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Items: 1 to 20 of 89

1.

Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPARγ; a Model for Ligand-Dependent Antagonism.

Zheng J, Corzo C, Chang MR, Shang J, Lam VQ, Brust R, Blayo AL, Bruning JB, Kamenecka TM, Kojetin DJ, Griffin PR.

Structure. 2018 Aug 8. pii: S0969-2126(18)30253-3. doi: 10.1016/j.str.2018.07.007. [Epub ahead of print]

PMID:
30146169
2.

Identification of potent RORβ modulators: Scaffold variation.

Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Novick S, Ciesla A, Campbell S, Solt LA, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2018 Aug 16. pii: S0960-894X(18)30676-0. doi: 10.1016/j.bmcl.2018.08.017. [Epub ahead of print]

PMID:
30143422
3.

PPARγ in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix.

Frkic RL, Marshall AC, Blayo AL, Pukala TL, Kamenecka TM, Griffin PR, Bruning JB.

iScience. 2018 Feb 27;5:69-79. doi: 10.1016/j.isci.2018.06.012. Epub 2018 Jul 2.

4.

Ablation of PM20D1 reveals N-acyl amino acid control of metabolism and nociception.

Long JZ, Roche AM, Berdan CA, Louie SM, Roberts AJ, Svensson KJ, Dou FY, Bateman LA, Mina AI, Deng Z, Jedrychowski MP, Lin H, Kamenecka TM, Asara JM, Griffin PR, Banks AS, Nomura DK, Spiegelman BM.

Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6937-E6945. doi: 10.1073/pnas.1803389115. Epub 2018 Jul 2.

5.

Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation.

Zhao J, Zhang L, Mu X, Doebelin C, Nguyen W, Wallace C, Reay DP, McGowan SJ, Corbo L, Clemens PR, Wilson GM, Watkins SC, Solt LA, Cameron MD, Huard J, Niedernhofer LJ, Kamenecka TM, Robbins PD.

PLoS Biol. 2018 Jun 11;16(6):e2004663. doi: 10.1371/journal.pbio.2004663. eCollection 2018 Jun.

6.

Site-Selective γ-C(sp3 )-H and γ-C(sp2 )-H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group.

Lin H, Wang C, Bannister TD, Kamenecka TM.

Chemistry. 2018 Jul 5;24(38):9535-9541. doi: 10.1002/chem.201802465. Epub 2018 Jun 6.

PMID:
29775502
7.

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.

8.

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
9.

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
10.

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
11.

REV-ERBβ is required to maintain normal wakefulness and the wake-inducing effect of dual REV-ERB agonist SR9009.

Amador A, Kamenecka TM, Solt LA, Burris TP.

Biochem Pharmacol. 2018 Apr;150:1-8. doi: 10.1016/j.bcp.2018.01.009. Epub 2018 Jan 23.

PMID:
29355503
12.

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.

13.

RORα modulates semaphorin 3E transcription and neurovascular interaction in pathological retinal angiogenesis.

Sun Y, Liu CH, Wang Z, Meng SS, Burnim SB, SanGiovanni JP, Kamenecka TM, Solt LA, Chen J.

FASEB J. 2017 Oct;31(10):4492-4502. doi: 10.1096/fj.201700172R. Epub 2017 Jun 23.

PMID:
28646017
14.

Multigram-scale Synthesis of Enantiopure 3,3-Difluoroproline.

Doebelin C, He Y, Kamenecka TM.

Tetrahedron Lett. 2016 Dec 14;57(50):5658-5660. doi: 10.1016/j.tetlet.2016.11.012. Epub 2016 Nov 3.

15.

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.

16.

GLP-1 acts on habenular avoidance circuits to control nicotine intake.

Tuesta LM, Chen Z, Duncan A, Fowler CD, Ishikawa M, Lee BR, Liu XA, Lu Q, Cameron M, Hayes MR, Kamenecka TM, Pletcher M, Kenny PJ.

Nat Neurosci. 2017 May;20(5):708-716. doi: 10.1038/nn.4540. Epub 2017 Apr 3.

17.

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.

18.

Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor.

Brust R, Lin H, Fuhrmann J, Asteian A, Kamenecka TM, Kojetin DJ.

ACS Chem Biol. 2017 Apr 21;12(4):969-978. doi: 10.1021/acschembio.6b01015. Epub 2017 Feb 16.

19.

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
20.

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.

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