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Items: 8

1.

Small molecule G protein-coupled receptor kinase inhibitors attenuate GRK2-mediated desensitization of vasoconstrictor-induced arterial contractions.

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

Mol Pharmacol. 2018 Jul 6. pii: mol.118.112524. doi: 10.1124/mol.118.112524. [Epub ahead of print]

2.

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.

PMID:
29627263
3.

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.

PMID:
29070696
4.

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.

5.

Occludin S471 Phosphorylation Contributes to Epithelial Monolayer Maturation.

Bolinger MT, Ramshekar A, Waldschmidt HV, Larsen SD, Bewley MC, Flanagan JM, Antonetti DA.

Mol Cell Biol. 2016 Jul 14;36(15):2051-66. doi: 10.1128/MCB.00053-16. Print 2016 Aug 1.

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.

7.

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.

8.

Translation of structure-activity relationships from cyclic mixed efficacy opioid peptides to linear analogues.

Anand JP, Porter-Barrus VR, Waldschmidt HV, Yeomans L, Pogozheva ID, Traynor JR, Mosberg HI.

Biopolymers. 2014 Jan;102(1):107-14. doi: 10.1002/bip.22437. Erratum in: Biopolymers. 2014 Sep;102(5):426.

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