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Items: 1 to 50 of 93

1.

Chemical validation and optimization of pharmacoperones targeting vasopressin type 2 receptor mutant.

Janovick JA, Spicer TP, Bannister TD, Smith E, Ganapathy V, Scampavia L.

Biochem J. 2018 Sep 25;475(18):2941-2953. doi: 10.1042/BCJ20180065.

PMID:
30068530
2.

Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias.

Janovick JA, Spicer TP, Bannister TD, Scampavia L, Conn PM.

PLoS One. 2017 Aug 2;12(8):e0181830. doi: 10.1371/journal.pone.0181830. eCollection 2017.

3.

Drug Library Screening for the Identification of Ionophores That Correct the Mistrafficking Disorder Associated with Oxalosis Kidney Disease.

Hou S, Madoux F, Scampavia L, Janovick JA, Conn PM, Spicer TP.

SLAS Discov. 2017 Aug;22(7):887-896. doi: 10.1177/2472555217689992. Epub 2017 Jan 31.

PMID:
28346094
4.

Receptor antagonism/agonism can be uncoupled from pharmacoperone activity.

Janovick JA, Spicer TP, Smith E, Bannister TD, Kenakin T, Scampavia L, Conn PM.

Mol Cell Endocrinol. 2016 Oct 15;434:176-85. doi: 10.1016/j.mce.2016.07.003. Epub 2016 Jul 4.

5.

Identification of Potential Pharmacoperones Capable of Rescuing the Functionality of Misfolded Vasopressin 2 Receptor Involved in Nephrogenic Diabetes Insipidus.

Smith E, Janovick JA, Bannister TD, Shumate J, Scampavia L, Conn PM, Spicer TP.

J Biomol Screen. 2016 Sep;21(8):824-31. doi: 10.1177/1087057116653925. Epub 2016 Jun 8.

6.

Assay strategies for identification of therapeutic leads that target protein trafficking.

Conn PM, Spicer TP, Scampavia L, Janovick JA.

Trends Pharmacol Sci. 2015 Aug;36(8):498-505. doi: 10.1016/j.tips.2015.05.004. Epub 2015 Jun 8. Review.

7.

Development of a phenotypic high-content assay to identify pharmacoperone drugs for the treatment of primary hyperoxaluria type 1 by high-throughput screening.

Madoux F, Janovick JA, Smithson D, Fargue S, Danpure CJ, Scampavia L, Chen YT, Spicer TP, Conn PM.

Assay Drug Dev Technol. 2015 Jan-Feb;13(1):16-24. doi: 10.1089/adt.2014.627.

PMID:
25710543
8.

A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor.

Conn PM, Smith E, Spicer T, Chase P, Scampavia L, Janovick JA.

Assay Drug Dev Technol. 2014 May;12(4):238-46. doi: 10.1089/adt.2014.576.

9.

Quality control autophagy degrades soluble ERAD-resistant conformers of the misfolded membrane protein GnRHR.

Houck SA, Ren HY, Madden VJ, Bonner JN, Conlin MP, Janovick JA, Conn PM, Cyr DM.

Mol Cell. 2014 Apr 10;54(1):166-179. doi: 10.1016/j.molcel.2014.02.025. Epub 2014 Mar 27.

10.

Transitioning pharmacoperones to therapeutic use: in vivo proof-of-principle and design of high throughput screens.

Conn PM, Smithson DC, Hodder PS, Stewart MD, Behringer RR, Smith E, Ulloa-Aguirre A, Janovick JA.

Pharmacol Res. 2014 May;83:38-51. doi: 10.1016/j.phrs.2013.12.004. Epub 2013 Dec 25. Review.

11.

Restoration of testis function in hypogonadotropic hypogonadal mice harboring a misfolded GnRHR mutant by pharmacoperone drug therapy.

Janovick JA, Stewart MD, Jacob D, Martin LD, Deng JM, Stewart CA, Wang Y, Cornea A, Chavali L, Lopez S, Mitalipov S, Kang E, Lee HS, Manna PR, Stocco DM, Behringer RR, Conn PM.

Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):21030-5. doi: 10.1073/pnas.1315194110. Epub 2013 Dec 9.

12.

"Pharmacoperone": what's in a word?

Conn PM, Ulloa-Aguirre A, Janovick JA.

Pharmacol Res. 2014 May;83:1-2. doi: 10.1016/j.phrs.2013.11.005. Epub 2013 Nov 20. Review. No abstract available.

PMID:
24269962
13.

Species sequence differences determine the interaction of GnRH receptor with the cellular quality control system.

Cabrera-Wrooman A, Janovick JA, Conn PM.

Mol Cell Endocrinol. 2013 Dec 5;381(1-2):1-7. doi: 10.1016/j.mce.2013.07.012. Epub 2013 Jul 24.

14.

High-throughput screen for pharmacoperones of the vasopressin type 2 receptor.

Conn PM, Smith E, Hodder P, Janovick JA, Smithson DC.

J Biomol Screen. 2013 Sep;18(8):930-7. doi: 10.1177/1087057113483559. Epub 2013 May 2.

15.

Therapeutic rescue of misfolded/mistrafficked mutants: automation-friendly high-throughput assays for identification of pharmacoperone drugs of GPCRs.

Smithson DC, Janovick JA, Conn PM.

Methods Enzymol. 2013;521:3-16. doi: 10.1016/B978-0-12-391862-8.00001-6.

PMID:
23351731
16.

Pharmacological chaperones correct misfolded GPCRs and rescue function: protein trafficking as a therapeutic target.

Maya-Núñez G, Ulloa-Aguirre A, Janovick JA, Conn PM.

Subcell Biochem. 2012;63:263-89. doi: 10.1007/978-94-007-4765-4_14. Review.

PMID:
23161143
17.

Mice harboring Gnrhr E90K, a mutation that causes protein misfolding and hypogonadotropic hypogonadism in humans, exhibit testis size reduction and ovulation failure.

Stewart MD, Deng JM, Stewart CA, Mullen RD, Wang Y, Lopez S, Serna MK, Huang CC, Janovick JA, Pask AJ, Schwartz RJ, Conn PM, Behringer RR.

Mol Endocrinol. 2012 Nov;26(11):1847-56. doi: 10.1210/me.2012-1072. Epub 2012 Aug 23.

18.

Rescue of misrouted GnRHR mutants reveals its constitutive activity.

Janovick JA, Pogozheva ID, Mosberg HI, Cornea A, Conn PM.

Mol Endocrinol. 2012 Jul;26(7):1179-88. doi: 10.1210/me.2012-1089. Epub 2012 May 17.

19.

Therapeutic rescue of misfolded mutants: validation of primary high throughput screens for identification of pharmacoperone drugs.

Janovick JA, Park BS, Conn PM.

PLoS One. 2011;6(7):e22784. doi: 10.1371/journal.pone.0022784. Epub 2011 Jul 27.

20.

Pharmacoperone identification for therapeutic rescue of misfolded mutant proteins.

Conn PM, Janovick JA.

Front Endocrinol (Lausanne). 2011 Mar 3;2(6). pii: 00006.

21.

Salt bridges overlapping the gonadotropin-releasing hormone receptor agonist binding site reveal a coincidence detector for G protein-coupled receptor activation.

Janovick JA, Pogozheva ID, Mosberg HI, Conn PM.

J Pharmacol Exp Ther. 2011 Aug;338(2):430-42. doi: 10.1124/jpet.111.180869. Epub 2011 Apr 28.

22.

Biochemical mechanism of pathogenesis of human gonadotropin-releasing hormone receptor mutants Thr104Ile and Tyr108Cys associated with familial hypogonadotropic hypogonadism.

Maya-Núñez G, Janovick JA, Aguilar-Rojas A, Jardón-Valadez E, Leaños-Miranda A, Zariñan T, Ulloa-Aguirre A, Conn PM.

Mol Cell Endocrinol. 2011 Apr 30;337(1-2):16-23. doi: 10.1016/j.mce.2011.01.016. Epub 2011 Jan 26.

23.

Use of pharmacoperones to reveal GPCR structural changes associated with constitutive activation and trafficking.

Janovick JA, Conn PM.

Methods Enzymol. 2010;485:277-92. doi: 10.1016/B978-0-12-381296-4.00016-6.

PMID:
21050923
24.

Salt bridge integrates GPCR activation with protein trafficking.

Janovick JA, Conn PM.

Proc Natl Acad Sci U S A. 2010 Mar 2;107(9):4454-8. doi: 10.1073/pnas.0914261107. Epub 2010 Feb 16.

25.

Drug development and the cellular quality control system.

Conn PM, Janovick JA.

Trends Pharmacol Sci. 2009 May;30(5):228-33. doi: 10.1016/j.tips.2009.02.002. Epub 2009 Mar 21. Review.

PMID:
19307028
27.

Molecular mechanism of action of pharmacoperone rescue of misrouted GPCR mutants: the GnRH receptor.

Janovick JA, Patny A, Mosley R, Goulet MT, Altman MD, Rush TS 3rd, Cornea A, Conn PM.

Mol Endocrinol. 2009 Feb;23(2):157-68. doi: 10.1210/me.2008-0384. Epub 2008 Dec 18.

28.

Trafficking and quality control of the gonadotropin releasing hormone receptor in health and disease.

Conn PM, Janovick JA.

Mol Cell Endocrinol. 2009 Feb 27;299(2):137-45. doi: 10.1016/j.mce.2008.10.051. Epub 2008 Nov 18. Review.

29.

Increased plasma membrane expression of human follicle-stimulating hormone receptor by a small molecule thienopyr(im)idine.

Janovick JA, Maya-Núñez G, Ulloa-Aguirre A, Huhtaniemi IT, Dias JA, Verbost P, Conn PM.

Mol Cell Endocrinol. 2009 Jan 27;298(1-2):84-8. doi: 10.1016/j.mce.2008.09.015. Epub 2008 Sep 20.

30.

G protein-coupled receptor trafficking in health and disease: lessons learned to prepare for therapeutic mutant rescue in vivo.

Conn PM, Ulloa-Aguirre A, Ito J, Janovick JA.

Pharmacol Rev. 2007 Sep;59(3):225-50. Review.

PMID:
17878512
31.

Refolding of misfolded mutant GPCR: post-translational pharmacoperone action in vitro.

Janovick JA, Brothers SP, Cornea A, Bush E, Goulet MT, Ashton WT, Sauer DR, Haviv F, Greer J, Conn PM.

Mol Cell Endocrinol. 2007 Jun 30;272(1-2):77-85. Epub 2007 May 3.

32.

Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.

Samant MP, White R, Hong DJ, Croston G, Conn PM, Janovick JA, Rivier J.

J Med Chem. 2007 May 3;50(9):2067-77. Epub 2007 Apr 3.

33.

Specializations of a G-protein-coupled receptor that appear to aid with detection of frequency-modulated signals from its ligand.

Janovick JA, Brothers SP, Knollman PE, Conn PM.

FASEB J. 2007 Feb;21(2):384-92. Epub 2006 Dec 15.

PMID:
17172315
34.

Calnexin regulated gonadotropin-releasing hormone receptor plasma membrane expression.

Brothers SP, Janovick JA, Conn PM.

J Mol Endocrinol. 2006 Dec;37(3):479-88.

PMID:
17170088
35.

G-protein-coupled receptor trafficking: understanding the chemical basis of health and disease.

Ulloa-Aguirre A, Janovick JA, Miranda AL, Conn PM.

ACS Chem Biol. 2006 Nov 21;1(10):631-8. Review.

PMID:
17168568
36.

'Effective inefficiency': cellular control of protein trafficking as a mechanism of post-translational regulation.

Conn PM, Janovick JA, Brothers SP, Knollman PE.

J Endocrinol. 2006 Jul;190(1):13-6.

PMID:
16837606
37.

Identification of new gonadotrophin-releasing hormone partial agonists.

Leaños-Miranda A, Ulloa-Aguirre A, Cervini LA, Janovick JA, Rivier J, Conn PM.

J Endocrinol. 2006 Jun;189(3):509-17.

PMID:
16731782
38.

Protein folding as posttranslational regulation: evolution of a mechanism for controlled plasma membrane expression of a G protein-coupled receptor.

Conn PM, Knollman PE, Brothers SP, Janovick JA.

Mol Endocrinol. 2006 Dec;20(12):3035-41. Epub 2006 Mar 23. Review.

PMID:
16556733
39.

Regulation of G protein-coupled receptor trafficking by inefficient plasma membrane expression: molecular basis of an evolved strategy.

Janovick JA, Knollman PE, Brothers SP, Ayala-Yáñez R, Aziz AS, Conn PM.

J Biol Chem. 2006 Mar 31;281(13):8417-25. Epub 2006 Jan 30.

40.

Parallel regulation of membrane trafficking and dominant-negative effects by misrouted gonadotropin-releasing hormone receptor mutants.

Knollman PE, Janovick JA, Brothers SP, Conn PM.

J Biol Chem. 2005 Jul 1;280(26):24506-14. Epub 2005 May 10.

41.

In vitro coexpression and pharmacological rescue of mutant gonadotropin-releasing hormone receptors causing hypogonadotropic hypogonadism in humans expressing compound heterozygous alleles.

Leaños-Miranda A, Ulloa-Aguirre A, Janovick JA, Conn PM.

J Clin Endocrinol Metab. 2005 May;90(5):3001-8. Epub 2005 Feb 22.

PMID:
15728205
42.

A novel mouse model of hypogonadotrophic hypogonadism: N-ethyl-N-nitrosourea-induced gonadotropin-releasing hormone receptor gene mutation.

Pask AJ, Kanasaki H, Kaiser UB, Conn PM, Janovick JA, Stockton DW, Hess DL, Justice MJ, Behringer RR.

Mol Endocrinol. 2005 Apr;19(4):972-81. Epub 2004 Dec 29.

PMID:
15625238
43.

Pharmacologic rescue of conformationally-defective proteins: implications for the treatment of human disease.

Ulloa-Aguirre A, Janovick JA, Brothers SP, Conn PM.

Traffic. 2004 Nov;5(11):821-37. Review.

44.
45.

Misrouted cell surface GnRH receptors as a disease aetiology for congenital isolated hypogonadotrophic hypogonadism.

Ulloa-Aguirre A, Janovick JA, Leaños-Miranda A, Conn PM.

Hum Reprod Update. 2004 Mar-Apr;10(2):177-92. Review.

PMID:
15073146
46.

Protein origami: therapeutic rescue of misfolded gene products.

Conn PM, Leaños-Miranda A, Janovick JA.

Mol Interv. 2002 Sep;2(5):308-16. Review.

PMID:
14993385
47.

Evolved regulation of gonadotropin-releasing hormone receptor cell surface expression.

Janovick JA, Ulloa-Aguirre A, Conn PM.

Endocrine. 2003 Dec;22(3):317-27.

PMID:
14709805
49.

Regulation of FSHbeta and GnRH receptor gene expression in activin receptor II knockout male mice.

Kumar TR, Agno J, Janovick JA, Conn PM, Matzuk MM.

Mol Cell Endocrinol. 2003 Dec 30;212(1-2):19-27.

PMID:
14654247
50.

Four naturally occurring mutations in the human GnRH receptor affect ligand binding and receptor function.

Bédécarrats GY, Linher KD, Janovick JA, Beranova M, Kada F, Seminara SB, Michael Conn P, Kaiser UB.

Mol Cell Endocrinol. 2003 Jul 31;205(1-2):51-64.

PMID:
12890567

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