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Items: 30

1.

SGLT2 knockout prevents hyperglycemia and is associated with reduced pancreatic β-cell death in genetically obese mice.

Jurczak MJ, Saini S, Ioja S, Costa DK, Udeh N, Zhao X, Whaley JM, Kibbey RG.

Islets. 2018;10(5):181-189. doi: 10.1080/19382014.2018.1503027. Epub 2018 Aug 17.

2.

Unique pharmacology of a novel allosteric agonist/sensitizer insulin receptor monoclonal antibody.

Hinke SA, Cieniewicz AM, Kirchner T, D'Aquino K, Nanjunda R, Aligo J, Perkinson R, Cooper P, Boayke K, Chiu ML, Jarantow S, Lacy ER, Liang Y, Johnson DL, Whaley JM, Lingham RB, Kihm AJ.

Mol Metab. 2018 Apr;10:87-99. doi: 10.1016/j.molmet.2018.01.014. Epub 2018 Feb 3.

3.

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.

Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27.

PMID:
29316397
4.

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9.

PMID:
28112924
5.

Novel Monoclonal Antibody Is an Allosteric Insulin Receptor Antagonist That Induces Insulin Resistance.

Cieniewicz AM, Kirchner T, Hinke SA, Nanjunda R, D'Aquino K, Boayke K, Cooper PR, Perkinson R, Chiu ML, Jarantow S, Johnson DL, Whaley JM, Lacy ER, Lingham RB, Liang Y, Kihm AJ.

Diabetes. 2017 Jan;66(1):206-217. doi: 10.2337/db16-0633. Epub 2016 Oct 26.

6.

Carcinogenicity risk assessment supports the chronic safety of dapagliflozin, an inhibitor of sodium-glucose co-transporter 2, in the treatment of type 2 diabetes mellitus.

Reilly TP, Graziano MJ, Janovitz EB, Dorr TE, Fairchild C, Lee F, Chen J, Wong T, Whaley JM, Tirmenstein M.

Diabetes Ther. 2014 Jun;5(1):73-96. doi: 10.1007/s13300-014-0053-3. Epub 2014 Jan 29.

7.

Nonclinical toxicology assessments support the chronic safety of dapagliflozin, a first-in-class sodium-glucose cotransporter 2 inhibitor.

Tirmenstein M, Dorr TE, Janovitz EB, Hagan D, Abell LM, Onorato JM, Whaley JM, Graziano MJ, Reilly TP.

Int J Toxicol. 2013 Sep-Oct;32(5):336-50. doi: 10.1177/1091581813505331. Epub 2013 Oct 4.

PMID:
24097127
8.

Targeting the kidney and glucose excretion with dapagliflozin: preclinical and clinical evidence for SGLT2 inhibition as a new option for treatment of type 2 diabetes mellitus.

Whaley JM, Tirmenstein M, Reilly TP, Poucher SM, Saye J, Parikh S, List JF.

Diabetes Metab Syndr Obes. 2012;5:135-48. doi: 10.2147/DMSO.S22503. Epub 2012 Jul 23.

9.

Targeting renal glucose reabsorption for the treatment of type 2 diabetes mellitus using the SGLT2 inhibitor dapagliflozin.

Jabbour SA, Whaley JM, Tirmenstein M, Poucher SM, Reilly TP, Boulton DW, Saye J, List JF, Parikh S.

Postgrad Med. 2012 Jul;124(4):62-73. doi: 10.3810/pgm.2012.07.2569. Review.

PMID:
22913895
10.

Quantitative PCR tissue expression profiling of the human SGLT2 gene and related family members.

Chen J, Williams S, Ho S, Loraine H, Hagan D, Whaley JM, Feder JN.

Diabetes Ther. 2010 Dec;1(2):57-92. doi: 10.1007/s13300-010-0006-4. Epub 2010 Dec 17.

11.

Glucose dynamics and mechanistic implications of SGLT2 inhibitors in animals and humans.

List JF, Whaley JM.

Kidney Int Suppl. 2011 Mar;(120):S20-7. doi: 10.1038/ki.2010.512. Review.

12.

SGLT2 deletion improves glucose homeostasis and preserves pancreatic beta-cell function.

Jurczak MJ, Lee HY, Birkenfeld AL, Jornayvaz FR, Frederick DW, Pongratz RL, Zhao X, Moeckel GW, Samuel VT, Whaley JM, Shulman GI, Kibbey RG.

Diabetes. 2011 Mar;60(3):890-8. doi: 10.2337/db10-1328.

13.

Inhibition of SGLT2: a novel strategy for treatment of type 2 diabetes mellitus.

Pfister M, Whaley JM, Zhang L, List JF.

Clin Pharmacol Ther. 2011 Apr;89(4):621-5. doi: 10.1038/clpt.2011.16. Epub 2011 Feb 23. Review. No abstract available.

PMID:
21346749
14.

The novel sodium glucose transporter 2 inhibitor dapagliflozin sustains pancreatic function and preserves islet morphology in obese, diabetic rats.

Macdonald FR, Peel JE, Jones HB, Mayers RM, Westgate L, Whaley JM, Poucher SM.

Diabetes Obes Metab. 2010 Nov;12(11):1004-12. doi: 10.1111/j.1463-1326.2010.01291.x.

PMID:
20880347
15.

In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans.

Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG.

Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8.

PMID:
19996149
16.

Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.

Mapelli C, Natarajan SI, Meyer JP, Bastos MM, Bernatowicz MS, Lee VG, Pluscec J, Riexinger DJ, Sieber-McMaster ES, Constantine KL, Smith-Monroy CA, Golla R, Ma Z, Longhi DA, Shi D, Xin L, Taylor JR, Koplowitz B, Chi CL, Khanna A, Robinson GW, Seethala R, Antal-Zimanyi IA, Stoffel RH, Han S, Whaley JM, Huang CS, Krupinski J, Ewing WR.

J Med Chem. 2009 Dec 10;52(23):7788-99. doi: 10.1021/jm900752a.

PMID:
19702274
17.

Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

Ellsworth BA, Meng W, Patel M, Girotra RN, Wu G, Sher PM, Hagan DL, Obermeier MT, Humphreys WG, Robertson JG, Wang A, Han S, Waldron TL, Morgan NN, Whaley JM, Washburn WN.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4770-3. doi: 10.1016/j.bmcl.2008.07.109. Epub 2008 Jul 31.

PMID:
18707880
18.

Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats.

Han S, Hagan DL, Taylor JR, Xin L, Meng W, Biller SA, Wetterau JR, Washburn WN, Whaley JM.

Diabetes. 2008 Jun;57(6):1723-9. doi: 10.2337/db07-1472. Epub 2008 Mar 20.

19.

Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN.

J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q. Epub 2008 Feb 9.

PMID:
18260618
20.

Alternate choice of initiation codon produces a biologically active product of the von Hippel Lindau gene with tumor suppressor activity.

Blankenship C, Naglich JG, Whaley JM, Seizinger B, Kley N.

Oncogene. 1999 Feb 25;18(8):1529-35.

21.

The von Hippel-Lindau tumor suppressor protein is required for proper assembly of an extracellular fibronectin matrix.

Ohh M, Yauch RL, Lonergan KM, Whaley JM, Stemmer-Rachamimov AO, Louis DN, Gavin BJ, Kley N, Kaelin WG Jr, Iliopoulos O.

Mol Cell. 1998 Jun;1(7):959-68.

22.

Tau protein in cerebrospinal fluid as an aid in the diagnosis of Alzheimer's disease.

Munroe WA, Southwick PC, Chang L, Scharre DW, Echols CL Jr, Fu PC, Whaley JM, Wolfert RL.

Ann Clin Lab Sci. 1995 May-Jun;25(3):207-17.

PMID:
7605102
24.

Germ-line mutations in the von Hippel-Lindau tumor-suppressor gene are similar to somatic von Hippel-Lindau aberrations in sporadic renal cell carcinoma.

Whaley JM, Naglich J, Gelbert L, Hsia YE, Lamiell JM, Green JS, Collins D, Neumann HP, Laidlaw J, Li FP, et al.

Am J Hum Genet. 1994 Dec;55(6):1092-102. Erratum in: Am J Hum Genet 1995 Jan;56(1):356.

25.

Comparative study of p53 gene and protein alterations in human astrocytic tumors.

Louis DN, von Deimling A, Chung RY, Rubio MP, Whaley JM, Eibl RH, Ohgaki H, Wiestler OD, Thor AD, Seizinger BR.

J Neuropathol Exp Neurol. 1993 Jan;52(1):31-8.

PMID:
8381161
26.

Cytogenetic and molecular studies of a familial renal cell carcinoma.

Decker HJ, Wullich B, Whaley JM, Herrera G, Klauck SM, Sandberg AA, Yandell DW, Seizinger BR.

Cancer Genet Cytogenet. 1992 Oct 1;63(1):25-31.

PMID:
1423222
27.

Efficient mutation induction by 125I and 131I decays in DNA of human cells.

Whaley JM, Little JB.

Radiat Res. 1990 Jul;123(1):68-74.

PMID:
2371380
28.

Chromosome 17p deletions and p53 gene mutations associated with the formation of malignant neurofibrosarcomas in von Recklinghausen neurofibromatosis.

Menon AG, Anderson KM, Riccardi VM, Chung RY, Whaley JM, Yandell DW, Farmer GE, Freiman RN, Lee JK, Li FP, et al.

Proc Natl Acad Sci U S A. 1990 Jul;87(14):5435-9.

29.

Mutation induction by 125iodoacetylproflavine, a DNA-intercalating agent, in human cells.

Whaley JM, Kassis AI, Kinsey BM, Adelstein SJ, Little JB.

Int J Radiat Biol. 1990 Jun;57(6):1087-103.

PMID:
1971836
30.

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