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Items: 1 to 50 of 81

1.

Protein and chemical determinants of BL-1249 action and selectivity for K2P channels.

Pope L, Arrigoni C, Lou H, Bryant C, Gallardo-Godoy A, Renslo AR, Minor DL.

ACS Chem Neurosci. 2018 Aug 8. doi: 10.1021/acschemneuro.8b00337. [Epub ahead of print]

PMID:
30089357
2.

Antibacterial Spectrum of a Tetrazole-Based Reversible Inhibitor of Serine β-Lactamases.

Pemberton OA, Zhang X, Nichols DA, DeFrees K, Jaishankar P, Bonnet R, Adams J, Shaw LN, Renslo AR, Chen Y.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e02563-17. doi: 10.1128/AAC.02563-17. Print 2018 Aug.

PMID:
29844038
3.

Structure of the nucleotide exchange factor eIF2B reveals mechanism of memory-enhancing molecule.

Tsai JC, Miller-Vedam LE, Anand AA, Jaishankar P, Nguyen HC, Renslo AR, Frost A, Walter P.

Science. 2018 Mar 30;359(6383). pii: eaaq0939. doi: 10.1126/science.aaq0939.

PMID:
29599213
4.

Toward a Ferrous Iron-Cleavable Linker for Antibody-Drug Conjugates.

Spangler B, Kline T, Hanson J, Li X, Zhou S, Wells JA, Sato AK, Renslo AR.

Mol Pharm. 2018 May 7;15(5):2054-2059. doi: 10.1021/acs.molpharmaceut.8b00242. Epub 2018 Mar 23.

PMID:
29569925
5.

cAMP signaling regulates DNA hydroxymethylation by augmenting the intracellular labile ferrous iron pool.

Camarena V, Sant DW, Huff TC, Mustafi S, Muir RK, Aron AT, Chang CJ, Renslo AR, Monje PV, Wang G.

Elife. 2017 Dec 14;6. pii: e29750. doi: 10.7554/eLife.29750.

6.

In vivo bioluminescence imaging of labile iron accumulation in a murine model of Acinetobacter baumannii infection.

Aron AT, Heffern MC, Lonergan ZR, Vander Wal MN, Blank BR, Spangler B, Zhang Y, Park HM, Stahl A, Renslo AR, Skaar EP, Chang CJ.

Proc Natl Acad Sci U S A. 2017 Nov 28;114(48):12669-12674. doi: 10.1073/pnas.1708747114. Epub 2017 Nov 14.

7.

USP7 small-molecule inhibitors interfere with ubiquitin binding.

Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE.

Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18.

PMID:
29045385
8.

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM.

Cell Chem Biol. 2017 Dec 21;24(12):1455-1466.e14. doi: 10.1016/j.chembiol.2017.08.025. Epub 2017 Oct 12.

PMID:
29033317
9.

A Liquid Chromatography/Mass Spectrometry Method for Screening Disulfide Tethering Fragments.

Hallenbeck KK, Davies JL, Merron C, Ogden P, Sijbesma E, Ottmann C, Renslo AR, Wilson C, Arkin MR.

SLAS Discov. 2018 Feb;23(2):183-192. doi: 10.1177/2472555217732072. Epub 2017 Sep 25.

PMID:
28945980
10.

Allosteric Inhibitors, Crystallography, and Comparative Analysis Reveal Network of Coordinated Movement across Human Herpesvirus Proteases.

Acker TM, Gable JE, Bohn MF, Jaishankar P, Thompson MC, Fraser JS, Renslo AR, Craik CS.

J Am Chem Soc. 2017 Aug 30;139(34):11650-11653. doi: 10.1021/jacs.7b04030. Epub 2017 Aug 17.

11.

Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.

Blank BR, Gut J, Rosenthal PJ, Renslo AR.

J Med Chem. 2017 Jul 27;60(14):6400-6407. doi: 10.1021/acs.jmedchem.7b00699. Epub 2017 Jul 10.

12.

Identification and Optimization of Thienopyridine Carboxamides as Inhibitors of HIV Regulatory Complexes.

Nakamura RL, Burlingame MA, Yang S, Crosby DC, Talbot DJ, Chui K, Frankel AD, Renslo AR.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e02366-16. doi: 10.1128/AAC.02366-16. Print 2017 Jul.

13.

A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models.

Spangler B, Fontaine SD, Shi Y, Sambucetti L, Mattis AN, Hann B, Wells JA, Renslo AR.

J Med Chem. 2016 Dec 22;59(24):11161-11170. doi: 10.1021/acs.jmedchem.6b01470. Epub 2016 Dec 12.

14.

Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery.

Hallenbeck KK, Turner DM, Renslo AR, Arkin MR.

Curr Top Med Chem. 2017;17(1):4-15. Review.

15.

Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch.

Gallagher CM, Garri C, Cain EL, Ang KK, Wilson CG, Chen S, Hearn BR, Jaishankar P, Aranda-Diaz A, Arkin MR, Renslo AR, Walter P.

Elife. 2016 Jul 20;5. pii: e11878. doi: 10.7554/eLife.11878.

16.

A reactivity-based probe of the intracellular labile ferrous iron pool.

Spangler B, Morgan CW, Fontaine SD, Vander Wal MN, Chang CJ, Wells JA, Renslo AR.

Nat Chem Biol. 2016 Sep;12(9):680-5. doi: 10.1038/nchembio.2116. Epub 2016 Jul 4.

17.

Structure-Activity Studies of Bis-O-Arylglycolamides: Inhibitors of the Integrated Stress Response.

Hearn BR, Jaishankar P, Sidrauski C, Tsai JC, Vedantham P, Fontaine SD, Walter P, Renslo AR.

ChemMedChem. 2016 Apr 19;11(8):870-80. doi: 10.1002/cmdc.201500483. Epub 2016 Jan 20.

PMID:
26789650
18.

Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.

Lauterwasser EM, Fontaine SD, Li H, Gut J, Katneni K, Charman SA, Rosenthal PJ, Bogyo M, Renslo AR.

ACS Med Chem Lett. 2015 Oct 2;6(11):1145-9. doi: 10.1021/acsmedchemlett.5b00296. eCollection 2015 Nov 12.

19.

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations.

Mott BT, Eastman RT, Guha R, Sherlach KS, Siriwardana A, Shinn P, McKnight C, Michael S, Lacerda-Queiroz N, Patel PR, Khine P, Sun H, Kasbekar M, Aghdam N, Fontaine SD, Liu D, Mierzwa T, Mathews-Griner LA, Ferrer M, Renslo AR, Inglese J, Yuan J, Roepe PD, Su XZ, Thomas CJ.

Sci Rep. 2015 Sep 25;5:13891. doi: 10.1038/srep13891.

20.

Antileishmanial Activity of Disulfiram and Thiuram Disulfide Analogs in an Ex Vivo Model System Is Selectively Enhanced by the Addition of Divalent Metal Ions.

Peniche AG, Renslo AR, Melby PC, Travi BL.

Antimicrob Agents Chemother. 2015 Oct;59(10):6463-70. doi: 10.1128/AAC.05131-14. Epub 2015 Aug 3.

21.

Different 2-Aminothiazole Therapeutics Produce Distinct Patterns of Scrapie Prion Neuropathology in Mouse Brains.

Giles K, Berry DB, Condello C, Hawley RC, Gallardo-Godoy A, Bryant C, Oehler A, Elepano M, Bhardwaj S, Patel S, Silber BM, Guan S, DeArmond SJ, Renslo AR, Prusiner SB.

J Pharmacol Exp Ther. 2015 Oct;355(1):2-12. doi: 10.1124/jpet.115.224659. Epub 2015 Jul 29.

22.

Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease.

Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin MR, Ellman JA, Renslo AR.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4834-4837. doi: 10.1016/j.bmcl.2015.06.066. Epub 2015 Jun 23.

23.

Ligand-Induced Proton Transfer and Low-Barrier Hydrogen Bond Revealed by X-ray Crystallography.

Nichols DA, Hargis JC, Sanishvili R, Jaishankar P, Defrees K, Smith EW, Wang KK, Prati F, Renslo AR, Woodcock HL, Chen Y.

J Am Chem Soc. 2015 Jul 1;137(25):8086-95. doi: 10.1021/jacs.5b00749. Epub 2015 Jun 22.

24.

Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response.

Sidrauski C, Tsai JC, Kampmann M, Hearn BR, Vedantham P, Jaishankar P, Sokabe M, Mendez AS, Newton BW, Tang EL, Verschueren E, Johnson JR, Krogan NJ, Fraser CS, Weissman JS, Renslo AR, Walter P.

Elife. 2015 Apr 15;4:e07314. doi: 10.7554/eLife.07314.

25.

A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP.

Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin MR, Kelly MJ.

J Biomol Screen. 2015 Jul;20(6):788-800. doi: 10.1177/1087057115570550. Epub 2015 Feb 17.

PMID:
25690569
26.

Protease inhibitors targeting coronavirus and filovirus entry.

Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R Jr, Nunneley JW, Barnard D, Pöhlmann S, McKerrow JH, Renslo AR, Simmons G.

Antiviral Res. 2015 Apr;116:76-84. doi: 10.1016/j.antiviral.2015.01.011. Epub 2015 Feb 7.

27.

Simple plate-based, parallel synthesis of disulfide fragments using the CuAAC click reaction.

Turner DM, Tom CT, Renslo AR.

ACS Comb Sci. 2014 Dec 8;16(12):661-4. doi: 10.1021/co500132q. Epub 2014 Nov 12.

PMID:
25353066
28.

Efficient and stereocontrolled synthesis of 1,2,4-trioxolanes useful for ferrous iron-dependent drug delivery.

Fontaine SD, DiPasquale AG, Renslo AR.

Org Lett. 2014 Nov 7;16(21):5776-9. doi: 10.1021/ol5028392. Epub 2014 Oct 21.

29.

Drug delivery to the malaria parasite using an arterolane-like scaffold.

Fontaine SD, Spangler B, Gut J, Lauterwasser EM, Rosenthal PJ, Renslo AR.

ChemMedChem. 2015 Jan;10(1):47-51. doi: 10.1002/cmdc.201402362. Epub 2014 Oct 14.

30.

Lead identification to clinical candidate selection: drugs for Chagas disease.

Neitz RJ, Chen S, Supek F, Yeh V, Kellar D, Gut J, Bryant C, Gallardo-Godoy A, Molteni V, Roach SL, Khare S, Stinson M, Chatterjee AK, Robertson S, Renslo AR, Arkin M, Glynne R, McKerrow J, Siqueira-Neto JL.

J Biomol Screen. 2015 Jan;20(1):101-11. doi: 10.1177/1087057114553103. Epub 2014 Oct 3. Erratum in: J Biomol Screen. 2015 Aug;20(7):927.

PMID:
25281737
31.

Broad-spectrum allosteric inhibition of herpesvirus proteases.

Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS.

Biochemistry. 2014 Jul 22;53(28):4648-60. doi: 10.1021/bi5003234. Epub 2014 Jul 11.

32.

Hsp90 inhibitors as new leads to target parasitic diarrheal diseases.

Debnath A, Shahinas D, Bryant C, Hirata K, Miyamoto Y, Hwang G, Gut J, Renslo AR, Pillai DR, Eckmann L, Reed SL, McKerrow JH.

Antimicrob Agents Chemother. 2014 Jul;58(7):4138-44. doi: 10.1128/AAC.02576-14. Epub 2014 May 12.

33.

Antimalarial Drug Discovery: From Quinine to the Dream of Eradication.

Renslo AR.

ACS Med Chem Lett. 2013 Dec 12;4(12):1126-1128.

34.

Successes and challenges in phenotype-based lead discovery for prion diseases.

Ghaemmaghami S, Russo M, Renslo AR.

J Med Chem. 2014 Aug 28;57(16):6919-29. doi: 10.1021/jm5001425. Epub 2014 Apr 24. Review.

35.

UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area.

Arkin MR, Ang KK, Chen S, Davies J, Merron C, Tang Y, Wilson CG, Renslo AR.

Comb Chem High Throughput Screen. 2014 May;17(4):333-42.

PMID:
24661212
36.

Fragment-based inhibitor discovery against β-lactamase.

Nichols DA, Renslo AR, Chen Y.

Future Med Chem. 2014 Mar;6(4):413-27. doi: 10.4155/fmc.14.10. Review.

37.

Novel compounds lowering the cellular isoform of the human prion protein in cultured human cells.

Silber BM, Gever JR, Rao S, Li Z, Renslo AR, Widjaja K, Wong C, Giles K, Freyman Y, Elepano M, Irwin JJ, Jacobson MP, Prusiner SB.

Bioorg Med Chem. 2014 Mar 15;22(6):1960-72. doi: 10.1016/j.bmc.2014.01.001. Epub 2014 Jan 9.

38.

Tailoring small molecules for an allosteric site on procaspase-6.

Murray J, Giannetti AM, Steffek M, Gibbons P, Hearn BR, Cohen F, Tam C, Pozniak C, Bravo B, Lewcock J, Jaishankar P, Ly CQ, Zhao X, Tang Y, Chugha P, Arkin MR, Flygare J, Renslo AR.

ChemMedChem. 2014 Jan;9(1):73-7, 2. doi: 10.1002/cmdc.201300424. Epub 2013 Nov 20.

PMID:
24259468
39.

Modulating caspase activity: beyond the active site.

Murray J, Renslo AR.

Curr Opin Struct Biol. 2013 Dec;23(6):812-9. doi: 10.1016/j.sbi.2013.10.002. Epub 2013 Nov 8. Review.

PMID:
24215810
40.

Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.

Silber BM, Gever JR, Li Z, Gallardo-Godoy A, Renslo AR, Widjaja K, Irwin JJ, Rao S, Jacobson MP, Ghaemmaghami S, Prusiner SB.

Bioorg Med Chem. 2013 Dec 15;21(24):7999-8012. doi: 10.1016/j.bmc.2013.09.022. Epub 2013 Sep 18.

41.

Ferrous iron-dependent drug delivery enables controlled and selective release of therapeutic agents in vivo.

Deu E, Chen IT, Lauterwasser EM, Valderramos J, Li H, Edgington LE, Renslo AR, Bogyo M.

Proc Natl Acad Sci U S A. 2013 Nov 5;110(45):18244-9. doi: 10.1073/pnas.1312782110. Epub 2013 Oct 21.

42.

Drug resistance confounding prion therapeutics.

Berry DB, Lu D, Geva M, Watts JC, Bhardwaj S, Oehler A, Renslo AR, DeArmond SJ, Prusiner SB, Giles K.

Proc Natl Acad Sci U S A. 2013 Oct 29;110(44):E4160-9. doi: 10.1073/pnas.1317164110. Epub 2013 Oct 15.

43.

Development of an ex vivo lymph node explant model for identification of novel molecules active against Leishmania major.

Peniche AG, Osorio Y, Renslo AR, Frantz DE, Melby PC, Travi BL.

Antimicrob Agents Chemother. 2014;58(1):78-87. doi: 10.1128/AAC.00887-13. Epub 2013 Oct 14.

44.

Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice.

Lu D, Giles K, Li Z, Rao S, Dolghih E, Gever JR, Geva M, Elepano ML, Oehler A, Bryant C, Renslo AR, Jacobson MP, Dearmond SJ, Silber BM, Prusiner SB.

J Pharmacol Exp Ther. 2013 Nov;347(2):325-38. doi: 10.1124/jpet.113.205799. Epub 2013 Aug 21.

45.

Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected].

Nishino M, Choy JW, Gushwa NN, Oses-Prieto JA, Koupparis K, Burlingame AL, Renslo AR, McKerrow JH, Taunton J.

Elife. 2013 Jul 9;2:e00712. doi: 10.7554/eLife.00712. Erratum in: Elife. 2013;e01214.

46.

Pharmacological brake-release of mRNA translation enhances cognitive memory.

Sidrauski C, Acosta-Alvear D, Khoutorsky A, Vedantham P, Hearn BR, Li H, Gamache K, Gallagher CM, Ang KK, Wilson C, Okreglak V, Ashkenazi A, Hann B, Nader K, Arkin MR, Renslo AR, Sonenberg N, Walter P.

Elife. 2013 May 28;2:e00498. doi: 10.7554/eLife.00498.

47.

A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels.

Bagriantsev SN, Ang KH, Gallardo-Godoy A, Clark KA, Arkin MR, Renslo AR, Minor DL Jr.

ACS Chem Biol. 2013 Aug 16;8(8):1841-51. doi: 10.1021/cb400289x. Epub 2013 Jun 17.

48.

2-Aminothiazoles with improved pharmacotherapeutic properties for treatment of prion disease.

Li Z, Silber BM, Rao S, Gever JR, Bryant C, Gallardo-Godoy A, Dolghih E, Widjaja K, Elepano M, Jacobson MP, Prusiner SB, Renslo AR.

ChemMedChem. 2013 May;8(5):847-57. doi: 10.1002/cmdc.201300007. Epub 2013 Mar 18.

49.

Pharmacokinetics and metabolism of 2-aminothiazoles with antiprion activity in mice.

Silber BM, Rao S, Fife KL, Gallardo-Godoy A, Renslo AR, Dalvie DK, Giles K, Freyman Y, Elepano M, Gever JR, Li Z, Jacobson MP, Huang Y, Benet LZ, Prusiner SB.

Pharm Res. 2013 Apr;30(4):932-50. doi: 10.1007/s11095-012-0912-4. Epub 2013 Feb 16.

50.

Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target.

Choy JW, Bryant C, Calvet CM, Doyle PS, Gunatilleke SS, Leung SS, Ang KK, Chen S, Gut J, Oses-Prieto JA, Johnston JB, Arkin MR, Burlingame AL, Taunton J, Jacobson MP, McKerrow JM, Podust LM, Renslo AR.

Beilstein J Org Chem. 2013;9:15-25. doi: 10.3762/bjoc.9.3. Epub 2013 Jan 4.

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