NCO, VILLENEUVE MS et al.: Differential activity of rosiglitazone enantiomers at PPARy. Bioorg. Med. Chem. Lett. (1998) 8:3657–3658.
  • BANTICK JR, BEATON HG, COOPER SL et al.: New non-peptide angiotensin II receptor antagonists. 1: Structure-activity relationships of a series of 2 (111)-pyridiones. Bioorg. Med. Chem. Lett. (1994) 4:121–126.
  • BIESER N, LABITZKE E, MEDERSKI WKRN et al: Synthesisof 7-ethyl-1,2-dihydroquinolin-2-ones as angiotensin II receptor antagonists. Heterocycles (1994) 39:117–131.
  • ZWAAGSTRA ME, TIMMERMAN H, TAMURA M et al.: Synthesis and strucutre-activity relationships of carboxylated chalcones: a novel series of Cys-LT1 (LTD4) receptor antagonists. J Med. Chem. (1997) 40:1075–1089.
  • SMITH SA: Peroxisome proliferator activated receptors(PPARy): molecular target for hypolipidaemic agents and insulin sensitisers. Pharmacol. Rev. Commun. (1996) 8:57–64.
  • WAHLI W, BRAISSANT 0, DESVERGNE B.: Peroxisome proliferator activated receptors: transcriptional regulators of adipogenesis, lipid metabolism and more. Curr. Biol. (1995) 2:261–266.
  • SHEPHERD J: Mechanism of action of fibrates. Postgrad. Med. J. (1993) 69:S34–S41.
  • BROWN PJ, SMITH-OLIVER TA CHARIFSON PS et al.: Identification of peroxisome proliferator-activated receptor ligands from biased chemical libraries. Chem. Biol. (1997) 4:909–918.
  • KLIEWER SA, SUNDSETH SS, JONES SA et al: Fatty acids and eicosanoids regluate gene expression through direct interactions with peroxisome proliferator-activated receptors a and y. Proc. Natl. Acad. Sci. USA (1997) 94:4318–4323.
  • MURAKAMI K, TOBE T, IDE T et al.: A novel insulin sensitiser acts as a coligand for peroxisome prolif-erator activated receptor-a and PPARy. Diabetes (1998) 47:1841–1847.
  • •First disclosure of thiazolidinedione with dual activity at PPARa and PPARy.
  • NOMURAM, KINOSHITA S, SATOH H et al: (3-Substituted benzy0thiazolidine-2,4-diones as structurally new antihyperglycaemic agents. Bioorg. Med. Chem. Lett. (1999) 9:533–538.
  • SCRIP (16 May 1997) 2232:22.
  • SCRIP (2 August 1999) 2460:21.
  • CANTELLO BCC, CAWTHORNE MA, COTTAM GP et al: [[w- (Heterocyclylamino)alkoxy]benzyll- 2,4 - thiazolidinediones as potent antihyperglycaemic agents. J. Med. Chem. (1994) 37:3977–3985.
  • BREIDER MA, GOUGH AW, HASKINS JR et al.: Troglitazone-induced heart and adipose tissue cell proliferation in mice. Toxicol. Pathol. (1999) 27:545–552.
  • MUKHERJEE R, DAVIES PJA, CROMBIE DL et al.: Sensitisa-tion of diabetic and obese mice to insulin by retinoid X receptor agonists. Nature (1997) 386:407–410.

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