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Items: 1 to 50 of 68

1.

Octopamine-signaling in the metazoan pathogen, Schistosoma mansoni: localization, small-molecule screening and opportunities for drug development.

El-Sakkary N, Chen S, Arkin MR, Caffrey CR, Ribeiro P.

Dis Model Mech. 2018 Jul 9. pii: dmm.033563. doi: 10.1242/dmm.033563. [Epub ahead of print]

2.

Small-Molecule Screening for Genetic Diseases.

Markossian S, Ang KK, Wilson CG, Arkin MR.

Annu Rev Genomics Hum Genet. 2018 May 23. doi: 10.1146/annurev-genom-083117-021452. [Epub ahead of print]

PMID:
29799800
3.

Inhibition of Protein-Protein Interactions: Cell-Based Assays.

Wade M, Méndez J, Coussens NP, Arkin MR, Glicksman MA.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Hass JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2017 Nov 20.

4.

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
5.

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
6.

High-Throughput Screening To Identify Potent and Specific Inhibitors of Microbial Sulfate Reduction.

Carlson HK, Mullan MR, Mosqueda LA, Chen S, Arkin MR, Coates JD.

Environ Sci Technol. 2017 Jun 20;51(12):7278-7285. doi: 10.1021/acs.est.7b00686. Epub 2017 May 26.

PMID:
28492331
7.

A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site.

Burnett JC, Lim C, Peyser BD, Samankumara LP, Kovaliov M, Colombo R, Bulfer SL, LaPorte MG, Hermone AR, McGrath CF, Arkin MR, Gussio R, Huryn DM, Wipf P.

Org Biomol Chem. 2017 May 16;15(19):4096-4114. doi: 10.1039/c7ob00526a.

8.

Identification of Inhibitors of the Association of ZAP-70 with the T Cell Receptor by High-Throughput Screen.

Visperas PR, Wilson CG, Winger JA, Yan Q, Lin K, Arkin MR, Weiss A, Kuriyan J.

SLAS Discov. 2017 Mar;22(3):324-331. doi: 10.1177/1087057116681407. Epub 2016 Dec 13.

9.

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.

10.

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.

11.

p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions.

Bulfer SL, Chou TF, Arkin MR.

ACS Chem Biol. 2016 Aug 19;11(8):2112-6. doi: 10.1021/acschembio.6b00350. Epub 2016 Jun 13.

12.

Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.

Alverez C, Bulfer SL, Chakrasali R, Chimenti MS, Deshaies RJ, Green N, Kelly M, LaPorte MG, Lewis TS, Liang M, Moore WJ, Neitz RJ, Peshkov VA, Walters MA, Zhang F, Arkin MR, Wipf P, Huryn DM.

ACS Med Chem Lett. 2015 Dec 22;7(2):182-7. doi: 10.1021/acsmedchemlett.5b00396. eCollection 2016 Feb 11.

13.

Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

Alverez C, Arkin MR, Bulfer SL, Colombo R, Kovaliov M, LaPorte MG, Lim C, Liang M, Moore WJ, Neitz RJ, Yan Y, Yue Z, Huryn DM, Wipf P.

ACS Med Chem Lett. 2015 Oct 23;6(12):1225-30. doi: 10.1021/acsmedchemlett.5b00364. eCollection 2015 Dec 10.

14.

A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver.

Suzawa M, Miranda DA, Ramos KA, Ang KK, Faivre EJ, Wilson CG, Caboni L, Arkin MR, Kim YS, Fletterick RJ, Diaz A, Schneekloth JS, Ingraham HA.

Elife. 2015 Dec 11;4. pii: e09003. doi: 10.7554/eLife.09003.

15.

Covalent targeting of acquired cysteines in cancer.

Visscher M, Arkin MR, Dansen TB.

Curr Opin Chem Biol. 2016 Feb;30:61-67. doi: 10.1016/j.cbpa.2015.11.004. Epub 2015 Nov 28. Review.

16.

Tackling reproducibility in academic preclinical drug discovery.

Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS.

Nat Rev Drug Discov. 2015 Nov;14(11):733-4. doi: 10.1038/nrd4737. Epub 2015 Sep 21.

PMID:
26388229
17.

Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease.

Khare S, Roach SL, Barnes SW, Hoepfner D, Walker JR, Chatterjee AK, Neitz RJ, Arkin MR, McNamara CW, Ballard J, Lai Y, Fu Y, Molteni V, Yeh V, McKerrow JH, Glynne RJ, Supek F.

PLoS Pathog. 2015 Jul 17;11(7):e1005058. doi: 10.1371/journal.ppat.1005058. eCollection 2015 Jul.

18.

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.

19.

Biophysical methods for identifying fragment-based inhibitors of protein-protein interactions.

Pfaff SJ, Chimenti MS, Kelly MJ, Arkin MR.

Methods Mol Biol. 2015;1278:587-613. doi: 10.1007/978-1-4939-2425-7_39.

PMID:
25859978
20.

Altered cofactor regulation with disease-associated p97/VCP mutations.

Zhang X, Gui L, Zhang X, Bulfer SL, Sanghez V, Wong DE, Lee Y, Lehmann L, Lee JS, Shih PY, Lin HJ, Iacovino M, Weihl CC, Arkin MR, Wang Y, Chou TF.

Proc Natl Acad Sci U S A. 2015 Apr 7;112(14):E1705-14. doi: 10.1073/pnas.1418820112. Epub 2015 Mar 16.

21.

Tethering in RNA: an RNA-binding fragment discovery tool.

Tran K, Arkin MR, Beal PA.

Molecules. 2015 Mar 4;20(3):4148-61. doi: 10.3390/molecules20034148.

22.

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
23.

A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1.

Rettenmaier TJ, Sadowsky JD, Thomsen ND, Chen SC, Doak AK, Arkin MR, Wells JA.

Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5. doi: 10.1073/pnas.1415365112. Epub 2014 Dec 17.

24.

Modification by covalent reaction or oxidation of cysteine residues in the tandem-SH2 domains of ZAP-70 and Syk can block phosphopeptide binding.

Visperas PR, Winger JA, Horton TM, Shah NH, Aum DJ, Tao A, Barros T, Yan Q, Wilson CG, Arkin MR, Weiss A, Kuriyan J.

Biochem J. 2015 Jan 1;465(1):149-61. doi: 10.1042/BJ20140793.

25.

Small-molecule inhibitors of protein-protein interactions: progressing toward the reality.

Arkin MR, Tang Y, Wells JA.

Chem Biol. 2014 Sep 18;21(9):1102-14. doi: 10.1016/j.chembiol.2014.09.001. Review.

26.

Screening for noise in gene expression identifies drug synergies.

Dar RD, Hosmane NN, Arkin MR, Siliciano RF, Weinberger LS.

Science. 2014 Jun 20;344(6190):1392-6. doi: 10.1126/science.1250220. Epub 2014 Jun 5.

27.

Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains.

Chou TF, Bulfer SL, Weihl CC, Li K, Lis LG, Walters MA, Schoenen FJ, Lin HJ, Deshaies RJ, Arkin MR.

J Mol Biol. 2014 Jul 29;426(15):2886-99. doi: 10.1016/j.jmb.2014.05.022. Epub 2014 May 27.

28.

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
29.

Probing structural adaptivity at PPI interfaces with small molecules.

Wilson CG, Arkin MR.

Drug Discov Today Technol. 2013 Dec;10(4):e501-8. doi: 10.1016/j.ddtec.2012.10.009. Review.

PMID:
24451641
30.

Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases.

Flygare JA, Arkin MR.

Curr Top Med Chem. 2014;14(3):319-25. Review.

PMID:
24283214
31.

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
32.

Imaging-based chemical screening reveals activity-dependent neural differentiation of pluripotent stem cells.

Sun Y, Dong Z, Jin T, Ang KH, Huang M, Haston KM, Peng J, Zhong TP, Finkbeiner S, Weiss WA, Arkin MR, Jan LY, Guo S.

Elife. 2013 Sep 10;2:e00508. doi: 10.7554/eLife.00508.

33.

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.

34.

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.

35.

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.

36.

Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6.

Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, Tang Y, Zhao X, Lewcock JW, Renslo AR, Flygare J, Arkin MR.

PLoS One. 2012;7(12):e50864. doi: 10.1371/journal.pone.0050864. Epub 2012 Dec 5.

37.

FLIPR™ Assays for GPCR and Ion Channel Targets.

Arkin MR, Connor PR, Emkey R, Garbison KE, Heinz BA, Wiernicki TR, Johnston PA, Kandasamy RA, Rankl NB, Sittampalam S.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Hass JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2012 Oct 1].

38.

Inhibition of Protein-Protein Interactions: Non-Cellular Assay Formats.

Arkin MR, Glicksman MA, Fu H, Havel JJ, Du Y.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Hass JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 Mar 18 [updated 2012 Oct 1].

39.

Small molecule inhibitors of Smoothened ciliary localization and ciliogenesis.

Wu VM, Chen SC, Arkin MR, Reiter JF.

Proc Natl Acad Sci U S A. 2012 Aug 21;109(34):13644-9. doi: 10.1073/pnas.1207170109. Epub 2012 Aug 3.

40.

Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51.

Gunatilleke SS, Calvet CM, Johnston JB, Chen CK, Erenburg G, Gut J, Engel JC, Ang KK, Mulvaney J, Chen S, Arkin MR, McKerrow JH, Podust LM.

PLoS Negl Trop Dis. 2012;6(7):e1736. doi: 10.1371/journal.pntd.0001736. Epub 2012 Jul 31.

41.

Novel cruzain inhibitors for the treatment of Chagas' disease.

Rogers KE, Keränen H, Durrant JD, Ratnam J, Doak A, Arkin MR, McCammon JA.

Chem Biol Drug Des. 2012 Sep;80(3):398-405. doi: 10.1111/j.1747-0285.2012.01416.x. Epub 2012 Jun 27.

42.

A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target.

Debnath A, Parsonage D, Andrade RM, He C, Cobo ER, Hirata K, Chen S, García-Rivera G, Orozco E, Martínez MB, Gunatilleke SS, Barrios AM, Arkin MR, Poole LB, McKerrow JH, Reed SL.

Nat Med. 2012 Jun;18(6):956-60. doi: 10.1038/nm.2758.

43.

Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.

Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J, Arkin MR, Evanchik MJ, Flanagan WM, Hoch U, Hyde J, Prabhu S, Silverman JA, Wright J.

ACS Med Chem Lett. 2012 Jan 31;3(3):203-6. doi: 10.1021/ml2002482. eCollection 2012 Mar 8.

44.

Structural and enzymatic insights into caspase-2 protein substrate recognition and catalysis.

Tang Y, Wells JA, Arkin MR.

J Biol Chem. 2011 Sep 30;286(39):34147-54. doi: 10.1074/jbc.M111.247627. Epub 2011 Aug 2.

45.

A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit.

De Muylder G, Ang KK, Chen S, Arkin MR, Engel JC, McKerrow JH.

PLoS Negl Trop Dis. 2011 Jul;5(7):e1253. doi: 10.1371/journal.pntd.0001253. Epub 2011 Jul 19.

46.

Mining a cathepsin inhibitor library for new antiparasitic drug leads.

Ang KK, Ratnam J, Gut J, Legac J, Hansell E, Mackey ZB, Skrzypczynska KM, Debnath A, Engel JC, Rosenthal PJ, McKerrow JH, Arkin MR, Renslo AR.

PLoS Negl Trop Dis. 2011 May 3;5(5):e1023. doi: 10.1371/journal.pntd.0001023.

47.

An image-based assay for high throughput screening of Giardia lamblia.

Gut J, Ang KK, Legac J, Arkin MR, Rosenthal PJ, McKerrow JH.

J Microbiol Methods. 2011 Mar;84(3):398-405. doi: 10.1016/j.mimet.2010.12.026. Epub 2011 Jan 22.

PMID:
21262276
48.

Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.

Zhong M, Hanan EJ, Shen W, Bui M, Arkin MR, Barr KJ, Evanchik MJ, Hoch U, Hyde J, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):307-10. doi: 10.1016/j.bmcl.2010.11.014. Epub 2010 Nov 5.

PMID:
21109434
49.

Small-molecule inhibitors of IL-2/IL-2R: lessons learned and applied.

Wilson CG, Arkin MR.

Curr Top Microbiol Immunol. 2011;348:25-59. doi: 10.1007/82_2010_93.

PMID:
20703966
50.

Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.

Zhong M, Shen W, Barr KJ, Arbitrario JP, Arkin MR, Bui M, Chen T, Cunningham BC, Evanchik MJ, Hanan EJ, Hoch U, Huen K, Hyde J, Kumer JL, Lac T, Lawrence CE, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5269-73. doi: 10.1016/j.bmcl.2010.06.145. Epub 2010 Jul 23.

PMID:
20655213

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