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A Novel Microtubule-Binding Drug Attenuates and Reverses Protein Aggregation in Animal Models of Alzheimer's Disease.

Kakraba S, Ayyadevara S, Penthala NR, Balasubramaniam M, Ganne A, Liu L, Alla R, Bommagani SB, Barger SW, Griffin WST, Crooks PA, Shmookler Reis RJ.

Front Mol Neurosci. 2019 Dec 12;12:310. doi: 10.3389/fnmol.2019.00310. eCollection 2019.


Aggregate Interactome Based on Protein Cross-linking Interfaces Predicts Drug Targets to Limit Aggregation in Neurodegenerative Diseases.

Balasubramaniam M, Ayyadevara S, Ganne A, Kakraba S, Penthala NR, Du X, Crooks PA, Griffin ST, Shmookler Reis RJ.

iScience. 2019 Oct 25;20:248-264. doi: 10.1016/j.isci.2019.09.026. Epub 2019 Sep 21.


GZ-11608, a Vesicular Monoamine Transporter-2 Inhibitor, Decreases the Neurochemical and Behavioral Effects of Methamphetamine.

Lee NR, Zheng G, Leggas M, Janganati V, Nickell JR, Crooks PA, Bardo MT, Dwoskin LP.

J Pharmacol Exp Ther. 2019 Nov;371(2):526-543. doi: 10.1124/jpet.119.258699. Epub 2019 Aug 14.


Inhibition of Human DNA Polymerases Eta and Kappa by Indole-Derived Molecules Occurs through Distinct Mechanisms.

Ketkar A, Maddukuri L, Penthala NR, Reed MR, Zafar MK, Crooks PA, Eoff RL.

ACS Chem Biol. 2019 Jun 21;14(6):1337-1351. doi: 10.1021/acschembio.9b00304. Epub 2019 May 22.


Reduced Tolerance and Asymmetrical Crosstolerance to Effects of the Indole Quinuclidinone Analog PNR-4-20, a G Protein-Biased Cannabinoid 1 Receptor Agonist in Mice: Comparisons with Δ9-Tetrahydrocannabinol and JWH-018.

Ford BM, Cabanlong CV, Tai S, Franks LN, Penthala NR, Crooks PA, Prather PL, Fantegrossi WE.

J Pharmacol Exp Ther. 2019 May;369(2):259-269. doi: 10.1124/jpet.118.252965. Epub 2019 Mar 4.


Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.

Kearney SE, Zahoránszky-Kőhalmi G, Brimacombe KR, Henderson MJ, Lynch C, Zhao T, Wan KK, Itkin Z, Dillon C, Shen M, Cheff DM, Lee TD, Bougie D, Cheng K, Coussens NP, Dorjsuren D, Eastman RT, Huang R, Iannotti MJ, Karavadhi S, Klumpp-Thomas C, Roth JS, Sakamuru S, Sun W, Titus SA, Yasgar A, Zhang YQ, Zhao J, Andrade RB, Brown MK, Burns NZ, Cha JK, Mevers EE, Clardy J, Clement JA, Crooks PA, Cuny GD, Ganor J, Moreno J, Morrill LA, Picazo E, Susick RB, Garg NK, Goess BC, Grossman RB, Hughes CC, Johnston JN, Joullie MM, Kinghorn AD, Kingston DGI, Krische MJ, Kwon O, Maimone TJ, Majumdar S, Maloney KN, Mohamed E, Murphy BT, Nagorny P, Olson DE, Overman LE, Brown LE, Snyder JK, Porco JA Jr, Rivas F, Ross SA, Sarpong R, Sharma I, Shaw JT, Xu Z, Shen B, Shi W, Stephenson CRJ, Verano AL, Tan DS, Tang Y, Taylor RE, Thomson RJ, Vosburg DA, Wu J, Wuest WM, Zakarian A, Zhang Y, Ren T, Zuo Z, Inglese J, Michael S, Simeonov A, Zheng W, Shinn P, Jadhav A, Boxer MB, Hall MD, Xia M, Guha R, Rohde JM.

ACS Cent Sci. 2018 Dec 26;4(12):1727-1741. doi: 10.1021/acscentsci.8b00747. Epub 2018 Dec 5.


N-Naphthoyl-substituted indole thio-barbituric acid analogs inhibit the helicase activity of the hepatitis C virus NS3.

Marecki JC, Aarattuthodiyil S, Byrd AK, Penthala NR, Crooks PA, Raney KD.

Bioorg Med Chem Lett. 2019 Feb 1;29(3):430-434. doi: 10.1016/j.bmcl.2018.12.026. Epub 2018 Dec 13.


A novel tetrazole analogue of resveratrol is a potent anticancer agent.

Bommagani S, Penthala NR, Balasubramaniam M, Kuravi S, Caldas-Lopes E, Guzman ML, Balusu R, Crooks PA.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):172-178. doi: 10.1016/j.bmcl.2018.12.006. Epub 2018 Dec 4.


Crystal structure of 13-(E)-(2-amino-benzyl-idene)parthenolide.

Bommagani S, Penthala NR, Parkin S, Crooks PA.

Acta Crystallogr E Crystallogr Commun. 2018 Oct 9;74(Pt 11):1543-1546. doi: 10.1107/S2056989018013622. eCollection 2018 Nov 1.


An improved model of ethanol and nicotine co-use in female P rats: Effects of naltrexone, varenicline, and the selective nicotinic α6β2* antagonist r-bPiDI.

Maggio SE, Saunders MA, Nixon K, Prendergast MA, Zheng G, Crooks PA, Dwoskin LP, Bell RL, Bardo MT.

Drug Alcohol Depend. 2018 Dec 1;193:154-161. doi: 10.1016/j.drugalcdep.2018.09.008. Epub 2018 Oct 17.


Actinomycin-D and dimethylamino-parthenolide synergism in treating human pancreatic cancer cells.

Lamture G, Crooks PA, Borrelli MJ.

Drug Dev Res. 2018 Sep;79(6):287-294. doi: 10.1002/ddr.21441. Epub 2018 Sep 17.


MMB triazole analogs are potent NF-κB inhibitors and anti-cancer agents against both hematological and solid tumor cells.

Janganati V, Ponder J, Balasubramaniam M, Bhat-Nakshatri P, Bar EE, Nakshatri H, Jordan CT, Crooks PA.

Eur J Med Chem. 2018 Sep 5;157:562-581. doi: 10.1016/j.ejmech.2018.08.010. Epub 2018 Aug 10.


Highly sulphated cellulose: a versatile, reusable and selective desilylating agent for deprotection of alcoholic TBDMS ethers.

Dachavaram SS, Penthala NR, Calahan JL, Munson EJ, Crooks PA.

Org Biomol Chem. 2018 Aug 22;16(33):6057-6062. doi: 10.1039/c8ob01438h.


Parthenolide and DMAPT induce cell death in primitive CML cells through reactive oxygen species.

Flores-Lopez G, Moreno-Lorenzana D, Ayala-Sanchez M, Aviles-Vazquez S, Torres-Martinez H, Crooks PA, Guzman ML, Mayani H, Chávez-González A.

J Cell Mol Med. 2018 Oct;22(10):4899-4912. doi: 10.1111/jcmm.13755. Epub 2018 Aug 5.


Evaluation of morphine-like effects of the mixed mu/delta agonist morphine-6-O-sulfate in rats: Drug discrimination and physical dependence.

Yadlapalli JSK, Bommagani SB, Mahelona RD, Wan A, Gannon BM, Penthala NR, Dobretsov M, Crooks PA, Fantegrossi WE.

Pharmacol Res Perspect. 2018 Jun 19;6(4):e00403. doi: 10.1002/prp2.403. eCollection 2018 Jul.


Pinprick hypo- and hyperalgesia in diabetic rats: Can diet content affect experimental outcome?

Yadlapalli JSK, Dogra N, Walbaum AW, Prather PL, Crooks PA, Dobretsov M.

Neurosci Lett. 2018 Apr 23;673:24-27. doi: 10.1016/j.neulet.2018.02.054. Epub 2018 Feb 25.


New Scaffold for Lead Compounds to Treat Methamphetamine Use Disorders.

Lee NR, Zheng G, Crooks PA, Bardo MT, Dwoskin LP.

AAPS J. 2018 Feb 9;20(2):29. doi: 10.1208/s12248-018-0192-y.


A Small-Molecule Inhibitor of Human DNA Polymerase η Potentiates the Effects of Cisplatin in Tumor Cells.

Zafar MK, Maddukuri L, Ketkar A, Penthala NR, Reed MR, Eddy S, Crooks PA, Eoff RL.

Biochemistry. 2018 Feb 20;57(7):1262-1273. doi: 10.1021/acs.biochem.7b01176. Epub 2018 Jan 30.


Preclinical assessment of utility of M6S for multimodal acute and chronic pain treatment in diabetic neuropathy.

Yadlapalli JSK, Dogra N, Walbaum AW, Prather PL, Crooks PA, Dobretsov M.

Life Sci. 2018 Jan 1;192:151-159. doi: 10.1016/j.lfs.2017.11.042. Epub 2017 Nov 28.


Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2.

Hankosky ER, Joolakanti SR, Nickell JR, Janganati V, Dwoskin LP, Crooks PA.

Bioorg Med Chem Lett. 2017 Dec 15;27(24):5467-5472. doi: 10.1016/j.bmcl.2017.10.039. Epub 2017 Oct 20.


Pharmacological Dual Inhibition of Tumor and Tumor-Induced Functional Limitations in a Transgenic Model of Breast Cancer.

Wang R, Bhat-Nakshatri P, Padua MB, Prasad MS, Anjanappa M, Jacobson M, Finnearty C, Sefcsik V, McElyea K, Redmond R, Sandusky G, Penthala N, Crooks PA, Liu J, Zimmers T, Nakshatri H.

Mol Cancer Ther. 2017 Dec;16(12):2747-2758. doi: 10.1158/1535-7163.MCT-17-0717. Epub 2017 Oct 4.


Varenicline and GZ-793A differentially decrease methamphetamine self-administration under a multiple schedule of reinforcement in rats.

Kangiser MM, Dwoskin LP, Zheng G, Crooks PA, Stairs DJ.

Behav Pharmacol. 2018 Feb;29(1):87-97. doi: 10.1097/FBP.0000000000000340.


Characterization of structurally novel G protein biased CB1 agonists: Implications for drug development.

Ford BM, Franks LN, Tai S, Fantegrossi WE, Stahl EL, Berquist MD, Cabanlong CV, Wilson CD, Penthala NR, Crooks PA, Prather PL.

Pharmacol Res. 2017 Nov;125(Pt B):161-177. doi: 10.1016/j.phrs.2017.08.008. Epub 2017 Aug 23.


DMAPT inhibits NF-κB activity and increases sensitivity of prostate cancer cells to X-rays in vitro and in tumor xenografts in vivo.

Mendonca MS, Turchan WT, Alpuche ME, Watson CN, Estabrook NC, Chin-Sinex H, Shapiro JB, Imasuen-Williams IE, Rangel G, Gilley DP, Huda N, Crooks PA, Shapiro RH.

Free Radic Biol Med. 2017 Nov;112:318-326. doi: 10.1016/j.freeradbiomed.2017.08.001. Epub 2017 Aug 3.


Crystal structure of 4,4'-bis-[3-(piperidin-1-yl)prop-1-yn-1-yl]-1,1'-biphen-yl.

Walbaum A, Fifer EK, Parkin S, Crooks PA.

Acta Crystallogr E Crystallogr Commun. 2017 May 19;73(Pt 6):864-866. doi: 10.1107/S2056989017007277. eCollection 2017 Jun 1.


Succinamide derivatives of melampomagnolide B and their anti-cancer activities.

Janganati V, Ponder J, Thakkar S, Jordan CT, Crooks PA.

Bioorg Med Chem. 2017 Jul 15;25(14):3694-3705. doi: 10.1016/j.bmc.2017.05.008. Epub 2017 May 8.


Indole carboxylic acid esters of melampomagnolide B are potent anticancer agents against both hematological and solid tumor cells.

Bommagani S, Ponder J, Penthala NR, Janganati V, Jordan CT, Borrelli MJ, Crooks PA.

Eur J Med Chem. 2017 Aug 18;136:393-405. doi: 10.1016/j.ejmech.2017.05.031. Epub 2017 May 11.


Evaluation of Analgesia, Tolerance, and the Mechanism of Action of Morphine-6-O-Sulfate Across Multiple Pain Modalities in Sprague-Dawley Rats.

Yadlapalli JSK, Dogra N, Walbaum AW, Wessinger WD, Prather PL, Crooks PA, Dobretsov M.

Anesth Analg. 2017 Sep;125(3):1021-1031. doi: 10.1213/ANE.0000000000002006.


Synthesis and Evaluation of 2-Naphthaleno trans-Stilbenes and Cyanostilbenes as Anticancer Agents.

Madadi NR, Penthala NR, Ketkar A, Eoff RL, Trujullo-Alonso V, Guzman ML, Crooks PA.

Anticancer Agents Med Chem. 2018;18(4):556-564. doi: 10.2174/1871521409666170412115703.


Stability studies of potent opioid analgesic, morphine-6-O-sulfate in various buffers and biological matrices by HPLC-DAD analysis.

Yadlapalli JSK, Albayati ZAF, Penthala NR, Hendrickson HP, Crooks PA.

Biomed Chromatogr. 2017 Sep;31(9). doi: 10.1002/bmc.3957. Epub 2017 Mar 24.


Identification of a melampomagnolide B analog as a potential lead molecule for treatment of acute myelogenous leukemia.

Albayati ZAF, Janganati V, Chen Z, Ponder J, Breen PJ, Jordan CT, Crooks PA.

Bioorg Med Chem. 2017 Feb 1;25(3):1235-1241. doi: 10.1016/j.bmc.2016.12.036. Epub 2016 Dec 26.


GZ-793A inhibits the neurochemical effects of methamphetamine via a selective interaction with the vesicular monoamine transporter-2.

Nickell JR, Siripurapu KB, Horton DB, Zheng G, Crooks PA, Dwoskin LP.

Eur J Pharmacol. 2017 Jan 15;795:143-149. doi: 10.1016/j.ejphar.2016.12.016. Epub 2016 Dec 13.


Rational design of a parthenolide-based drug regimen that selectively eradicates acute myelogenous leukemia stem cells.

Pei S, Minhajuddin M, D'Alessandro A, Nemkov T, Stevens BM, Adane B, Khan N, Hagen FK, Yadav VK, De S, Ashton JM, Hansen KC, Gutman JA, Pollyea DA, Crooks PA, Smith C, Jordan CT.

J Biol Chem. 2016 Nov 25;291(48):25280. No abstract available.


N-[11CH3]Dimethylaminoparthenolide (DMAPT) uptake into orthotopic 9LSF glioblastoma tumors in the rat.

Penthala NR, Janganati V, Alpe TL, Apana SM, Berridge MS, Crooks PA, Borrelli MJ.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5883-5886. doi: 10.1016/j.bmcl.2016.11.015. Epub 2016 Nov 9.


Targeting Enox1 in tumor stroma increases the efficacy of fractionated radiotherapy.

Smith CA, Mont S, Traver G, Sekhar KR, Crooks PA, Freeman ML.

Oncotarget. 2016 Nov 22;7(47):77926-77936. doi: 10.18632/oncotarget.12845.


Synthesis of (2R,8' S,3' E)-δ-tocodienol, a tocoflexol family member designed to have a superior pharmacokinetic profile compared to δ-tocotrienol.

Liu X, Gujarathi S, Zhang X, Shao L, Boerma M, Compadre CM, Crooks PA, Hauer-Jensen M, Zhou D, Zheng G.

Tetrahedron. 2016 Jul;72(27-28):4001-4006. Epub 2016 May 12.


Antinociceptive effects of the 6-O-sulfate ester of morphine in normal and diabetic rats: Comparative role of mu- and delta-opioid receptors.

Yadlapalli JSK, Ford BM, Ketkar A, Wan A, Penthala NR, Eoff RL, Prather PL, Dobretsov M, Crooks PA.

Pharmacol Res. 2016 Nov;113(Pt A):335-347. doi: 10.1016/j.phrs.2016.09.012. Epub 2016 Sep 13.


Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies.

Laxmi SV, Anil P, Rajitha G, Rao AJ, Crooks PA, Rajitha B.

J Chem Biol. 2016 Jul 15;9(4):97-106. eCollection 2016 Oct.


Rational Design of a Parthenolide-based Drug Regimen That Selectively Eradicates Acute Myelogenous Leukemia Stem Cells.

Pei S, Minhajuddin M, D'Alessandro A, Nemkov T, Stevens BM, Adane B, Khan N, Hagen FK, Yadav VK, De S, Ashton JM, Hansen KC, Gutman JA, Pollyea DA, Crooks PA, Smith C, Jordan CT.

J Biol Chem. 2016 Oct 14;291(42):21984-22000. Epub 2016 Aug 29. Erratum in: J Biol Chem. 2016 Nov 25;291(48):25280.


Synthesis and in vitro evaluation of water-soluble 1,4-diphenethylpiperazine analogs as novel inhibitors of the vesicular monoamine transporter-2.

Nickell JR, Culver JP, Janganati V, Zheng G, Dwoskin LP, Crooks PA.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4441-4445. doi: 10.1016/j.bmcl.2016.08.001. Epub 2016 Aug 2.


Identification of resveratrol analogs as potent anti-dengue agents using a cell-based assay.

Han YS, Penthala NR, Oliveira M, Mesplède T, Xu H, Quan Y, Crooks PA, Wainberg MA.

J Med Virol. 2017 Mar;89(3):397-407. doi: 10.1002/jmv.24660. Epub 2016 Aug 22.


Crystal structures of (Z)-5-[2-(benzo[b]thio-phen-2-yl)-1-(3,5-di-meth-oxy-phen-yl)ethen-yl]-1H-tetra-zole and (Z)-5-[2-(benzo[b]thio-phen-3-yl)-1-(3,4,5-tri-meth-oxy-phen-yl)ethen-yl]-1H-tetra-zole.

Penthala NR, Yadlapalli JK, Parkin S, Crooks PA.

Acta Crystallogr E Crystallogr Commun. 2016 Apr 8;72(Pt 5):652-5. doi: 10.1107/S2056989016005600. eCollection 2016 May 1.


Persistent Activation of NF-κB in BRCA1-Deficient Mammary Progenitors Drives Aberrant Proliferation and Accumulation of DNA Damage.

Sau A, Lau R, Cabrita MA, Nolan E, Crooks PA, Visvader JE, Pratt MA.

Cell Stem Cell. 2016 Jul 7;19(1):52-65. doi: 10.1016/j.stem.2016.05.003. Epub 2016 Jun 9.


1,4-Diphenalkylpiperidines: A new scaffold for the design of potent inhibitors of the vesicular monoamine transporter-2.

Nickell JR, Culver JP, Janganati V, Zheng G, Dwoskin LP, Crooks PA.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):2997-3000. doi: 10.1016/j.bmcl.2016.05.025. Epub 2016 May 10.


Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2.

Joolakanti SR, Nickell JR, Janganati V, Zheng G, Dwoskin LP, Crooks PA.

Bioorg Med Chem Lett. 2016 May 15;26(10):2422-2427. doi: 10.1016/j.bmcl.2016.03.119. Epub 2016 Apr 1.


Synthesis and anti-cancer screening of novel heterocyclic-(2H)-1,2,3-triazoles as potential anti-cancer agents.

Penthala NR, Madhukuri L, Thakkar S, Madadi NR, Lamture G, Eoff RL, Crooks PA.

Medchemcomm. 2015 Aug 1;6(8):1535-1543. Epub 2015 Jun 30.


Dioxol and dihydrodioxin analogs of 2- and 3-phenylacetonitriles as potent anti-cancer agents with nanomolar activity against a variety of human cancer cells.

Madadi NR, Ketkar A, Penthala NR, Bostian AC, Eoff RL, Crooks PA.

Bioorg Med Chem Lett. 2016 May 1;26(9):2164-9. doi: 10.1016/j.bmcl.2016.03.068. Epub 2016 Mar 17.


Crystal structure of (E)-13-(pyrimidin-5-yl)parthenolide.

Bommagani S, Penthala NR, Parkin S, Crooks PA.

Acta Crystallogr E Crystallogr Commun. 2015 Nov 28;71(Pt 12):1536-8. doi: 10.1107/S2056989015021507. eCollection 2015 Dec 1.


Synthesis of Lobeline, Lobelane and their Analogues. A Review.

Zheng G, Crooks PA.

Org Prep Proced Int. 2015;47(5):317-337. Epub 2015 Aug 17. No abstract available.


In vivo targeting of leukemia stem cells by directing parthenolide-loaded nanoparticles to the bone marrow niche.

Zong H, Sen S, Zhang G, Mu C, Albayati ZF, Gorenstein DG, Liu X, Ferrari M, Crooks PA, Roboz GJ, Shen H, Guzman ML.

Leukemia. 2016 Jul;30(7):1582-6. doi: 10.1038/leu.2015.343. Epub 2015 Dec 16. No abstract available.

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