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Additive neuroprotective effects of 24(S)-hydroxycholesterol and allopregnanolone in an ex vivo rat glaucoma model.

Ishikawa M, Yoshitomi T, Covey DF, Zorumski CF, Izumi Y.

Sci Rep. 2018 Aug 27;8(1):12851. doi: 10.1038/s41598-018-31239-2.


A neurosteroid analogue with T-type calcium channel blocking properties is an effective hypnotic, but is not harmful to neonatal rat brain.

Atluri N, Joksimovic SM, Oklopcic A, Milanovic D, Klawitter J, Eggan P, Krishnan K, Covey DF, Todorovic SM, Jevtovic-Todorovic V.

Br J Anaesth. 2018 Apr;120(4):768-778. doi: 10.1016/j.bja.2017.12.039. Epub 2018 Feb 9.


Mapping two neurosteroid-modulatory sites in the prototypic pentameric ligand-gated ion channel GLIC.

Cheng WWL, Chen ZW, Bracamontes JR, Budelier MM, Krishnan K, Shin DJ, Wang C, Jiang X, Covey DF, Akk G, Evers AS.

J Biol Chem. 2018 Feb 23;293(8):3013-3027. doi: 10.1074/jbc.RA117.000359. Epub 2018 Jan 4.


Structural design of intrinsically fluorescent oxysterols.

Nåbo LJ, Modzel M, Krishnan K, Covey DF, Fujiwara H, Ory DS, Szomek M, Khandelia H, Wüstner D, Kongsted J.

Chem Phys Lipids. 2018 May;212:26-34. doi: 10.1016/j.chemphyslip.2017.12.005. Epub 2017 Dec 26.


ACCP Template for Evaluating a Clinical Pharmacist.

Lee M, Badowski ME, Acquisto NM, Covey DF, Fox BD, Gaffney SM, Haines ST, Hilaire ML, Raymond A, Salvo MC, Turner K.

Pharmacotherapy. 2017 May;37(5):e21-e29. doi: 10.1002/phar.1927. Epub 2017 Apr 17.


Photoaffinity labeling with cholesterol analogues precisely maps a cholesterol-binding site in voltage-dependent anion channel-1.

Budelier MM, Cheng WWL, Bergdoll L, Chen ZW, Janetka JW, Abramson J, Krishnan K, Mydock-McGrane L, Covey DF, Whitelegge JP, Evers AS.

J Biol Chem. 2017 Jun 2;292(22):9294-9304. doi: 10.1074/jbc.M116.773069. Epub 2017 Apr 10.


Lysosomal cholesterol activates mTORC1 via an SLC38A9-Niemann-Pick C1 signaling complex.

Castellano BM, Thelen AM, Moldavski O, Feltes M, van der Welle RE, Mydock-McGrane L, Jiang X, van Eijkeren RJ, Davis OB, Louie SM, Perera RM, Covey DF, Nomura DK, Ory DS, Zoncu R.

Science. 2017 Mar 24;355(6331):1306-1311. doi: 10.1126/science.aag1417.


Synthesis of side-chain oxysterols and their enantiomers through cross-metathesis reactions of Δ22 steroids.

Brownholland DP, Covey DF.

Steroids. 2017 May;121:22-31. doi: 10.1016/j.steroids.2017.03.002. Epub 2017 Mar 12.


Click Chemistry Reagent for Identification of Sites of Covalent Ligand Incorporation in Integral Membrane Proteins.

Budelier MM, Cheng WW, Bergdoll L, Chen ZW, Abramson J, Krishnan K, Qian M, Covey DF, Janetka JW, Evers AS.

Anal Chem. 2017 Feb 21;89(4):2636-2644. doi: 10.1021/acs.analchem.6b05003. Epub 2017 Feb 9.


A novel mechanism of non-feminizing estrogens in neuroprotection.

Engler-Chiurazzi EB, Covey DF, Simpkins JW.

Exp Gerontol. 2017 Aug;94:99-102. doi: 10.1016/j.exger.2016.10.013. Epub 2016 Nov 3. Review.


Fatty acid synthesis configures the plasma membrane for inflammation in diabetes.

Wei X, Song H, Yin L, Rizzo MG, Sidhu R, Covey DF, Ory DS, Semenkovich CF.

Nature. 2016 Nov 10;539(7628):294-298. doi: 10.1038/nature20117. Epub 2016 Nov 2.


Structure-activity studies of non-steroid analogues structurally-related to neuroprotective estrogens.

Qian M, Engler-Chiurazzi EB, Lewis SE, Rath NP, Simpkins JW, Covey DF.

Org Biomol Chem. 2016 Oct 18;14(41):9790-9805.


Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling.

Luchetti G, Sircar R, Kong JH, Nachtergaele S, Sagner A, Byrne EF, Covey DF, Siebold C, Rohatgi R.

Elife. 2016 Oct 5;5. pii: e20304. doi: 10.7554/eLife.20304.


TSPO activation modulates the effects of high pressure in a rat ex vivo glaucoma model.

Ishikawa M, Yoshitomi T, Covey DF, Zorumski CF, Izumi Y.

Neuropharmacology. 2016 Dec;111:142-159. doi: 10.1016/j.neuropharm.2016.09.001. Epub 2016 Sep 3.


Structural basis of Smoothened regulation by its extracellular domains.

Byrne EFX, Sircar R, Miller PS, Hedger G, Luchetti G, Nachtergaele S, Tully MD, Mydock-McGrane L, Covey DF, Rambo RP, Sansom MSP, Newstead S, Rohatgi R, Siebold C.

Nature. 2016 Jul 28;535(7613):517-522. doi: 10.1038/nature18934. Epub 2016 Jul 20.


Development of a bile acid-based newborn screen for Niemann-Pick disease type C.

Jiang X, Sidhu R, Mydock-McGrane L, Hsu FF, Covey DF, Scherrer DE, Earley B, Gale SE, Farhat NY, Porter FD, Dietzen DJ, Orsini JJ, Berry-Kravis E, Zhang X, Reunert J, Marquardt T, Runz H, Giugliani R, Schaffer JE, Ory DS.

Sci Transl Med. 2016 May 4;8(337):337ra63. doi: 10.1126/scitranslmed.aaf2326.


A clickable neurosteroid photolabel reveals selective Golgi compartmentalization with preferential impact on proximal inhibition.

Jiang X, Shu HJ, Krishnan K, Qian M, Taylor AA, Covey DF, Zorumski CF, Mennerick S.

Neuropharmacology. 2016 Sep;108:193-206. doi: 10.1016/j.neuropharm.2016.04.031. Epub 2016 Apr 22.


Comparison of Steroid Modulation of Spontaneous Inhibitory Postsynaptic Currents in Cultured Hippocampal Neurons and Steady-State Single-Channel Currents from Heterologously Expressed α1β2γ2L GABA(A) Receptors.

Chakrabarti S, Qian M, Krishnan K, Covey DF, Mennerick S, Akk G.

Mol Pharmacol. 2016 Apr;89(4):399-406. doi: 10.1124/mol.115.102202. Epub 2016 Jan 14.


Structural determinants of ligand binding in the ternary complex of human ileal bile acid binding protein with glycocholate and glycochenodeoxycholate obtained from solution NMR.

Horváth G, Bencsura Á, Simon Á, Tochtrop GP, DeKoster GT, Covey DF, Cistola DP, Toke O.

FEBS J. 2016 Feb;283(3):541-55. doi: 10.1111/febs.13610. Epub 2016 Jan 4.


A novel intrinsically fluorescent probe for study of uptake and trafficking of 25-hydroxycholesterol.

Iaea DB, Gale SE, Bielska AA, Krishnan K, Fujiwara H, Jiang H, Maxfield FR, Schlesinger PH, Covey DF, Schaffer JE, Ory DS.

J Lipid Res. 2015 Dec;56(12):2408-19. doi: 10.1194/jlr.D064287. Epub 2015 Oct 24.


Correction to Synthesis of a Smoothened Cholesterol: 18,19-Di-nor-cholesterol.

Mydock-McGrane L, Rath NP, Covey DF.

J Org Chem. 2015 Jun 5;80(11):6000. doi: 10.1021/acs.joc.5b01073. Epub 2015 May 19. No abstract available.


Eliminating the roughness in cholesterol's β-face: does it matter?

Krause MR, Wang M, Mydock-McGrane L, Covey DF, Tejada E, Almeida PF, Regen SL.

Langmuir. 2014 Oct 21;30(41):12114-8. doi: 10.1021/la503075e. Epub 2014 Oct 10.


Membrane dipole potential is sensitive to cholesterol stereospecificity: implications for receptor function.

Bandari S, Chakraborty H, Covey DF, Chattopadhyay A.

Chem Phys Lipids. 2014 Dec;184:25-9. doi: 10.1016/j.chemphyslip.2014.09.001. Epub 2014 Sep 16.


Different oxysterols have opposing actions at N-methyl-D-aspartate receptors.

Linsenbardt AJ, Taylor A, Emnett CM, Doherty JJ, Krishnan K, Covey DF, Paul SM, Zorumski CF, Mennerick S.

Neuropharmacology. 2014 Oct;85:232-42. doi: 10.1016/j.neuropharm.2014.05.027. Epub 2014 May 27.


Synthesis of a smoothened cholesterol: 18,19-di-nor-cholesterol.

Mydock-McGrane L, Rath NP, Covey DF.

J Org Chem. 2014 Jun 20;79(12):5636-43. doi: 10.1021/jo500813n. Epub 2014 May 29. Erratum in: J Org Chem. 2015 Jun 5;80(11):6000.


Inhibition of CaV3.2 T-type calcium channels in peripheral sensory neurons contributes to analgesic properties of epipregnanolone.

Ayoola C, Hwang SM, Hong SJ, Rose KE, Boyd C, Bozic N, Park JY, Osuru HP, DiGruccio MR, Covey DF, Jevtovic-Todorovic V, Todorovic SM.

Psychopharmacology (Berl). 2014 Sep;231(17):3503-3515. doi: 10.1007/s00213-014-3588-0. Epub 2014 May 7.


Side-chain oxysterols modulate cholesterol accessibility through membrane remodeling.

Bielska AA, Olsen BN, Gale SE, Mydock-McGrane L, Krishnan K, Baker NA, Schlesinger PH, Covey DF, Ory DS.

Biochemistry. 2014 May 13;53(18):3042-51. doi: 10.1021/bi5000096. Epub 2014 May 1.


11-trifluoromethyl-phenyldiazirinyl neurosteroid analogues: potent general anesthetics and photolabeling reagents for GABAA receptors.

Chen ZW, Wang C, Krishnan K, Manion BD, Hastings R, Bracamontes J, Taylor A, Eaton MM, Zorumski CF, Steinbach JH, Akk G, Mennerick S, Covey DF, Evers AS.

Psychopharmacology (Berl). 2014 Sep;231(17):3479-91. doi: 10.1007/s00213-014-3568-4. Epub 2014 Apr 23.


Anticonvulsant potencies of the enantiomers of the neurosteroids androsterone and etiocholanolone exceed those of the natural forms.

Zolkowska D, Dhir A, Krishnan K, Covey DF, Rogawski MA.

Psychopharmacology (Berl). 2014 Sep;231(17):3325-32. doi: 10.1007/s00213-014-3546-x. Epub 2014 Apr 5.


Tracking the subcellular fate of 20(s)-hydroxycholesterol with click chemistry reveals a transport pathway to the Golgi.

Peyrot SM, Nachtergaele S, Luchetti G, Mydock-McGrane LK, Fujiwara H, Scherrer D, Jallouk A, Schlesinger PH, Ory DS, Covey DF, Rohatgi R.

J Biol Chem. 2014 Apr 18;289(16):11095-110. doi: 10.1074/jbc.M113.540351. Epub 2014 Mar 4.


Neuroprotection by the synthetic neurosteroid enantiomers ent-PREGS and ent-DHEAS against Aβ₂₅₋₃₅ peptide-induced toxicity in vitro and in vivo in mice.

El Bitar F, Meunier J, Villard V, Alméras M, Krishnan K, Covey DF, Maurice T, Akwa Y.

Psychopharmacology (Berl). 2014 Sep;231(17):3293-3312. doi: 10.1007/s00213-014-3435-3. Epub 2014 Jan 31.


Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.

Qian M, Krishnan K, Kudova E, Li P, Manion BD, Taylor A, Elias G, Akk G, Evers AS, Zorumski CF, Mennerick S, Covey DF.

J Med Chem. 2014 Jan 9;57(1):171-90. doi: 10.1021/jm401577c. Epub 2013 Dec 24.


Modulation of the human ρ1 GABAA receptor by inhibitory steroids.

Eaton MM, Lim YB, Covey DF, Akk G.

Psychopharmacology (Berl). 2014 Sep;231(17):3467-78. doi: 10.1007/s00213-013-3379-z. Epub 2013 Dec 7.


Structural requirements of steroidal agonists of transient receptor potential melastatin 3 (TRPM3) cation channels.

Drews A, Mohr F, Rizun O, Wagner TF, Dembla S, Rudolph S, Lambert S, Konrad M, Philipp SE, Behrendt M, Marchais-Oberwinkler S, Covey DF, Oberwinkler J.

Br J Pharmacol. 2014 Feb;171(4):1019-32. doi: 10.1111/bph.12521.


Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling.

Nachtergaele S, Whalen DM, Mydock LK, Zhao Z, Malinauskas T, Krishnan K, Ingham PW, Covey DF, Siebold C, Rohatgi R.

Elife. 2013 Oct 29;2:e01340. doi: 10.7554/eLife.01340.


The structural basis of cholesterol accessibility in membranes.

Olsen BN, Bielska AA, Lee T, Daily MD, Covey DF, Schlesinger PH, Baker NA, Ory DS.

Biophys J. 2013 Oct 15;105(8):1838-47. doi: 10.1016/j.bpj.2013.08.042.


Stereospecific requirement of cholesterol in the function of the serotonin1A receptor.

Jafurulla M, Rao BD, Sreedevi S, Ruysschaert JM, Covey DF, Chattopadhyay A.

Biochim Biophys Acta. 2014 Jan;1838(1 Pt B):158-63. doi: 10.1016/j.bbamem.2013.08.015. Epub 2013 Sep 2.


Reversal of neuropathic pain in diabetes by targeting glycosylation of Ca(V)3.2 T-type calcium channels.

Orestes P, Osuru HP, McIntire WE, Jacus MO, Salajegheh R, Jagodic MM, Choe W, Lee J, Lee SS, Rose KE, Poiro N, Digruccio MR, Krishnan K, Covey DF, Lee JH, Barrett PQ, Jevtovic-Todorovic V, Todorovic SM.

Diabetes. 2013 Nov;62(11):3828-38. doi: 10.2337/db13-0813. Epub 2013 Jul 8.


The transcription factor STAT-1 couples macrophage synthesis of 25-hydroxycholesterol to the interferon antiviral response.

Blanc M, Hsieh WY, Robertson KA, Kropp KA, Forster T, Shui G, Lacaze P, Watterson S, Griffiths SJ, Spann NJ, Meljon A, Talbot S, Krishnan K, Covey DF, Wenk MR, Craigon M, Ruzsics Z, Haas J, Angulo A, Griffiths WJ, Glass CK, Wang Y, Ghazal P.

Immunity. 2013 Jan 24;38(1):106-18. doi: 10.1016/j.immuni.2012.11.004. Epub 2012 Dec 27.


Neurosteroids, stress and depression: potential therapeutic opportunities.

Zorumski CF, Paul SM, Izumi Y, Covey DF, Mennerick S.

Neurosci Biobehav Rev. 2013 Jan;37(1):109-22. doi: 10.1016/j.neubiorev.2012.10.005. Epub 2012 Oct 17. Review.


Neurosteroid analog photolabeling of a site in the third transmembrane domain of the β3 subunit of the GABA(A) receptor.

Chen ZW, Manion B, Townsend RR, Reichert DE, Covey DF, Steinbach JH, Sieghart W, Fuchs K, Evers AS.

Mol Pharmacol. 2012 Sep;82(3):408-19. doi: 10.1124/mol.112.078410. Epub 2012 May 30.


Neuroprotection with non-feminizing estrogen analogues: an overlooked possible therapeutic strategy.

Simpkins JW, Richardson TE, Yi KD, Perez E, Covey DF.

Horm Behav. 2013 Feb;63(2):278-83. doi: 10.1016/j.yhbeh.2012.03.013. Epub 2012 Apr 3. Review.


A neurosteroid analogue photolabeling reagent labels the colchicine-binding site on tubulin: a mass spectrometric analysis.

Chen ZW, Chen LH, Akentieva N, Lichti CF, Darbandi R, Hastings R, Covey DF, Reichert DE, Townsend RR, Evers AS.

Electrophoresis. 2012 Feb;33(4):666-74. doi: 10.1002/elps.201100434.


Oxysterols as non-genomic regulators of cholesterol homeostasis.

Bielska AA, Schlesinger P, Covey DF, Ory DS.

Trends Endocrinol Metab. 2012 Mar;23(3):99-106. doi: 10.1016/j.tem.2011.12.002. Epub 2012 Jan 11.


Oxysterols are allosteric activators of the oncoprotein Smoothened.

Nachtergaele S, Mydock LK, Krishnan K, Rammohan J, Schlesinger PH, Covey DF, Rohatgi R.

Nat Chem Biol. 2012 Jan 8;8(2):211-20. doi: 10.1038/nchembio.765.


Neurosteroid analogues. 17. Inverted binding orientations of androsterone enantiomers at the steroid potentiation site on γ-aminobutyric acid type A receptors.

Krishnan K, Manion BD, Taylor A, Bracamontes J, Steinbach JH, Reichert DE, Evers AS, Zorumski CF, Mennerick S, Covey DF.

J Med Chem. 2012 Feb 9;55(3):1334-45. doi: 10.1021/jm2014925. Epub 2012 Jan 18.


Cholesterol tuning of BK ethanol response is enantioselective, and is a function of accompanying lipids.

Yuan C, Chen M, Covey DF, Johnston LJ, Treistman SN.

PLoS One. 2011;6(11):e27572. doi: 10.1371/journal.pone.0027572. Epub 2011 Nov 29.


Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes.

Shu HJ, Bracamontes J, Taylor A, Wu K, Eaton MM, Akk G, Manion B, Evers AS, Krishnan K, Covey DF, Zorumski CF, Steinbach JH, Mennerick S.

Br J Pharmacol. 2012 Apr;165(7):2228-43. doi: 10.1111/j.1476-5381.2011.01690.x.


Glucuronidation of the steroid enantiomers ent-17β-estradiol, ent-androsterone and ent-etiocholanolone by the human UDP-glucuronosyltransferases.

Sneitz N, Krishnan K, Covey DF, Finel M.

J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):282-8. doi: 10.1016/j.jsbmb.2011.08.008. Epub 2011 Aug 27.

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