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Items: 1 to 50 of 188

1.

Orally bioavailable glutamine antagonist prodrug JHU-083 penetrates mouse brain and suppresses the growth of MYC-driven medulloblastoma.

Hanaford AR, Alt J, Rais R, Wang SZ, Kaur H, Thorek DLJ, Eberhart CG, Slusher BS, Martin AM, Raabe EH.

Transl Oncol. 2019 Jul 21;12(10):1314-1322. doi: 10.1016/j.tranon.2019.05.013. [Epub ahead of print]

2.

Erratum.

Soomro I, Sun Y, Li Z, Diggs L, Hatzivassiliou G, Thomas AG, Rais R, Parker SJ, Slusher BS, Kimmelman AC, Somlo S, Skolnik EY.

Nephrol Dial Transplant. 2019 May 20. pii: gfz109. doi: 10.1093/ndt/gfz109. [Epub ahead of print] No abstract available.

PMID:
31329939
3.

Unbiased Metabolic Profiling Predicts Sensitivity of High MYC-Expressing Atypical Teratoid/Rhabdoid Tumors to Glutamine Inhibition with 6-Diazo-5-Oxo-L-Norleucine.

Wang SZ, Poore B, Alt J, Price A, Allen SJ, Hanaford AR, Kaur H, Orr BA, Slusher BS, Eberhart CG, Raabe EH, Rubens JA.

Clin Cancer Res. 2019 Jul 12. doi: 10.1158/1078-0432.CCR-19-0189. [Epub ahead of print]

PMID:
31300448
4.

The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists.

Battiti FO, Cemaj SL, Guerrero AM, Shaik AB, Lam J, Rais R, Slusher BS, Deschamps JR, Imler GH, Newman AH, Bonifazi A.

J Med Chem. 2019 Jul 11;62(13):6287-6314. doi: 10.1021/acs.jmedchem.9b00702. Epub 2019 Jul 1.

PMID:
31257877
5.

Upregulation of the Glutaminase II Pathway Contributes to Glutamate Production upon Glutaminase 1 Inhibition in Pancreatic Cancer.

Udupa S, Nguyen S, Hoang G, Nguyen T, Quinones A, Pham K, Asaka R, Nguyen K, Zhang C, Elgogary A, Jung JG, Xu Q, Fu J, Thomas AG, Tsukamoto T, Hanes J, Slusher BS, Cooper AJL, Le A.

Proteomics. 2019 Jun 24:e1800451. doi: 10.1002/pmic.201800451. [Epub ahead of print]

PMID:
31231915
6.

Glutamine Antagonist JHU083 Normalizes Aberrant Glutamate Production and Cognitive Deficits in the EcoHIV Murine Model of HIV-Associated Neurocognitive Disorders.

Nedelcovych MT, Kim BH, Zhu X, Lovell LE, Manning AA, Kelschenbach J, Hadas E, Chao W, Prchalová E, Dash RP, Wu Y, Alt J, Thomas AG, Rais R, Kamiya A, Volsky DJ, Slusher BS.

J Neuroimmune Pharmacol. 2019 Jun 17. doi: 10.1007/s11481-019-09859-w. [Epub ahead of print]

PMID:
31209775
7.

DCC-related developmental effects of abused- versus therapeutic-like amphetamine doses in adolescence.

Cuesta S, Restrepo-Lozano JM, Popescu C, He S, Reynolds LM, Israel S, Hernandez G, Rais R, Slusher BS, Flores C.

Addict Biol. 2019 Jun 13:e12791. doi: 10.1111/adb.12791. [Epub ahead of print]

PMID:
31192517
8.

Intranasal insulin therapy reverses hippocampal dendritic injury and cognitive impairment in a model of HIV-associated neurocognitive disorders in EcoHIV-infected mice.

Kim BH, Kelschenbach J, Borjabad A, Hadas E, He H, Potash MJ, Nedelcovych MT, Rais R, Haughey NJ, McArthur JC, Slusher BS, Volsky DJ.

AIDS. 2019 May 1;33(6):973-984. doi: 10.1097/QAD.0000000000002150.

9.

Neutral sphingomyelinase 2 inhibitors based on the 4-(1H-imidazol-2-yl)-2,6-dialkoxyphenol scaffold.

Stepanek O, Hin N, Thomas AG, Dash RP, Alt J, Rais R, Rojas C, Slusher BS, Tsukamoto T.

Eur J Med Chem. 2019 May 15;170:276-289. doi: 10.1016/j.ejmech.2019.03.015. Epub 2019 Mar 9.

PMID:
30921693
10.

Tumor-Targeted Delivery of 6-Diazo-5-oxo-l-norleucine (DON) Using Substituted Acetylated Lysine Prodrugs.

Tenora L, Alt J, Dash RP, Gadiano AJ, Novotná K, Veeravalli V, Lam J, Kirkpatrick QR, Lemberg KM, Majer P, Rais R, Slusher BS.

J Med Chem. 2019 Apr 11;62(7):3524-3538. doi: 10.1021/acs.jmedchem.8b02009. Epub 2019 Mar 29.

PMID:
30892035
11.

The NAAG'ing Concerns of Modeling Human Alzheimer's Disease in Mice.

Hollinger KR, Alt J, Rais R, Kaplin AI, Slusher BS.

J Alzheimers Dis. 2019;68(3):939-945. doi: 10.3233/JAD-181251.

PMID:
30883361
12.

Correction: JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.

Zhu X, Nedelcovych MT, Thomas AG, Hasegawa Y, Moreno-Megui A, Coomer W, Vohra V, Saito A, Perez G, Wu Y, Alt J, Prchalova E, Tenora L, Majer P, Rais R, Rojas C, Slusher BS, Kamiya A.

Neuropsychopharmacology. 2019 May;44(6):1178. doi: 10.1038/s41386-019-0354-3. Epub 2019 Mar 13.

13.

Dopamine D3R antagonist VK4-116 attenuates oxycodone self-administration and reinstatement without compromising its antinociceptive effects.

You ZB, Bi GH, Galaj E, Kumar V, Cao J, Gadiano A, Rais R, Slusher BS, Gardner EL, Xi ZX, Newman AH.

Neuropsychopharmacology. 2019 Jul;44(8):1415-1424. doi: 10.1038/s41386-018-0284-5. Epub 2018 Nov 27.

PMID:
30555159
14.

Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.

Barinka C, Novakova Z, Hin N, Bím D, Ferraris DV, Duvall B, Kabarriti G, Tsukamoto R, Budesinsky M, Motlova L, Rojas C, Slusher BS, Rokob TA, Rulíšek L, Tsukamoto T.

Bioorg Med Chem. 2019 Jan 15;27(2):255-264. doi: 10.1016/j.bmc.2018.11.022. Epub 2018 Nov 14.

PMID:
30552009
15.

DPTIP, a newly identified potent brain penetrant neutral sphingomyelinase 2 inhibitor, regulates astrocyte-peripheral immune communication following brain inflammation.

Rojas C, Barnaeva E, Thomas AG, Hu X, Southall N, Marugan J, Chaudhuri AD, Yoo SW, Hin N, Stepanek O, Wu Y, Zimmermann SC, Gadiano AG, Tsukamoto T, Rais R, Haughey N, Ferrer M, Slusher BS.

Sci Rep. 2018 Dec 7;8(1):17715. doi: 10.1038/s41598-018-36144-2.

16.

MRI demonstrates glutamine antagonist-mediated reversal of cerebral malaria pathology in mice.

Riggle BA, Sinharay S, Schreiber-Stainthorp W, Munasinghe JP, Maric D, Prchalova E, Slusher BS, Powell JD, Miller LH, Pierce SK, Hammoud DA.

Proc Natl Acad Sci U S A. 2018 Dec 18;115(51):E12024-E12033. doi: 10.1073/pnas.1812909115. Epub 2018 Dec 4.

17.

Ghrelin agonist HM01 attenuates chemotherapy-induced neurotoxicity in rodent models.

Chiorazzi A, Wozniak KM, Rais R, Wu Y, Gadiano AJ, Farah MH, Liu Y, Canta A, Alberti P, Rodriguez-Menendez V, Meregalli C, Fumagalli G, Monza L, Pozzi E, Vornov JJ, Polydefkis M, Pietra C, Slusher BS, Cavaletti G.

Eur J Pharmacol. 2018 Dec 5;840:89-103. doi: 10.1016/j.ejphar.2018.09.029. Epub 2018 Sep 27.

PMID:
30268665
18.

Structural basis for potent inhibition of d-amino acid oxidase by thiophene carboxylic acids.

Kato Y, Hin N, Maita N, Thomas AG, Kurosawa S, Rojas C, Yorita K, Slusher BS, Fukui K, Tsukamoto T.

Eur J Med Chem. 2018 Nov 5;159:23-34. doi: 10.1016/j.ejmech.2018.09.040. Epub 2018 Sep 18.

PMID:
30265959
19.

Inhibition of mTORC1 in pediatric low-grade glioma depletes glutathione and therapeutically synergizes with carboplatin.

Poore B, Yuan M, Arnold A, Price A, Alt J, Rubens JA, Slusher BS, Eberhart CG, Raabe EH.

Neuro Oncol. 2019 Feb 14;21(2):252-263. doi: 10.1093/neuonc/noy150.

PMID:
30239952
20.

We're Not "DON" Yet: Optimal Dosing and Prodrug Delivery of 6-Diazo-5-oxo-L-norleucine.

Lemberg KM, Vornov JJ, Rais R, Slusher BS.

Mol Cancer Ther. 2018 Sep;17(9):1824-1832. doi: 10.1158/1535-7163.MCT-17-1148. Review.

PMID:
30181331
21.

JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.

Zhu X, Nedelcovych MT, Thomas AG, Hasegawa Y, Moreno-Megui A, Coomer W, Vohra V, Saito A, Perez G, Wu Y, Alt J, Prchalova E, Tenora L, Majer P, Rais R, Rojas C, Slusher BS, Kamiya A.

Neuropsychopharmacology. 2019 Mar;44(4):683-694. doi: 10.1038/s41386-018-0177-7. Epub 2018 Aug 13. Erratum in: Neuropsychopharmacology. 2019 May;44(6):1178.

PMID:
30127344
22.

Differential Morphological and Biochemical Recovery from Chemotherapy-Induced Peripheral Neuropathy Following Paclitaxel, Ixabepilone, or Eribulin Treatment in Mouse Sciatic Nerves.

Cook BM, Wozniak KM, Proctor DA, Bromberg RB, Wu Y, Slusher BS, Littlefield BA, Jordan MA, Wilson L, Feinstein SC.

Neurotox Res. 2018 Oct;34(3):677-692. doi: 10.1007/s12640-018-9929-8. Epub 2018 Jul 26.

PMID:
30051419
23.

NaV1.1 inhibition can reduce visceral hypersensitivity.

Salvatierra J, Castro J, Erickson A, Li Q, Braz J, Gilchrist J, Grundy L, Rychkov GY, Deiteren A, Rais R, King GF, Slusher BS, Basbaum A, Pasricha PJ, Brierley SM, Bosmans F.

JCI Insight. 2018 Jun 7;3(11). pii: 121000. doi: 10.1172/jci.insight.121000. eCollection 2018 Jun 7.

24.

N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs.

Zimmermann SC, Tichý T, Vávra J, Dash RP, Slusher CE, Gadiano AJ, Wu Y, Jančařík A, Tenora L, Monincová L, Prchalová E, Riggins GJ, Majer P, Slusher BS, Rais R.

J Med Chem. 2018 May 10;61(9):3918-3929. doi: 10.1021/acs.jmedchem.7b01792. Epub 2018 Apr 19.

PMID:
29648826
25.

Glutamine metabolism via glutaminase 1 in autosomal-dominant polycystic kidney disease.

Soomro I, Sun Y, Li Z, Diggs L, Hatzivassiliou G, Thomas AG, Rais R, Slusher BS, Somlo S, Skolnik EY.

Nephrol Dial Transplant. 2018 Aug 1;33(8):1343-1353. doi: 10.1093/ndt/gfx349.

26.

Pharmacokinetics of Intranasal versus Subcutaneous Insulin in the Mouse.

Nedelcovych MT, Gadiano AJ, Wu Y, Manning AA, Thomas AG, Khuder SS, Yoo SW, Xu J, McArthur JC, Haughey NJ, Volsky DJ, Rais R, Slusher BS.

ACS Chem Neurosci. 2018 Apr 18;9(4):809-816. doi: 10.1021/acschemneuro.7b00434. Epub 2018 Jan 4.

27.

Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.

Zou MF, Cao J, Abramyan AM, Kopajtic T, Zanettini C, Guthrie DA, Rais R, Slusher BS, Shi L, Loland CJ, Newman AH.

J Med Chem. 2017 Dec 28;60(24):10172-10187. doi: 10.1021/acs.jmedchem.7b01454. Epub 2017 Dec 11.

28.

Atypical dopamine transporter inhibitors attenuate compulsive-like methamphetamine self-administration in rats.

Tunstall BJ, Ho CP, Cao J, Vendruscolo JCM, Schmeichel BE, Slack RD, Tanda G, Gadiano AJ, Rais R, Slusher BS, Koob GF, Newman AH, Vendruscolo LF.

Neuropharmacology. 2018 Mar 15;131:96-103. doi: 10.1016/j.neuropharm.2017.12.006. Epub 2017 Dec 5.

29.

Peripheral Neuropathy Induced by Microtubule-Targeted Chemotherapies: Insights into Acute Injury and Long-term Recovery.

Wozniak KM, Vornov JJ, Wu Y, Liu Y, Carozzi VA, Rodriguez-Menendez V, Ballarini E, Alberti P, Pozzi E, Semperboni S, Cook BM, Littlefield BA, Nomoto K, Condon K, Eckley S, DesJardins C, Wilson L, Jordan MA, Feinstein SC, Cavaletti G, Polydefkis M, Slusher BS.

Cancer Res. 2018 Feb 1;78(3):817-829. doi: 10.1158/0008-5472.CAN-17-1467. Epub 2017 Nov 30.

30.

Development of a primary microglia screening assay and its use to characterize inhibition of system xc- by erastin and its analogs.

Figuera-Losada M, Thomas AG, Stathis M, Stockwell BR, Rojas C, Slusher BS.

Biochem Biophys Rep. 2017 Jan 17;9:266-272. doi: 10.1016/j.bbrep.2016.12.009. eCollection 2017 Mar.

31.

The Low-Affinity Binding of Second Generation Radiotracers Targeting TSPO is Associated with a Unique Allosteric Binding Site.

Rojas C, Stathis M, Coughlin JM, Pomper M, Slusher BS.

J Neuroimmune Pharmacol. 2018 Mar;13(1):1-5. doi: 10.1007/s11481-017-9765-2. Epub 2017 Sep 5.

32.

Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs.

Nedelcovych M, Dash RP, Tenora L, Zimmermann SC, Gadiano AJ, Garrett C, Alt J, Hollinger KR, Pommier E, Jančařík A, Rojas C, Thomas AG, Wu Y, Wozniak K, Majer P, Slusher BS, Rais R.

Mol Pharm. 2017 Oct 2;14(10):3248-3257. doi: 10.1021/acs.molpharmaceut.7b00231. Epub 2017 Aug 31.

33.

N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.

Nedelcovych MT, Tenora L, Kim BH, Kelschenbach J, Chao W, Hadas E, Jančařík A, Prchalová E, Zimmermann SC, Dash RP, Gadiano AJ, Garrett C, Furtmüller G, Oh B, Brandacher G, Alt J, Majer P, Volsky DJ, Rais R, Slusher BS.

J Med Chem. 2017 Aug 24;60(16):7186-7198. doi: 10.1021/acs.jmedchem.7b00966. Epub 2017 Aug 14.

34.

Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain.

Rais R, Vávra J, Tichý T, Dash RP, Gadiano AJ, Tenora L, Monincová L, Bařinka C, Alt J, Zimmermann SC, Slusher CE, Wu Y, Wozniak K, Majer P, Tsukamoto T, Slusher BS.

J Med Chem. 2017 Sep 28;60(18):7799-7809. doi: 10.1021/acs.jmedchem.7b00825. Epub 2017 Sep 18.

35.

The Psychiatric Impact of HIV.

Nedelcovych MT, Manning AA, Semenova S, Gamaldo C, Haughey NJ, Slusher BS.

ACS Chem Neurosci. 2017 Jul 19;8(7):1432-1434. doi: 10.1021/acschemneuro.7b00169. Epub 2017 May 24.

36.

Glutamine antagonist-mediated immune suppression decreases pathology but delays virus clearance in mice during nonfatal alphavirus encephalomyelitis.

Baxter VK, Glowinski R, Braxton AM, Potter MC, Slusher BS, Griffin DE.

Virology. 2017 Aug;508:134-149. doi: 10.1016/j.virol.2017.05.013. Epub 2017 May 19.

37.

Microtubule-Targeting Agents Eribulin and Paclitaxel Differentially Affect Neuronal Cell Bodies in Chemotherapy-Induced Peripheral Neuropathy.

Benbow SJ, Wozniak KM, Kulesh B, Savage A, Slusher BS, Littlefield BA, Jordan MA, Wilson L, Feinstein SC.

Neurotox Res. 2017 Jul;32(1):151-162. doi: 10.1007/s12640-017-9729-6. Epub 2017 Apr 8.

38.

Property-Guided Synthesis of Aza-Tricyclic Indolines: Development of Gold Catalysis En Route.

Barbour PM, Wang W, Chang L, Pickard KL, Rais R, Slusher BS, Wang X.

Adv Synth Catal. 2016 Apr 28;358(9):1482-1490. doi: 10.1002/adsc.201501101. Epub 2016 Mar 3.

39.

Role of Academic Drug Discovery in the Quest for New CNS Therapeutics.

Yokley BH, Hartman M, Slusher BS.

ACS Chem Neurosci. 2017 Mar 15;8(3):429-431. doi: 10.1021/acschemneuro.7b00040. Epub 2017 Feb 14.

40.

Local enema treatment to inhibit FOLH1/GCPII as a novel therapy for inflammatory bowel disease.

Date AA, Rais R, Babu T, Ortiz J, Kanvinde P, Thomas AG, Zimmermann SC, Gadiano AJ, Halpert G, Slusher BS, Ensign LM.

J Control Release. 2017 Oct 10;263:132-138. doi: 10.1016/j.jconrel.2017.01.036. Epub 2017 Jan 31.

41.

Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.

Cao J, Slack RD, Bakare OM, Burzynski C, Rais R, Slusher BS, Kopajtic T, Bonifazi A, Ellenberger MP, Yano H, He Y, Bi GH, Xi ZX, Loland CJ, Newman AH.

J Med Chem. 2016 Dec 8;59(23):10676-10691. Epub 2016 Nov 28.

42.

Valley of death: A proposal to build a "translational bridge" for the next generation.

Gamo NJ, Birknow MR, Sullivan D, Kondo MA, Horiuchi Y, Sakurai T, Slusher BS, Sawa A.

Neurosci Res. 2017 Feb;115:1-4. doi: 10.1016/j.neures.2016.11.003. Epub 2016 Nov 19. Review.

43.

Discovery of 6-Diazo-5-oxo-l-norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma.

Rais R, Jančařík A, Tenora L, Nedelcovych M, Alt J, Englert J, Rojas C, Le A, Elgogary A, Tan J, Monincová L, Pate K, Adams R, Ferraris D, Powell J, Majer P, Slusher BS.

J Med Chem. 2016 Sep 22;59(18):8621-33. doi: 10.1021/acs.jmedchem.6b01069. Epub 2016 Sep 6.

PMID:
27560860
44.

Neuromuscular NMDA Receptors Modulate Developmental Synapse Elimination.

Personius KE, Slusher BS, Udin SB.

J Neurosci. 2016 Aug 24;36(34):8783-9. doi: 10.1523/JNEUROSCI.1181-16.2016. Erratum in: J Neurosci. 2018 Nov 7;38(45):9801.

45.

Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer.

Elgogary A, Xu Q, Poore B, Alt J, Zimmermann SC, Zhao L, Fu J, Chen B, Xia S, Liu Y, Neisser M, Nguyen C, Lee R, Park JK, Reyes J, Hartung T, Rojas C, Rais R, Tsukamoto T, Semenza GL, Hanes J, Slusher BS, Le A.

Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36. doi: 10.1073/pnas.1611406113. Epub 2016 Aug 24.

46.

FOLH1/GCPII is elevated in IBD patients, and its inhibition ameliorates murine IBD abnormalities.

Rais R, Jiang W, Zhai H, Wozniak KM, Stathis M, Hollinger KR, Thomas AG, Rojas C, Vornov JJ, Marohn M, Li X, Slusher BS.

JCI Insight. 2016 Aug 4;1(12). pii: e88634.

47.

Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.

Kumar V, Bonifazi A, Ellenberger MP, Keck TM, Pommier E, Rais R, Slusher BS, Gardner E, You ZB, Xi ZX, Newman AH.

J Med Chem. 2016 Aug 25;59(16):7634-50. doi: 10.1021/acs.jmedchem.6b00860. Epub 2016 Aug 10.

48.

Protective Effects of Glutamine Antagonist 6-Diazo-5-Oxo-l-Norleucine in Mice with Alphavirus Encephalomyelitis.

Manivannan S, Baxter VK, Schultz KL, Slusher BS, Griffin DE.

J Virol. 2016 Sep 29;90(20):9251-62. doi: 10.1128/JVI.01045-16. Print 2016 Oct 15.

49.

Structural Basis for Induction of Peripheral Neuropathy by Microtubule-Targeting Cancer Drugs.

Smith JA, Slusher BS, Wozniak KM, Farah MH, Smiyun G, Wilson L, Feinstein S, Jordan MA.

Cancer Res. 2016 Sep 1;76(17):5115-23. doi: 10.1158/0008-5472.CAN-15-3116. Epub 2016 Aug 3.

50.

Paclitaxel causes degeneration of both central and peripheral axon branches of dorsal root ganglia in mice.

Tasnim A, Rammelkamp Z, Slusher AB, Wozniak K, Slusher BS, Farah MH.

BMC Neurosci. 2016 Jul 11;17(1):47. doi: 10.1186/s12868-016-0285-4.

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