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Items: 1 to 50 of 203

1.

Defining a conformational ensemble that directs activation of PPARγ.

Chrisman IM, Nemetchek MD, de Vera IMS, Shang J, Heidari Z, Long Y, Reyes-Caballero H, Galindo-Murillo R, Cheatham TE 3rd, Blayo AL, Shin Y, Fuhrmann J, Griffin PR, Kamenecka TM, Kojetin DJ, Hughes TS.

Nat Commun. 2018 May 4;9(1):1794. doi: 10.1038/s41467-018-04176-x.

2.

Lipid binding promotes the open conformation and tumor-suppressive activity of neurofibromin 2.

Chinthalapudi K, Mandati V, Zheng J, Sharff AJ, Bricogne G, Griffin PR, Kissil J, Izard T.

Nat Commun. 2018 Apr 6;9(1):1338. doi: 10.1038/s41467-018-03648-4.

3.

CINPA1 binds directly to constitutive androstane receptor and inhibits its activity.

Cherian MT, Chai SC, Wright WC, Singh A, Alexandra Casal M, Zheng J, Wu J, Lee RE, Griffin PR, Chen T.

Biochem Pharmacol. 2018 Jun;152:211-223. doi: 10.1016/j.bcp.2018.03.029. Epub 2018 Mar 31.

PMID:
29608908
4.

The AP-1-BATF and -BATF3 module is essential for growth, survival and TH17/ILC3 skewing of anaplastic large cell lymphoma.

Schleussner N, Merkel O, Costanza M, Liang HC, Hummel F, Romagnani C, Durek P, Anagnostopoulos I, Hummel M, Jöhrens K, Niedobitek A, Griffin PR, Piva R, Sczakiel HL, Woessmann W, Damm-Welk C, Hinze C, Stoiber D, Gillissen B, Turner SD, Kaergel E, von Hoff L, Grau M, Lenz G, Dörken B, Scheidereit C, Kenner L, Janz M, Mathas S.

Leukemia. 2018 Mar 28. doi: 10.1038/s41375-018-0045-9. [Epub ahead of print]

PMID:
29588546
5.

Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.

Lin H, Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Bayona CR, Cameron MD, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2018 May 1;28(8):1313-1319. doi: 10.1016/j.bmcl.2018.03.019. Epub 2018 Mar 8.

PMID:
29548571
6.

Identification of an aminothiazole series of RORβ modulators.

Patouret R, Doebelin C, Garcia-Ordonez RD, Chang MR, Ruiz C, Cameron MD, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2018 Apr 15;28(7):1178-1181. doi: 10.1016/j.bmcl.2018.03.001. Epub 2018 Mar 3.

PMID:
29534930
7.

Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.

Lin H, Long JZ, Roche AM, Svensson KJ, Dou FY, Chang MR, Strutzenberg T, Ruiz C, Cameron MD, Novick SJ, Berdan CA, Louie SM, Nomura DK, Spiegelman BM, Griffin PR, Kamenecka TM.

J Med Chem. 2018 Apr 12;61(7):3224-3230. doi: 10.1021/acs.jmedchem.8b00029. Epub 2018 Mar 22.

PMID:
29533650
8.

Interactome Analysis Reveals Regulator of G Protein Signaling 14 (RGS14) is a Novel Calcium/Calmodulin (Ca2+/CaM) and CaM Kinase II (CaMKII) Binding Partner.

Evans PR, Gerber KJ, Dammer EB, Duong DM, Goswami D, Lustberg DJ, Zou J, Yang JJ, Dudek SM, Griffin PR, Seyfried NT, Hepler JR.

J Proteome Res. 2018 Apr 6;17(4):1700-1711. doi: 10.1021/acs.jproteome.8b00027. Epub 2018 Mar 20.

PMID:
29518331
9.

Biophysical Interactions of Direct AMPK Activators.

Kurumbail RG, West GM, Dharmarajan V, Borzilleri KA, Withka JM, Ward J, Reyes AR, Rajamohan F, Griffin PR, Calabrese MF.

Methods Mol Biol. 2018;1732:29-55. doi: 10.1007/978-1-4939-7598-3_3.

PMID:
29480467
10.

Small molecule PGC-1α1 protein stabilizers induce adipocyte Ucp1 expression and uncoupled mitochondrial respiration.

Pettersson-Klein AT, Izadi M, Ferreira DMS, Cervenka I, Correia JC, Martinez-Redondo V, Southern M, Cameron M, Kamenecka T, Agudelo LZ, Porsmyr-Palmertz M, Martens U, Lundgren B, Otrocka M, Jenmalm-Jensen A, Griffin PR, Ruas JL.

Mol Metab. 2018 Mar;9:28-42. doi: 10.1016/j.molmet.2018.01.017. Epub 2018 Feb 3.

11.

Noncanonical agonist PPARγ ligands modulate the response to DNA damage and sensitize cancer cells to cytotoxic chemotherapy.

Khandekar MJ, Banks AS, Laznik-Bogoslavski D, White JP, Choi JH, Kazak L, Lo JC, Cohen P, Wong KK, Kamenecka TM, Griffin PR, Spiegelman BM.

Proc Natl Acad Sci U S A. 2018 Jan 16;115(3):561-566. doi: 10.1073/pnas.1717776115. Epub 2018 Jan 2.

PMID:
29295932
12.

HDX reveals the conformational dynamics of DNA sequence specific VDR co-activator interactions.

Zheng J, Chang MR, Stites RE, Wang Y, Bruning JB, Pascal BD, Novick SJ, Garcia-Ordonez RD, Stayrook KR, Chalmers MJ, Dodge JA, Griffin PR.

Nat Commun. 2017 Oct 13;8(1):923. doi: 10.1038/s41467-017-00978-7.

13.

Unique Interactome Network Signatures for Peroxisome Proliferator-activated Receptor Gamma (PPARγ) Modulation by Functional Selective Ligands.

Lam VQ, Zheng J, Griffin PR.

Mol Cell Proteomics. 2017 Dec;16(12):2098-2110. doi: 10.1074/mcp.RA117.000308. Epub 2017 Sep 29.

PMID:
28972081
14.

Nucleotide Binding to ARL2 in the TBCD∙ARL2∙β-Tubulin Complex Drives Conformational Changes in β-Tubulin.

Francis JW, Goswami D, Novick SJ, Pascal BD, Weikum ER, Ortlund EA, Griffin PR, Kahn RA.

J Mol Biol. 2017 Nov 24;429(23):3696-3716. doi: 10.1016/j.jmb.2017.09.016. Epub 2017 Sep 29.

PMID:
28970104
15.

SPA70 is a potent antagonist of human pregnane X receptor.

Lin W, Wang YM, Chai SC, Lv L, Zheng J, Wu J, Zhang Q, Wang YD, Griffin PR, Chen T.

Nat Commun. 2017 Sep 29;8(1):741. doi: 10.1038/s41467-017-00780-5.

16.

Synergistic Regulation of Coregulator/Nuclear Receptor Interaction by Ligand and DNA.

de Vera IMS, Zheng J, Novick S, Shang J, Hughes TS, Brust R, Munoz-Tello P, Gardner WJ Jr, Marciano DP, Kong X, Griffin PR, Kojetin DJ.

Structure. 2017 Oct 3;25(10):1506-1518.e4. doi: 10.1016/j.str.2017.07.019. Epub 2017 Sep 7.

PMID:
28890360
17.

Identification of Phosphorylation Codes for Arrestin Recruitment by G Protein-Coupled Receptors.

Zhou XE, He Y, de Waal PW, Gao X, Kang Y, Van Eps N, Yin Y, Pal K, Goswami D, White TA, Barty A, Latorraca NR, Chapman HN, Hubbell WL, Dror RO, Stevens RC, Cherezov V, Gurevich VV, Griffin PR, Ernst OP, Melcher K, Xu HE.

Cell. 2017 Jul 27;170(3):457-469.e13. doi: 10.1016/j.cell.2017.07.002.

PMID:
28753425
18.

Deconvoluting AMP-activated protein kinase (AMPK) adenine nucleotide binding and sensing.

Gu X, Yan Y, Novick SJ, Kovach A, Goswami D, Ke J, Tan MHE, Wang L, Li X, de Waal PW, Webb MR, Griffin PR, Xu HE, Melcher K.

J Biol Chem. 2017 Jul 28;292(30):12653-12666. doi: 10.1074/jbc.M117.793018. Epub 2017 Jun 14.

19.

Structural Basis of TPR-Mediated Oligomerization and Activation of Oncogenic Fusion Kinases.

Pal K, Bandyopadhyay A, Zhou XE, Xu Q, Marciano DP, Brunzelle JS, Yerrum S, Griffin PR, Vande Woude G, Melcher K, Xu HE.

Structure. 2017 Jun 6;25(6):867-877.e3. doi: 10.1016/j.str.2017.04.015. Epub 2017 May 18.

20.

Structure of the full-length glucagon class B G-protein-coupled receptor.

Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B.

Nature. 2017 Jun 8;546(7657):259-264. doi: 10.1038/nature22363. Epub 2017 May 17.

21.

Corrigendum: Full antagonism of the estrogen receptor without a prototypical ligand side chain.

Srinivasan S, Nwachukwu JC, Bruno NE, Dharmarajan V, Goswami D, Kastrati I, Novick S, Nowak J, Cavett V, Zhou HB, Boonmuen N, Zhao Y, Min J, Frasor J, Katzenellenbogen BS, Griffin PR, Katzenellenbogen JA, Nettles KW.

Nat Chem Biol. 2017 May 17;13(6):691. doi: 10.1038/nchembio0617-691c. No abstract available.

PMID:
28514424
22.

Erratum: Full antagonism of the estrogen receptor without a prototypical ligand side chain.

Srinivasan S, Nwachukwu JC, Bruno NE, Dharmarajan V, Goswami D, Kastrati I, Novick S, Nowak J, Cavett V, Zhou HB, Boonmuen N, Zhao Y, Min J, Frasor J, Katzenellenbogen BS, Griffin PR, Katzenellenbogen JA, Nettles KW.

Nat Chem Biol. 2017 May 17;13(6):691. doi: 10.1038/nchembio0617-691b. No abstract available.

PMID:
28514419
23.

Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand.

Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F.

Nat Commun. 2017 May 17;8:15383. doi: 10.1038/ncomms15383.

24.

Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics.

Frkic RL, He Y, Rodriguez BB, Chang MR, Kuruvilla D, Ciesla A, Abell AD, Kamenecka TM, Griffin PR, Bruning JB.

J Med Chem. 2017 Jun 8;60(11):4584-4593. doi: 10.1021/acs.jmedchem.6b01727. Epub 2017 May 22.

25.

Structure and Dynamics of the Liver Receptor Homolog 1-PGC1α Complex.

Mays SG, Okafor CD, Tuntland ML, Whitby RJ, Dharmarajan V, Stec J, Griffin PR, Ortlund EA.

Mol Pharmacol. 2017 Jul;92(1):1-11. doi: 10.1124/mol.117.108514. Epub 2017 Mar 31.

PMID:
28363985
26.

GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity.

Sturchler E, Li X, de Lourdes Ladino M, Kaczanowska K, Cameron M, Griffin PR, Finn MG, Markou A, McDonald P.

Pharmacol Res Perspect. 2017 Mar 24;5(2):e00288. doi: 10.1002/prp2.288. eCollection 2017 Apr.

27.

Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes.

Sharabi K, Lin H, Tavares CDJ, Dominy JE, Camporez JP, Perry RJ, Schilling R, Rines AK, Lee J, Hickey M, Bennion M, Palmer M, Nag PP, Bittker JA, Perez J, Jedrychowski MP, Ozcan U, Gygi SP, Kamenecka TM, Shulman GI, Schreiber SL, Griffin PR, Puigserver P.

Cell. 2017 Mar 23;169(1):148-160.e15. doi: 10.1016/j.cell.2017.03.001.

28.

Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor.

Jin Z, Lin H, Srinivasan S, Nwachukwu JC, Bruno N, Griffin PR, Nettles KW, Kamenecka TM.

Bioorg Med Chem Lett. 2017 Jan 15;27(2):347-353. doi: 10.1016/j.bmcl.2016.11.007. Epub 2016 Nov 15.

PMID:
27919657
29.

N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists.

Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Kuruvilla DS, Novick SJ, Lin L, Cameron MD, Griffin PR, Kamenecka TM.

ChemMedChem. 2016 Dec 6;11(23):2607-2620. doi: 10.1002/cmdc.201600491. Epub 2016 Nov 23.

30.

Full antagonism of the estrogen receptor without a prototypical ligand side chain.

Srinivasan S, Nwachukwu JC, Bruno NE, Dharmarajan V, Goswami D, Kastrati I, Novick S, Nowak J, Cavett V, Zhou HB, Boonmuen N, Zhao Y, Min J, Frasor J, Katzenellenbogen BS, Griffin PR, Katzenellenbogen JA, Nettles KW.

Nat Chem Biol. 2017 Jan;13(1):111-118. doi: 10.1038/nchembio.2236. Epub 2016 Nov 21. Erratum in: Nat Chem Biol. 2017 May 17;13(6):691. Nat Chem Biol. 2017 May 17;13(6):691.

31.

A Residue-Resolved Bayesian Approach to Quantitative Interpretation of Hydrogen-Deuterium Exchange from Mass Spectrometry: Application to Characterizing Protein-Ligand Interactions.

Saltzberg DJ, Broughton HB, Pellarin R, Chalmers MJ, Espada A, Dodge JA, Pascal BD, Griffin PR, Humblet C, Sali A.

J Phys Chem B. 2017 Apr 20;121(15):3493-3501. doi: 10.1021/acs.jpcb.6b09358. Epub 2016 Dec 1.

32.

Proteolysis by Granzyme B Enhances Presentation of Autoantigenic Peptidylarginine Deiminase 4 Epitopes in Rheumatoid Arthritis.

Darrah E, Kim A, Zhang X, Boronina T, Cole RN, Fava A, Giles JT, Bingham III CO, Chalmers MJ, Griffin PR, Sadegh-Nasseri S, Rosen A.

J Proteome Res. 2017 Jan 6;16(1):355-365. doi: 10.1021/acs.jproteome.6b00617. Epub 2016 Oct 20.

33.

Crystal Structures of the Nuclear Receptor, Liver Receptor Homolog 1, Bound to Synthetic Agonists.

Mays SG, Okafor CD, Whitby RJ, Goswami D, Stec J, Flynn AR, Dugan MC, Jui NT, Griffin PR, Ortlund EA.

J Biol Chem. 2016 Dec 2;291(49):25281-25291. Epub 2016 Sep 30.

34.

PPARG Post-translational Modifications Regulate Bone Formation and Bone Resorption.

Stechschulte LA, Czernik PJ, Rotter ZC, Tausif FN, Corzo CA, Marciano DP, Asteian A, Zheng J, Bruning JB, Kamenecka TM, Rosen CJ, Griffin PR, Lecka-Czernik B.

EBioMedicine. 2016 Aug;10:174-84. doi: 10.1016/j.ebiom.2016.06.040. Epub 2016 Jun 29.

35.

The Secreted Enzyme PM20D1 Regulates Lipidated Amino Acid Uncouplers of Mitochondria.

Long JZ, Svensson KJ, Bateman LA, Lin H, Kamenecka T, Lokurkar IA, Lou J, Rao RR, Chang MR, Jedrychowski MP, Paulo JA, Gygi SP, Griffin PR, Nomura DK, Spiegelman BM.

Cell. 2016 Jul 14;166(2):424-435. doi: 10.1016/j.cell.2016.05.071. Epub 2016 Jun 30.

36.

Neddylation requires glycyl-tRNA synthetase to protect activated E2.

Mo Z, Zhang Q, Liu Z, Lauer J, Shi Y, Sun L, Griffin PR, Yang XL.

Nat Struct Mol Biol. 2016 Aug;23(8):730-7. doi: 10.1038/nsmb.3250. Epub 2016 Jun 27.

37.

Two-Site Evaluation of the Repeatability and Precision of an Automated Dual-Column Hydrogen/Deuterium Exchange Mass Spectrometry Platform.

Cummins DJ, Espada A, Novick SJ, Molina-Martin M, Stites RE, Espinosa JF, Broughton H, Goswami D, Pascal BD, Dodge JA, Chalmers MJ, Griffin PR.

Anal Chem. 2016 Jun 21;88(12):6607-14. doi: 10.1021/acs.analchem.6b01650. Epub 2016 Jun 13.

PMID:
27224086
38.

The Methionine Transamination Pathway Controls Hepatic Glucose Metabolism through Regulation of the GCN5 Acetyltransferase and the PGC-1α Transcriptional Coactivator.

Tavares CD, Sharabi K, Dominy JE, Lee Y, Isasa M, Orozco JM, Jedrychowski MP, Kamenecka TM, Griffin PR, Gygi SP, Puigserver P.

J Biol Chem. 2016 May 13;291(20):10635-45. doi: 10.1074/jbc.M115.706200. Epub 2016 Mar 28.

39.

The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency.

Feng L, Dharmarajan V, Serrao E, Hoyte A, Larue RC, Slaughter A, Sharma A, Plumb MR, Kessl JJ, Fuchs JR, Bushman FD, Engelman AN, Griffin PR, Kvaratskhelia M.

ACS Chem Biol. 2016 May 20;11(5):1313-21. doi: 10.1021/acschembio.6b00167. Epub 2016 Mar 2.

40.

Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.

Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL.

Elife. 2016 Feb 2;5. pii: e12792. doi: 10.7554/eLife.12792.

41.

Corrigendum: CMT2D neuropathy is linked to the neomorphic binding activity of glycyl-tRNA synthetase.

He W, Bai G, Zhou H, Wei N, White NM, Lauer J, Liu H, Shi Y, Dan Dumitru C, Lettieri K, Shubayev V, Jordanova A, Guergueltcheva V, Griffin PR, Burgess RW, Pfaff SL, Yang XL.

Nature. 2016 Apr 21;532(7599):402. doi: 10.1038/nature16499. Epub 2016 Jan 20. No abstract available.

PMID:
26789244
42.

Synthetic RORγt Agonists Enhance Protective Immunity.

Chang MR, Dharmarajan V, Doebelin C, Garcia-Ordonez RD, Novick SJ, Kuruvilla DS, Kamenecka TM, Griffin PR.

ACS Chem Biol. 2016 Apr 15;11(4):1012-8. doi: 10.1021/acschembio.5b00899. Epub 2016 Jan 25.

43.

Identification and function of conformational dynamics in the multidomain GTPase dynamin.

Srinivasan S, Dharmarajan V, Reed DK, Griffin PR, Schmid SL.

EMBO J. 2016 Feb 15;35(4):443-57. doi: 10.15252/embj.201593477. Epub 2016 Jan 18.

44.

PPARγ Antagonist Gleevec Improves Insulin Sensitivity and Promotes the Browning of White Adipose Tissue.

Choi SS, Kim ES, Jung JE, Marciano DP, Jo A, Koo JY, Choi SY, Yang YR, Jang HJ, Kim EK, Park J, Kwon HM, Lee IH, Park SB, Myung KJ, Suh PG, Griffin PR, Choi JH.

Diabetes. 2016 Apr;65(4):829-39. doi: 10.2337/db15-1382. Epub 2016 Jan 6.

45.

Autocrine selection of a GLP-1R G-protein biased agonist with potent antidiabetic effects.

Zhang H, Sturchler E, Zhu J, Nieto A, Cistrone PA, Xie J, He L, Yea K, Jones T, Turn R, Di Stefano PS, Griffin PR, Dawson PE, McDonald PH, Lerner RA.

Nat Commun. 2015 Dec 1;6:8918. doi: 10.1038/ncomms9918.

46.

SR2067 Reveals a Unique Kinetic and Structural Signature for PPARγ Partial Agonism.

van Marrewijk LM, Polyak SW, Hijnen M, Kuruvilla D, Chang MR, Shin Y, Kamenecka TM, Griffin PR, Bruning JB.

ACS Chem Biol. 2016 Jan 15;11(1):273-83. doi: 10.1021/acschembio.5b00580. Epub 2015 Dec 3.

47.

CMT2D neuropathy is linked to the neomorphic binding activity of glycyl-tRNA synthetase.

He W, Bai G, Zhou H, Wei N, White NM, Lauer J, Liu H, Shi Y, Dumitru CD, Lettieri K, Shubayev V, Jordanova A, Guergueltcheva V, Griffin PR, Burgess RW, Pfaff SL, Yang XL.

Nature. 2015 Oct 29;526(7575):710-4. doi: 10.1038/nature15510. Epub 2015 Oct 21. Erratum in: Nature. 2016 Apr 21;532(7599):402.

48.

Destabilization of strigolactone receptor DWARF14 by binding of ligand and E3-ligase signaling effector DWARF3.

Zhao LH, Zhou XE, Yi W, Wu Z, Liu Y, Kang Y, Hou L, de Waal PW, Li S, Jiang Y, Scaffidi A, Flematti GR, Smith SM, Lam VQ, Griffin PR, Wang Y, Li J, Melcher K, Xu HE.

Cell Res. 2015 Nov;25(11):1219-36. doi: 10.1038/cr.2015.122. Epub 2015 Oct 16.

49.

Identification of Bexarotene as a PPARγ Antagonist with HDX.

Marciano DP, Kuruvilla DS, Pascal BD, Griffin PR.

PPAR Res. 2015;2015:254560. doi: 10.1155/2015/254560. Epub 2015 Sep 15.

50.

SERBP1 Is a Component of the Liver Receptor Homologue-1 Transcriptional Complex.

Mari Y, West GM, Scharager-Tapia C, Pascal BD, Garcia-Ordonez RD, Griffin PR.

J Proteome Res. 2015 Nov 6;14(11):4571-80. doi: 10.1021/acs.jproteome.5b00379. Epub 2015 Oct 7.

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