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Structural analysis of lecithin:cholesterol acyltransferase bound to high density lipoprotein particles.

Manthei KA, Patra D, Wilson CJ, Fawaz MV, Piersimoni L, Shenkar JC, Yuan W, Andrews PC, Engen JR, Schwendeman A, Ohi MD, Tesmer JJG.

Commun Biol. 2020 Jan 15;3(1):28. doi: 10.1038/s42003-019-0749-z.


Discovery of small molecules that target the P-Rex1 PIP3-binding site and inhibit P-Rex1-dependent functions in neutrophils.

Cash JN, Chandan NR, Hsu AY, Sharma PV, Deng Q, Smrcka AV, Tesmer JJG.

Mol Pharmacol. 2020 Jan 3. pii: mol.119.117556. doi: 10.1124/mol.119.117556. [Epub ahead of print]


Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.

Rowlands RA, Cato MC, Waldschmidt HV, Bouley RA, Chen Q, Avramova L, Larsen SD, Tesmer JJG, White AD.

ACS Med Chem Lett. 2019 Nov 12;10(12):1628-1634. doi: 10.1021/acsmedchemlett.9b00365. eCollection 2019 Dec 12.


Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli.

Beyett TS, Chen Q, Labudde EJ, Krampen J, Sharma PV, Tesmer JJG.

Protein Expr Purif. 2019 Nov 29;168:105547. doi: 10.1016/j.pep.2019.105547. [Epub ahead of print]


Phospholipid component defines pharmacokinetic and pharmacodynamic properties of synthetic high-density lipoproteins.

Fawaz MV, Kim SY, Li D, Ming R, Xia Z, Olsen K, Pogozheva ID, Tesmer JJG, Schwendeman A.

J Pharmacol Exp Ther. 2019 Nov 27. pii: jpet.119.257568. doi: 10.1124/jpet.119.257568. [Epub ahead of print]


Cryo-electron microscopy structure and analysis of the P-Rex1-Gβγ signaling scaffold.

Cash JN, Urata S, Li S, Ravala SK, Avramova LV, Shost MD, Gutkind JS, Tesmer JJG, Cianfrocco MA.

Sci Adv. 2019 Oct 16;5(10):eaax8855. doi: 10.1126/sciadv.aax8855. eCollection 2019 Oct.


Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe.

Beyett TS, Fraley AE, Labudde E, Patra D, Coleman RC, Eguchi A, Glukhova A, Chen Q, Williams RM, Koch WJ, Sherman DH, Tesmer JJG.

Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15895-15900. doi: 10.1073/pnas.1818547116. Epub 2019 Jul 23.


Correction to "Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine".

Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJG, Larsen SD.

J Med Chem. 2019 Jun 27;62(12):5920. doi: 10.1021/acs.jmedchem.9b00844. Epub 2019 Jun 12. No abstract available.


Structural Basis of Lysosomal Phospholipase A2 Inhibition by Zn2.

Bouley RA, Hinkovska-Galcheva V, Shayman JA, Tesmer JJG.

Biochemistry. 2019 Apr 2;58(13):1709-1717. doi: 10.1021/acs.biochem.8b01124. Epub 2019 Mar 13.


Synthesis of deuterium-labelled amlexanox and its metabolic stability against mouse, rat, and human microsomes.

Gan X, Wilson MW, Beyett TS, Wen B, Sun D, Larsen SD, Tesmer JJG, Saltiel AR, Showalter HD.

J Labelled Comp Radiopharm. 2019 May 15;62(5):202-208. doi: 10.1002/jlcr.3716. Epub 2019 Apr 3.


Structure of the C-terminal guanine nucleotide exchange factor module of Trio in an autoinhibited conformation reveals its oncogenic potential.

Bandekar SJ, Arang N, Tully ES, Tang BA, Barton BL, Li S, Gutkind JS, Tesmer JJG.

Sci Signal. 2019 Feb 19;12(569). pii: eaav2449. doi: 10.1126/scisignal.aav2449.


Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol.

Manthei KA, Yang SM, Baljinnyam B, Chang L, Glukhova A, Yuan W, Freeman LA, Maloney DJ, Schwendeman A, Remaley AT, Jadhav A, Tesmer JJ.

Elife. 2018 Nov 27;7. pii: e41604. doi: 10.7554/eLife.41604.


Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity.

Beyett TS, Gan X, Reilly SM, Gomez AV, Chang L, Tesmer JJG, Saltiel AR, Showalter HD.

Bioorg Med Chem. 2018 Nov 1;26(20):5443-5461. doi: 10.1016/j.bmc.2018.09.020. Epub 2018 Sep 20.


Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKKε and Reveal Mechanisms for Selective Inhibition.

Beyett TS, Gan X, Reilly SM, Chang L, Gomez AV, Saltiel AR, Showalter HD, Tesmer JJG.

Mol Pharmacol. 2018 Oct;94(4):1210-1219. doi: 10.1124/mol.118.112185. Epub 2018 Aug 6.


Lysosomal phospholipase A2.

Shayman JA, Tesmer JJG.

Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Jun;1864(6):932-940. doi: 10.1016/j.bbalip.2018.07.012. Epub 2018 Aug 2. Review.


Small-Molecule G Protein-Coupled Receptor Kinase Inhibitors Attenuate G Protein-Coupled Receptor Kinase 2-Mediated Desensitization of Vasoconstrictor-Induced Arterial Contractions.

Rainbow RD, Brennan S, Jackson R, Beech AJ, Bengreed A, Waldschmidt HV, Tesmer JJG, Challiss RAJ, Willets JM.

Mol Pharmacol. 2018 Sep;94(3):1079-1091. doi: 10.1124/mol.118.112524. Epub 2018 Jul 6.


Determinants of pH profile and acyl chain selectivity in lysosomal phospholipase A2.

Hinkovska-Galcheva V, Kelly R, Manthei KA, Bouley R, Yuan W, Schwendeman A, Tesmer JJG, Shayman JA.

J Lipid Res. 2018 Jul;59(7):1205-1218. doi: 10.1194/jlr.M084012. Epub 2018 May 3.


Tracking the Cartoon mouse phenotype: Hemopexin domain-dependent regulation of MT1-MMP pericellular collagenolytic activity.

Sakr M, Li XY, Sabeh F, Feinberg TY, Tesmer JJG, Tang Y, Weiss SJ.

J Biol Chem. 2018 May 25;293(21):8113-8127. doi: 10.1074/jbc.RA117.001503. Epub 2018 Apr 11.


Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.

Waldschmidt HV, Bouley R, Kirchhoff PD, Lee P, Tesmer JJG, Larsen SD.

Bioorg Med Chem Lett. 2018 May 15;28(9):1507-1515. doi: 10.1016/j.bmcl.2018.03.082. Epub 2018 Mar 30.


Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.

Bouley R, Waldschmidt HV, Cato MC, Cannavo A, Song J, Cheung JY, Yao XQ, Koch WJ, Larsen SD, Tesmer JJG.

Mol Pharmacol. 2017 Dec;92(6):707-717. doi: 10.1124/mol.117.110130. Epub 2017 Oct 25.


A retractable lid in lecithin:cholesterol acyltransferase provides a structural mechanism for activation by apolipoprotein A-I.

Manthei KA, Ahn J, Glukhova A, Yuan W, Larkin C, Manett TD, Chang L, Shayman JA, Axley MJ, Schwendeman A, Tesmer JJG.

J Biol Chem. 2017 Dec 8;292(49):20313-20327. doi: 10.1074/jbc.M117.802736. Epub 2017 Oct 13.


Quantitative Multiple-Reaction Monitoring Proteomic Analysis of Gβ and Gγ Subunits in C57Bl6/J Brain Synaptosomes.

Yim YY, McDonald WH, Hyde K, Cruz-Rodríguez O, Tesmer JJG, Hamm HE.

Biochemistry. 2017 Oct 10;56(40):5405-5416. doi: 10.1021/acs.biochem.7b00433. Epub 2017 Sep 21.


Navigating the conformational landscape of G protein-coupled receptor kinases during allosteric activation.

Yao XQ, Cato MC, Labudde E, Beyett TS, Tesmer JJG, Grant BJ.

J Biol Chem. 2017 Sep 29;292(39):16032-16043. doi: 10.1074/jbc.M117.807461. Epub 2017 Aug 14.


Lecithin:Cholesterol Acyltransferase Activation by Sulfhydryl-Reactive Small Molecules: Role of Cysteine-31.

Freeman LA, Demosky SJ Jr, Konaklieva M, Kuskovsky R, Aponte A, Ossoli AF, Gordon SM, Koby RF, Manthei KA, Shen M, Vaisman BL, Shamburek RD, Jadhav A, Calabresi L, Gucek M, Tesmer JJG, Levine RL, Remaley AT.

J Pharmacol Exp Ther. 2017 Aug;362(2):306-318. doi: 10.1124/jpet.117.240457. Epub 2017 Jun 2.


Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.

Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJ, Larsen SD.

J Med Chem. 2017 Apr 13;60(7):3052-3069. doi: 10.1021/acs.jmedchem.7b00112. Epub 2017 Mar 29. Erratum in: J Med Chem. 2019 Jun 27;62(12):5920.


A Receptor on Acid.

Chen Q, Tesmer JJG.

Cell. 2017 Jan 26;168(3):339-341. doi: 10.1016/j.cell.2017.01.012.


Preferential hydrolysis of truncated oxidized glycerophospholipids by lysosomal phospholipase A2.

Abe A, Hiraoka M, Ohguro H, Tesmer JJ, Shayman JA.

J Lipid Res. 2017 Feb;58(2):339-349. doi: 10.1194/jlr.M070730. Epub 2016 Dec 19.


Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3.

Cash JN, Davis EM, Tesmer JJG.

Structure. 2016 May 3;24(5):730-740. doi: 10.1016/j.str.2016.02.022. Epub 2016 Apr 14.


Using iterative fragment assembly and progressive sequence truncation to facilitate phasing and crystal structure determination of distantly related proteins.

Wang Y, Virtanen J, Xue Z, Tesmer JJ, Zhang Y.

Acta Crystallogr D Struct Biol. 2016 May;72(Pt 5):616-28. doi: 10.1107/S2059798316003016. Epub 2016 Apr 26.


Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes.

Tesmer JJ.

Nat Rev Mol Cell Biol. 2016 Jul;17(7):439-50. doi: 10.1038/nrm.2016.36. Epub 2016 Apr 20. Review.


Effect of Lipid Composition on the Membrane Orientation of the G Protein-Coupled Receptor Kinase 2-Gβ1γ2 Complex.

Yang P, Homan KT, Li Y, Cruz-Rodríguez O, Tesmer JJ, Chen Z.

Biochemistry. 2016 May 24;55(20):2841-8. doi: 10.1021/acs.biochem.6b00354. Epub 2016 May 6.


Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.

Waldschmidt HV, Homan KT, Cruz-Rodríguez O, Cato MC, Waninger-Saroni J, Larimore KM, Cannavo A, Song J, Cheung JY, Kirchhoff PD, Koch WJ, Tesmer JJ, Larsen SD.

J Med Chem. 2016 Apr 28;59(8):3793-807. doi: 10.1021/acs.jmedchem.5b02000. Epub 2016 Apr 13.


Structure of the Regulator of G Protein Signaling 8 (RGS8)-Gαq Complex: MOLECULAR BASIS FOR Gα SELECTIVITY.

Taylor VG, Bommarito PA, Tesmer JJ.

J Biol Chem. 2016 Mar 4;291(10):5138-45. doi: 10.1074/jbc.M115.712075. Epub 2016 Jan 11.


Crystallographic Pursuit of a Protein-RNA Aptamer Complex.

Tesmer JJ.

Methods Mol Biol. 2016;1380:151-60. doi: 10.1007/978-1-4939-3197-2_12.


G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro.

Inagaki S, Ghirlando R, Vishnivetskiy SA, Homan KT, White JF, Tesmer JJ, Gurevich VV, Grisshammer R.

Biochemistry. 2015 Jul 21;54(28):4320-9. doi: 10.1021/acs.biochem.5b00285. Epub 2015 Jul 8.


Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.

Homan KT, Waldschmidt HV, Glukhova A, Cannavo A, Song J, Cheung JY, Koch WJ, Larsen SD, Tesmer JJ.

J Biol Chem. 2015 Aug 21;290(34):20649-59. doi: 10.1074/jbc.M115.647370. Epub 2015 Jun 1.


C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor.

Azevedo AW, Doan T, Moaven H, Sokal I, Baameur F, Vishnivetskiy SA, Homan KT, Tesmer JJ, Gurevich VV, Chen J, Rieke F.

Elife. 2015 Apr 24;4. doi: 10.7554/eLife.05981.


G Protein-coupled Receptor Kinases of the GRK4 Protein Subfamily Phosphorylate Inactive G Protein-coupled Receptors (GPCRs).

Li L, Homan KT, Vishnivetskiy SA, Manglik A, Tesmer JJ, Gurevich VV, Gurevich EV.

J Biol Chem. 2015 Apr 24;290(17):10775-90. doi: 10.1074/jbc.M115.644773. Epub 2015 Mar 13.


Paroxetine-mediated GRK2 inhibition reverses cardiac dysfunction and remodeling after myocardial infarction.

Schumacher SM, Gao E, Zhu W, Chen X, Chuprun JK, Feldman AM, Tesmer JJ, Koch WJ.

Sci Transl Med. 2015 Mar 4;7(277):277ra31. doi: 10.1126/scitranslmed.aaa0154.


Structure and function of lysosomal phospholipase A2 and lecithin:cholesterol acyltransferase.

Glukhova A, Hinkovska-Galcheva V, Kelly R, Abe A, Shayman JA, Tesmer JJ.

Nat Commun. 2015 Mar 2;6:6250. doi: 10.1038/ncomms7250.


Molecular mechanisms of phospholipase C β3 autoinhibition.

Lyon AM, Begley JA, Manett TD, Tesmer JJG.

Structure. 2014 Dec 2;22(12):1844-1854. doi: 10.1016/j.str.2014.10.008.


Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor.

Homan KT, Wu E, Cannavo A, Koch WJ, Tesmer JJ.

Molecules. 2014 Oct 22;19(10):16937-49. doi: 10.3390/molecules191016937.


Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.

Homan KT, Larimore KM, Elkins JM, Szklarz M, Knapp S, Tesmer JJ.

ACS Chem Biol. 2015 Jan 16;10(1):310-9. doi: 10.1021/cb5006323. Epub 2014 Oct 3.


Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays.

Beautrait A, Michalski KR, Lopez TS, Mannix KM, McDonald DJ, Cutter AR, Medina CB, Hebert AM, Francis CJ, Bouvier M, Tesmer JJ, Sterne-Marr R.

J Biol Chem. 2014 Sep 5;289(36):25262-75. doi: 10.1074/jbc.M114.593178. Epub 2014 Jul 21.


Molecular basis for small molecule inhibition of G protein-coupled receptor kinases.

Homan KT, Tesmer JJ.

ACS Chem Biol. 2015 Jan 16;10(1):246-56. doi: 10.1021/cb5003976. Epub 2014 Jul 14. Review.


Conserved modular domains team up to latch-open active protein kinase Cα.

Swanson CJ, Ritt M, Wang W, Lang MJ, Narayan A, Tesmer JJ, Westfall M, Sivaramakrishnan S.

J Biol Chem. 2014 Jun 20;289(25):17812-29. doi: 10.1074/jbc.M113.534750. Epub 2014 Apr 30.


Structural insights into G protein-coupled receptor kinase function.

Homan KT, Tesmer JJ.

Curr Opin Cell Biol. 2014 Apr;27:25-31. doi: 10.1016/ Epub 2013 Nov 26. Review.


Unveiling the membrane-binding properties of N-terminal and C-terminal regions of G protein-coupled receptor kinase 5 by combined optical spectroscopies.

Ding B, Glukhova A, Sobczyk-Kojiro K, Mosberg HI, Tesmer JJ, Chen Z.

Langmuir. 2014 Jan 28;30(3):823-31. doi: 10.1021/la404055a. Epub 2014 Jan 16.


Strike a pose: Gαq complexes at the membrane.

Lyon AM, Taylor VG, Tesmer JJ.

Trends Pharmacol Sci. 2014 Jan;35(1):23-30. doi: 10.1016/ Epub 2013 Nov 26. Review.


Membrane orientation and binding determinants of G protein-coupled receptor kinase 5 as assessed by combined vibrational spectroscopic studies.

Yang P, Glukhova A, Tesmer JJ, Chen Z.

PLoS One. 2013 Nov 22;8(11):e82072. doi: 10.1371/journal.pone.0082072. eCollection 2013.

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