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Items: 1 to 50 of 111

1.

A Cell-Based Renilla Luminescence Reporter Plasmid Assay for High-Throughput Screening to Identify Novel FDA-Approved Drug Inhibitors of HPV-16 Infection.

Walhart T, Isaacson-Wechsler E, Ang KH, Arkin M, Tugizov S, Palefsky JM.

SLAS Discov. 2019 Jul 30:2472555219860771. doi: 10.1177/2472555219860771. [Epub ahead of print]

PMID:
31361520
2.

Artificial cysteine-lipases with high activity and altered catalytic mechanism created by laboratory evolution.

Cen Y, Singh W, Arkin M, Moody TS, Huang M, Zhou J, Wu Q, Reetz MT.

Nat Commun. 2019 Jul 19;10(1):3198. doi: 10.1038/s41467-019-11155-3.

3.

Specificity for latent C termini links the E3 ubiquitin ligase CHIP to caspases.

Ravalin M, Theofilas P, Basu K, Opoku-Nsiah KA, Assimon VA, Medina-Cleghorn D, Chen YF, Bohn MF, Arkin M, Grinberg LT, Craik CS, Gestwicki JE.

Nat Chem Biol. 2019 Aug;15(8):786-794. doi: 10.1038/s41589-019-0322-6. Epub 2019 Jul 18.

PMID:
31320752
4.

Light-Driven Kinetic Resolution of α-Functionalized Carboxylic Acids Enabled by an Engineered Fatty Acid Photodecarboxylase.

Xu J, Hu Y, Fan J, Arkin M, Li D, Peng Y, Xu W, Lin X, Wu Q.

Angew Chem Int Ed Engl. 2019 Jun 17;58(25):8474-8478. doi: 10.1002/anie.201903165. Epub 2019 May 14.

PMID:
31033108
5.

Modulating protein-protein interaction networks in protein homeostasis.

Zhong M, Lee GM, Sijbesma E, Ottmann C, Arkin MR.

Curr Opin Chem Biol. 2019 Jun;50:55-65. doi: 10.1016/j.cbpa.2019.02.012. Epub 2019 Mar 23. Review.

PMID:
30913483
6.

Site-Directed Fragment-Based Screening for the Discovery of Protein-Protein Interaction Stabilizers.

Sijbesma E, Hallenbeck KK, Leysen S, de Vink PJ, Skóra L, Jahnke W, Brunsveld L, Arkin MR, Ottmann C.

J Am Chem Soc. 2019 Feb 27;141(8):3524-3531. doi: 10.1021/jacs.8b11658. Epub 2019 Feb 19.

PMID:
30707565
7.

Guidelines for DNA recombination and repair studies: Mechanistic assays of DNA repair processes.

Klein HL, Ang KKH, Arkin MR, Beckwitt EC, Chang YH, Fan J, Kwon Y, Morten MJ, Mukherjee S, Pambos OJ, El Sayyed H, Thrall ES, Vieira-da-Rocha JP, Wang Q, Wang S, Yeh HY, Biteen JS, Chi P, Heyer WD, Kapanidis AN, Loparo JJ, Strick TR, Sung P, Van Houten B, Niu H, Rothenberg E.

Microb Cell. 2019 Jan 7;6(1):65-101. doi: 10.15698/mic2019.01.665. Review.

8.

Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97.

LaPorte MG, Burnett JC, Colombo R, Bulfer SL, Alverez C, Chou TF, Neitz RJ, Green N, Moore WJ, Yue Z, Li S, Arkin MR, Wipf P, Huryn DM.

ACS Med Chem Lett. 2018 Sep 18;9(11):1075-1081. doi: 10.1021/acsmedchemlett.8b00372. eCollection 2018 Nov 8.

9.

Functional Assessment of 2,177 U.S. and International Drugs Identifies the Quinoline Nitroxoline as a Potent Amoebicidal Agent against the Pathogen Balamuthia mandrillaris.

Laurie MT, White CV, Retallack H, Wu W, Moser MS, Sakanari JA, Ang K, Wilson C, Arkin MR, DeRisi JL.

MBio. 2018 Oct 30;9(5). pii: e02051-18. doi: 10.1128/mBio.02051-18.

10.

Fibrin-targeting immunotherapy protects against neuroinflammation and neurodegeneration.

Ryu JK, Rafalski VA, Meyer-Franke A, Adams RA, Poda SB, Rios Coronado PE, Pedersen LØ, Menon V, Baeten KM, Sikorski SL, Bedard C, Hanspers K, Bardehle S, Mendiola AS, Davalos D, Machado MR, Chan JP, Plastira I, Petersen MA, Pfaff SJ, Ang KK, Hallenbeck KK, Syme C, Hakozaki H, Ellisman MH, Swanson RA, Zamvil SS, Arkin MR, Zorn SH, Pico AR, Mucke L, Freedman SB, Stavenhagen JB, Nelson RB, Akassoglou K.

Nat Immunol. 2018 Nov;19(11):1212-1223. doi: 10.1038/s41590-018-0232-x. Epub 2018 Oct 15.

11.

A Genetic Interaction Map of Insulin Production Identifies Mfi as an Inhibitor of Mitochondrial Fission.

Lee J, Pappalardo Z, Chopra DG, Hennings TG, Vaughn I, Lan C, Choe JJ, Ang K, Chen S, Arkin M, McManus MT, German MS, Ku GM.

Endocrinology. 2018 Sep 1;159(9):3321-3330. doi: 10.1210/en.2018-00426.

12.

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 30;11(7). pii: dmm033563. doi: 10.1242/dmm.033563.

13.

Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery.

Coussens NP, Sittampalam GS, Guha R, Brimacombe K, Grossman A, Chung TDY, Weidner JR, Riss T, Trask OJ, Auld D, Dahlin JL, Devanaryan V, Foley TL, McGee J, Kahl SD, Kales SC, Arkin M, Baell J, Bejcek B, Gal-Edd N, Glicksman M, Haas JV, Iversen PW, Hoeppner M, Lathrop S, Sayers E, Liu H, Trawick B, McVey J, Lemmon VP, Li Z, McManus O, Minor L, Napper A, Wildey MJ, Pacifici R, Chin WW, Xia M, Xu X, Lal-Nag M, Hall MD, Michael S, Inglese J, Simeonov A, Austin CP.

Clin Transl Sci. 2018 Sep;11(5):461-470. doi: 10.1111/cts.12570. Epub 2018 Jul 24. Review.

14.

Small-Molecule Screening for Genetic Diseases.

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

Annu Rev Genomics Hum Genet. 2018 Aug 31;19:263-288. doi: 10.1146/annurev-genom-083117-021452. Epub 2018 May 23. Review.

PMID:
29799800
15.

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

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

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, 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.

16.

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
17.

Probing the correlation of neuronal loss, neurofibrillary tangles, and cell death markers across the Alzheimer's disease Braak stages: a quantitative study in humans.

Theofilas P, Ehrenberg AJ, Nguy A, Thackrey JM, Dunlop S, Mejia MB, Alho AT, Paraizo Leite RE, Rodriguez RD, Suemoto CK, Nascimento CF, Chin M, Medina-Cleghorn D, Cuervo AM, Arkin M, Seeley WW, Miller BL, Nitrini R, Pasqualucci CA, Filho WJ, Rueb U, Neuhaus J, Heinsen H, Grinberg LT.

Neurobiol Aging. 2018 Jan;61:1-12. doi: 10.1016/j.neurobiolaging.2017.09.007. Epub 2017 Sep 20.

18.

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.

19.

Chemical Biology as a Driver of Innovation in Cancer Research and Drug Discovery.

Kostic M, Arkin M.

Cell Chem Biol. 2017 Sep 21;24(9):1057. doi: 10.1016/j.chembiol.2017.09.002. No abstract available.

20.

Joining Forces: The Chemical Biology-Medicinal Chemistry Continuum.

Plowright AT, Ottmann C, Arkin M, Auberson YP, Timmerman H, Waldmann H.

Cell Chem Biol. 2017 Sep 21;24(9):1058-1065. doi: 10.1016/j.chembiol.2017.05.019. Epub 2017 Jun 8. Review.

21.

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
22.

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.

23.

A Whole-Genome RNA Interference Screen Reveals a Role for Spry2 in Insulin Transcription and the Unfolded Protein Response.

Pappalardo Z, Gambhir Chopra D, Hennings TG, Richards H, Choe J, Yang K, Baeyens L, Ang K, Chen S, Arkin M, German MS, McManus MT, Ku GM.

Diabetes. 2017 Jun;66(6):1703-1712. doi: 10.2337/db16-0962. Epub 2017 Feb 28.

24.

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.

25.

A High-Content Larval Zebrafish Brain Imaging Method for Small Molecule Drug Discovery.

Liu H, Chen S, Huang K, Kim J, Mo H, Iovine R, Gendre J, Pascal P, Li Q, Sun Y, Dong Z, Arkin M, Guo S, Huang B.

PLoS One. 2016 Oct 12;11(10):e0164645. doi: 10.1371/journal.pone.0164645. eCollection 2016.

26.

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.

27.

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.

28.

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.

29.

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.

30.

Interview with Michelle Arkin, PhD.

Arkin M.

Assay Drug Dev Technol. 2016 Jan-Feb;14(1):14-8. doi: 10.1089/adt.2016.29033.mar. No abstract available.

PMID:
26866749
31.

2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition.

Banerjee S, Bartesaghi A, Merk A, Rao P, Bulfer SL, Yan Y, Green N, Mroczkowski B, Neitz RJ, Wipf P, Falconieri V, Deshaies RJ, Milne JL, Huryn D, Arkin M, Subramaniam S.

Science. 2016 Feb 19;351(6275):871-5. doi: 10.1126/science.aad7974. Epub 2016 Jan 28.

32.

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.

33.

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.

34.

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.

35.

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
36.

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.

37.

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.

38.

Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery.

Ekins S, de Siqueira-Neto JL, McCall LI, Sarker M, Yadav M, Ponder EL, Kallel EA, Kellar D, Chen S, Arkin M, Bunin BA, McKerrow JH, Talcott C.

PLoS Negl Trop Dis. 2015 Jun 26;9(6):e0003878. doi: 10.1371/journal.pntd.0003878. eCollection 2015.

39.

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
40.

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.

41.

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.

42.

Repurposing auranofin as a lead candidate for treatment of lymphatic filariasis and onchocerciasis.

Bulman CA, Bidlow CM, Lustigman S, Cho-Ngwa F, Williams D, Rascón AA Jr, Tricoche N, Samje M, Bell A, Suzuki B, Lim KC, Supakorndej N, Supakorndej P, Wolfe AR, Knudsen GM, Chen S, Wilson C, Ang KH, Arkin M, Gut J, Franklin C, Marcellino C, McKerrow JH, Debnath A, Sakanari JA.

PLoS Negl Trop Dis. 2015 Feb 20;9(2):e0003534. doi: 10.1371/journal.pntd.0003534. eCollection 2015 Feb.

43.

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
44.

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.

45.

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.

46.

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
47.

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.

48.

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.

49.

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.

50.

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

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