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Novel neuroactive steroid with hypnotic and T-channel blocking properties exerts effective analgesia in a rodent model of post-surgical pain.

Joksimovic SL, Joksimovic SM, Manzella FM, Asnake B, Orestes P, Raol YH, Krishnan K, Covey DF, Jevtovic-Todorovic V, Todorovic SM.

Br J Pharmacol. 2019 Nov 15. doi: 10.1111/bph.14930. [Epub ahead of print]


Cholesterol accessibility at the ciliary membrane controls hedgehog signaling.

Kinnebrew M, Iverson EJ, Patel BB, Pusapati GV, Kong JH, Johnson KA, Luchetti G, Eckert KM, McDonald JG, Covey DF, Siebold C, Radhakrishnan A, Rohatgi R.

Elife. 2019 Oct 30;8. pii: e50051. doi: 10.7554/eLife.50051.


Neurosteroids as novel antidepressants and anxiolytics: GABA-A receptors and beyond.

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

Neurobiol Stress. 2019 Sep 27;11:100196. doi: 10.1016/j.ynstr.2019.100196. eCollection 2019 Nov.


The morphogen Sonic hedgehog inhibits its receptor Patched by a pincer grasp mechanism.

Rudolf AF, Kinnebrew M, Kowatsch C, Ansell TB, El Omari K, Bishop B, Pardon E, Schwab RA, Malinauskas T, Qian M, Duman R, Covey DF, Steyaert J, Wagner A, Sansom MSP, Rohatgi R, Siebold C.

Nat Chem Biol. 2019 Oct;15(10):975-982. doi: 10.1038/s41589-019-0370-y. Epub 2019 Sep 23.


Binding and intracellular transport of 25-hydroxycholesterol by Niemann-Pick C2 protein.

Petersen D, Reinholdt P, Szomek M, Hansen SK, Poongavanam V, Dupont A, Heegaard CW, Krishnan K, Fujiwara H, Covey DF, Ory DS, Kongsted J, Wüstner D.

Biochim Biophys Acta Biomembr. 2019 Sep 12:183063. doi: 10.1016/j.bbamem.2019.183063. [Epub ahead of print]


Mechanism of Action of VP1-001 in cryAB(R120G)-Associated and Age-Related Cataracts.

Molnar KS, Dunyak BM, Su B, Izrayelit Y, McGlasson-Naumann B, Hamilton PD, Qian M, Covey DF, Gestwicki JE, Makley LN, Andley UP.

Invest Ophthalmol Vis Sci. 2019 Aug 1;60(10):3320-3331. doi: 10.1167/iovs.18-25647.


Multiple neurosteroid and cholesterol binding sites in voltage-dependent anion channel-1 determined by photo-affinity labeling.

Cheng WWL, Budelier MM, Sugasawa Y, Bergdoll L, Queralt-Martín M, Rosencrans W, Rostovtseva TK, Chen ZW, Abramson J, Krishnan K, Covey DF, Whitelegge JP, Evers AS.

Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Oct;1864(10):1269-1279. doi: 10.1016/j.bbalip.2019.06.004. Epub 2019 Jun 5.


The molecular determinants of neurosteroid binding in the GABA(A) receptor.

Sugasawa Y, Bracamontes JR, Krishnan K, Covey DF, Reichert DE, Akk G, Chen Q, Tang P, Evers AS, Cheng WWL.

J Steroid Biochem Mol Biol. 2019 Sep;192:105383. doi: 10.1016/j.jsbmb.2019.105383. Epub 2019 May 28.


Metabolism of Non-Enzymatically Derived Oxysterols: Clues from sterol metabolic disorders.

Griffiths WJ, Yutuc E, Abdel-Khalik J, Crick PJ, Hearn T, Dickson A, Bigger BW, Hoi-Yee Wu T, Goenka A, Ghosh A, Jones SA, Covey DF, Ory DS, Wang Y.

Free Radic Biol Med. 2019 Nov 20;144:124-133. doi: 10.1016/j.freeradbiomed.2019.04.020. Epub 2019 Apr 19.


Novel neurosteroid hypnotic blocks T-type calcium channel-dependent rebound burst firing and suppresses long-term potentiation in the rat subiculum.

Joksimovic SM, Izumi Y, Joksimovic SL, Tesic V, Krishnan K, Asnake B, Jevtovic-Todorovic V, Covey DF, Zorumski CF, Todorovic SM.

Br J Anaesth. 2019 May;122(5):643-651. doi: 10.1016/j.bja.2019.01.029. Epub 2019 Feb 28.


Multiple functional neurosteroid binding sites on GABAA receptors.

Chen ZW, Bracamontes JR, Budelier MM, Germann AL, Shin DJ, Kathiresan K, Qian MX, Manion B, Cheng WWL, Reichert DE, Akk G, Covey DF, Evers AS.

PLoS Biol. 2019 Mar 7;17(3):e3000157. doi: 10.1371/journal.pbio.3000157. eCollection 2019 Mar.


Neurosteroids and oxysterols as potential therapeutic agents for glaucoma and Alzheimer's disease.

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

Neuropsychiatry (London). 2018;8(1):344-359. doi: 10.4172/Neuropsychiatry.1000356.


Synthesis and characterization of diazirine alkyne probes for the study of intracellular cholesterol trafficking.

Feltes M, Moores S, Gale SE, Krishnan K, Mydock-McGrane L, Covey DF, Ory DS, Schaffer JE.

J Lipid Res. 2019 Mar;60(3):707-716. doi: 10.1194/jlr.D091470. Epub 2019 Jan 7.


A Clickable Oxysterol Photolabel Retains NMDA Receptor Activity and Accumulates in Neurons.

Chen DM, Ziolkowski L, Benz A, Qian M, Zorumski CF, Covey DF, Mennerick S.

Front Neurosci. 2018 Dec 6;12:923. doi: 10.3389/fnins.2018.00923. eCollection 2018.


Common binding sites for cholesterol and neurosteroids on a pentameric ligand-gated ion channel.

Budelier MM, Cheng WWL, Chen ZW, Bracamontes JR, Sugasawa Y, Krishnan K, Mydock-McGrane L, Covey DF, Evers AS.

Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Feb;1864(2):128-136. doi: 10.1016/j.bbalip.2018.11.005. Epub 2018 Nov 22.


Analysis of GABAA Receptor Activation by Combinations of Agonists Acting at the Same or Distinct Binding Sites.

Shin DJ, Germann AL, Covey DF, Steinbach JH, Akk G.

Mol Pharmacol. 2019 Jan;95(1):70-81. doi: 10.1124/mol.118.113464. Epub 2018 Oct 18.


Neurosteroids in Pain Management: A New Perspective on an Old Player.

Joksimovic SL, Covey DF, Jevtovic-Todorovic V, Todorovic SM.

Front Pharmacol. 2018 Oct 2;9:1127. doi: 10.3389/fphar.2018.01127. eCollection 2018. Review.


Visualizing pregnenolone sulfate-like modulators of NMDA receptor function reveals intracellular and plasma-membrane localization.

Chisari M, Wilding TJ, Brunwasser S, Krishnan K, Qian M, Benz A, Huettner JE, Zorumski CF, Covey DF, Mennerick S.

Neuropharmacology. 2019 Jan;144:91-103. doi: 10.1016/j.neuropharm.2018.10.015. Epub 2018 Oct 15.


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.

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