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Michelle Arkin, PhD

TitleAssociate Professor
SchoolUCSF School of Pharmacy
DepartmentPharmaceutical Chemistry
Address1700 4th St
San Francisco CA 94158
Phone415-514-4313
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    Collapse Biography 
    Collapse Awards and Honors
    Bryn Mawr College1989Shippen Science Scholarship
    Bryn Mawr College1989Dorothy Nepper Marshall Fellowship
    Armed Force1989Armed Forces Communications and Electronics Association Scholarship
    Bryn Mawr College1990  - 1991European Traveling Fellowship
    General Electric Foundation1991  - 1992Blodgett Fellowship
    National Science Foundation 1992  - 1995Predoctoral Fellowship
    National Institutes of Health 1995  - 1997National Institutes of Health Traineeship
    Daymon Runyon – Walter Winchell Cancer Research Foundation 1997  - 1999Daymon Runyon – Walter Winchell Cancer Research Foundation Postdoctoral Fellowship
    CHI2010Keynote address, Drug Discovery Chemistry, Protein-Protein Interactions
    International Society for Medicinal Chemistry (Berlin)2012Keynote address, European Federation of Medicinal Chemistry
    PPI-NET (London)2013Keynote address, PPI-NET
    SLAS2013Finalist, SLAS Innovation Award

    Collapse Overview 
    Collapse Overview
    Michelle’s lab develops innovative approaches to screen for chemical tools and drug leads, using biophysical approaches like fragment-based drug discovery and biological approaches including high-content imaging with primary cells and organisms. Our goal is to demonstrate ‘druggability’ of new target classes and to use our compounds to discover new targets for drug discovery. Areas of interest include protein-protein interactions, allosteric and scaffolding sites in enzymes, and orphan and neglected diseases. Michelle is Associate Director of the Small Molecule Discovery Center, a collaborative research and core lab that includes a high-throughput screening facility (smdc.ucsf.edu).


    Collapse Research 
    Collapse Research Activities and Funding
    A high content screen dissecting ciliogenesis and oncogenic Hedgehog signaling
    NIH/NCI R01CA181231Mar 23, 2016 - Feb 28, 2019
    Role: Co-Principal Investigator
    Screening for inhibitors of p300-mediated tau acetylation for Alzheimer's Disease
    NIH/NIA R21AG046526Jul 1, 2014 - Apr 30, 2016
    Role: Principal Investigator
    Translational Studies Linking Aging and Cancer
    NIH/NIA R01AG044515Sep 30, 2013 - Jun 30, 2018
    Role: Principal Investigator
    A novel high content screen for regulators of ciliogenesis and Hedgehog signaling
    NIH/NINDS R21NS066448Sep 27, 2010 - Aug 31, 2012
    Role: Principal Investigator
    An automated high throughput phenotypic screen for schistosomiasis drug discovery
    NIH/NIAID R01AI089896May 15, 2010 - Apr 30, 2014
    Role: Co-Principal Investigator
    2008 Biomolecular Interactions and Methods Gordon Research Conference
    NIH/NIGMS R13GM083379Jan 1, 2008 - Dec 31, 2008
    Role: Principal Investigator

    Collapse ORNG Applications 
    Collapse Websites
    Collapse In The News
    Collapse Global Health

    Collapse Bibliographic 
    Collapse Publications
    Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Researchers can login to make corrections and additions, or contact us for help.
    List All   |   Timeline
    1. Carlson HK, Mullan MR, Mosqueda LA, Chen S, Arkin MR, Coates JD. High-Throughput Screening To Identify Potent and Specific Inhibitors of Microbial Sulfate Reduction. Environ Sci Technol. 2017 Jun 20; 51(12):7278-7285. PMID: 28492331.
      View in: PubMed
    2. 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. A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site. Org Biomol Chem. 2017 May 16; 15(19):4096-4114. PMID: 28352916.
      View in: PubMed
    3. Pappalardo Z, Chopra DG, Hennings TG, Richards H, Choe J, Yang K, Baeyens L, Ang K, Chen S, Arkin M, German MS, McManus MT, Ku GM. A Whole-Genome RNA Interference Screen Reveals a Role for Spry2 in Insulin Transcription and the Unfolded Protein Response. Diabetes. 2017 Jun; 66(6):1703-1712. PMID: 28246293.
      View in: PubMed
    4. Hallenbeck KK, Turner DM, Renslo AR, Arkin MR. Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery. Curr Top Med Chem. 2017; 17(1):4-15. PMID: 27449257.
      View in: PubMed
    5. Visperas PR, Wilson CG, Winger JA, Yan Q, Lin K, Arkin MR, Weiss A, Kuriyan J. Identification of Inhibitors of the Association of ZAP-70 with the T Cell Receptor by High-Throughput Screen. SLAS Discov. 2017 Mar; 22(3):324-331. PMID: 27932698.
      View in: PubMed
    6. 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. A High-Content Larval Zebrafish Brain Imaging Method for Small Molecule Drug Discovery. PLoS One. 2016; 11(10):e0164645. PMID: 27732643.
      View in: PubMed
    7. 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. Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6a branch. Elife. 2016 Jul 20; 5. PMID: 27435960; PMCID: PMC4954757.
    8. Bulfer SL, Chou TF, Arkin M, et al. p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions. ACS Chem Biol. 2016 Aug 19; 11(8):2112-6. PMID: 27267671.
      View in: PubMed
    9. 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. 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition. Science. 2016 Feb 19; 351(6275):871-5. PMID: 26822609.
      View in: PubMed
    10. 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. Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway. ACS Med Chem Lett. 2016 Feb 11; 7(2):182-7. PMID: 26985295; PMCID: PMC4753542 [Available on 02/11/17].
    11. Suzawa M, Miranda DA, Ramos KA, Ang KK, Faivre EJ, Wilson CG, Caboni L, Arkin M, Kim YS, Fletterick RJ, Diaz A, Schneekloth JS, Ingraham HA. A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver. Elife. 2015 Dec 11; 4. PMID: 26653140; PMCID: PMC4749390.
    12. Visscher M, Arkin MR, Dansen TB. Covalent targeting of acquired cysteines in cancer. Curr Opin Chem Biol. 2016 Feb; 30:61-67. PMID: 26629855; PMCID: PMC4731306 [Available on 02/01/17].
    13. 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. Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97. ACS Med Chem Lett. 2015 Dec 10; 6(12):1225-30. PMID: 26713109; PMCID: PMC4677369 [Available on 12/10/16].
    14. Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS. Tackling reproducibility in academic preclinical drug discovery. Nat Rev Drug Discov. 2015 11; 14(11):733-4. PMID: 26388229.
      View in: PubMed
    15. 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. Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease. PLoS Pathog. 2015 Jul; 11(7):e1005058. PMID: 26186534; PMCID: PMC4506092.
    16. Ekins S, Lage de Siqueira-Neto J, McCall LI, Sarker M, Yadav M, Ponder EL, Kallel EA, Kellar D, Chen S, Arkin M, Bunin BA, McKerrow JH, Talcott C. Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery. PLoS Negl Trop Dis. 2015; 9(6):e0003878. PMID: 26114876; PMCID: PMC4482694.
    17. Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin MR, Ellman JA, Renslo AR. Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease. Bioorg Med Chem Lett. 2015 Nov 01; 25(21):4834-7. PMID: 26144347; PMCID: PMC4737481 [Available on 11/01/16].
    18. 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. Altered cofactor regulation with disease-associated p97/VCP mutations. Proc Natl Acad Sci U S A. 2015 Apr 07; 112(14):E1705-14. PMID: 25775548; PMCID: PMC4394316.
    19. Tran K, Arkin MR, Beal PA. Tethering in RNA: an RNA-binding fragment discovery tool. Molecules. 2015 Mar 04; 20(3):4148-61. PMID: 25749683; PMCID: PMC4760646.
    20. Bulman CA, Bidlow CM, Lustigman S, Cho-Ngwa F, Williams D, Rascón AA, 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. Repurposing auranofin as a lead candidate for treatment of lymphatic filariasis and onchocerciasis. PLoS Negl Trop Dis. 2015 Feb; 9(2):e0003534. PMID: 25700363; PMCID: PMC4336141.
    21. Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin MR, Kelly MJ. A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP. J Biomol Screen. 2015 Jul; 20(6):788-800. PMID: 25690569.
      View in: PubMed
    22. Pfaff SJ, Chimenti MS, Kelly MJ, Arkin MR. Biophysical methods for identifying fragment-based inhibitors of protein-protein interactions. Methods Mol Biol. 2015; 1278:587-613. PMID: 25859978.
      View in: PubMed
    23. Visperas PR, Winger JA, Horton TM, Shah NH, Aum DJ, Tao A, Barros T, Yan Q, Wilson CG, Arkin MR, Weiss A, Kuriyan J. Modification by covalent reaction or oxidation of cysteine residues in the tandem-SH2 domains of ZAP-70 and Syk can block phosphopeptide binding. Biochem J. 2015 Jan 01; 465(1):149-61. PMID: 25287889; PMCID: PMC4410814.
    24. Rettenmaier TJ, Sadowsky JD, Thomsen ND, Chen SC, Doak AK, Arkin MR, Wells JA. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30; 111(52):18590-5. PMID: 25518860; PMCID: PMC4284534.
    25. Neitz RJ, Chen S, Supek F, Yeh V, Kellar D, Gut J, Bryant C, Gallardo-Godoy A, Molteni V, Roach SL, Chatterjee AK, Robertson S, Renslo AR, Arkin M, Glynne R, McKerrow J, Siqueira-Neto JL. Lead identification to clinical candidate selection: drugs for Chagas disease. J Biomol Screen. 2015 Jan; 20(1):101-11. PMID: 25281737.
      View in: PubMed
    26. Arkin MR, Tang Y, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. Chem Biol. 2014 Sep 18; 21(9):1102-14. PMID: 25237857; PMCID: PMC4179228.
    27. Dar RD, Hosmane NN, Arkin MR, Siliciano RF, Weinberger LS. Screening for noise in gene expression identifies drug synergies. Science. 2014 Jun 20; 344(6190):1392-6. PMID: 24903562; PMCID: PMC4122234.
    28. Chou TF, Bulfer SL, Weihl CC, Li K, Lis LG, Walters MA, Schoenen FJ, Lin HJ, Deshaies RJ, Arkin MR. Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains. J Mol Biol. 2014 Jul 29; 426(15):2886-99. PMID: 24878061; PMCID: PMC4102644.
    29. Arkin MR, Ang KK, Chen S, Davies J, Merron C, Tang Y, Wilson CG, Renslo AR. UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area. Comb Chem High Throughput Screen. 2014 May; 17(4):333-42. PMID: 24661212.
      View in: PubMed
    30. Flygare JA, Arkin MR. Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases. Curr Top Med Chem. 2014; 14(3):319-25. PMID: 24283214.
      View in: PubMed
    31. Wilson CG, Arkin MR. Probing structural adaptivity at PPI interfaces with small molecules. Drug Discov Today Technol. 2013 Dec; 10(4):e501-8. PMID: 24451641.
      View in: PubMed
    32. 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. Tailoring small molecules for an allosteric site on procaspase-6. ChemMedChem. 2014 Jan; 9(1):73-7, 2. PMID: 24259468.
      View in: PubMed
    33. Slusher BS, Conn PJ, Frye S, Glicksman M, Arkin M. Bringing together the academic drug discovery community. Nat Rev Drug Discov. 2013 Nov; 12(11):811-2. PMID: 24172316; PMCID: PMC4076044.
    34. 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. Imaging-based chemical screening reveals activity-dependent neural differentiation of pluripotent stem cells. Elife. 2013 Sep 10; 2:e00508. PMID: 24040509; PMCID: PMC3771564.
    35. Bagriantsev SN, Ang KH, Gallardo-Godoy A, Clark KA, Arkin MR, Renslo AR, Minor DL. A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels. ACS Chem Biol. 2013 Aug 16; 8(8):1841-51. PMID: 23738709; PMCID: PMC3747594.
    36. 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. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013 May 28; 2:e00498. PMID: 23741617; PMCID: PMC3667625.
    37. 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. Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target. Beilstein J Org Chem. 2013; 9:15-25. PMID: 23400640; PMCID: PMC3566858.
    38. 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. Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6. PLoS One. 2012; 7(12):e50864. PMID: 23227217; PMCID: PMC3515450.
    39. Wu VM, Chen SC, Arkin MR, Reiter JF. Small molecule inhibitors of Smoothened ciliary localization and ciliogenesis. Proc Natl Acad Sci U S A. 2012 Aug 21; 109(34):13644-9. PMID: 22864913; PMCID: PMC3427101.
    40. 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. Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51. PLoS Negl Trop Dis. 2012; 6(7):e1736. PMID: 22860142; PMCID: PMC3409115.
    41. Pu M, Hayashi T, Cottam H, Mulvaney J, Arkin M, Corr M, Carson D, Messer K. Analysis of high-throughput screening assays using cluster enrichment. Stat Med. 2012 Dec 30; 31(30):4175-89. PMID: 22763983; PMCID: PMC3635947.
    42. Rogers KE, Keränen H, Durrant JD, Ratnam J, Doak A, Arkin MR, McCammon JA. Novel cruzain inhibitors for the treatment of Chagas' disease. Chem Biol Drug Des. 2012 Sep; 80(3):398-405. PMID: 22613098; PMCID: PMC3503458.
    43. 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. A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target. Nat Med. 2012 Jun; 18(6):956-60. PMID: 22610278; PMCID: PMC3411919.
    44. 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. Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye. ACS Med Chem Lett. 2012 Mar 08; 3(3):203-6. PMID: 24900456; PMCID: PMC4025648.
    45. Lee H, Moody-Davis A, Saha U, Suzuki BM, Asarnow D, Chen S, Arkin M, Caffrey CR, Singh R. Quantification and clustering of phenotypic screening data using time-series analysis for chemotherapy of schistosomiasis. BMC Genomics. 2012; 13 Suppl 1:S4. PMID: 22369037; PMCID: PMC3471343.
    46. Tang Y, Wells JA, Arkin MR. Structural and enzymatic insights into caspase-2 protein substrate recognition and catalysis. J Biol Chem. 2011 Sep 30; 286(39):34147-54. PMID: 21828056; PMCID: PMC3190824.
    47. De Muylder G, Ang KK, Chen S, Arkin MR, Engel JC, McKerrow JH. A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit. PLoS Negl Trop Dis. 2011 Jul; 5(7):e1253. PMID: 21811648; PMCID: PMC3139667.
    48. 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. Mining a cathepsin inhibitor library for new antiparasitic drug leads. PLoS Negl Trop Dis. 2011 May 03; 5(5):e1023. PMID: 21572521; PMCID: PMC3086806.
    49. Ben Khalaf N, De Muylder G, Ratnam J, Kean-Hooi Ang K, Arkin M, McKerrow J, Chenik M. A high-throughput turbidometric assay for screening inhibitors of Leishmania major protein disulfide isomerase. J Biomol Screen. 2011 Jun; 16(5):545-51. PMID: 21441416.
      View in: PubMed
    50. Gut J, Ang KK, Legac J, Arkin MR, Rosenthal PJ, McKerrow JH. An image-based assay for high throughput screening of Giardia lamblia. J Microbiol Methods. 2011 Mar; 84(3):398-405. PMID: 21262276.
      View in: PubMed
    51. Wilson CG, Arkin MR. Small-molecule inhibitors of IL-2/IL-2R: lessons learned and applied. Curr Top Microbiol Immunol. 2011; 348:25-59. PMID: 20703966.
      View in: PubMed
    52. 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. Structure-activity relationship (SAR) of the a-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists. Bioorg Med Chem Lett. 2011 Jan 01; 21(1):307-10. PMID: 21109434.
      View in: PubMed
    53. 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. Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists. Bioorg Med Chem Lett. 2010 Sep 01; 20(17):5269-73. PMID: 20655213.
      View in: PubMed
    54. Engel JC, Ang KK, Chen S, Arkin MR, McKerrow JH, Doyle PS. Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. Antimicrob Agents Chemother. 2010 Aug; 54(8):3326-34. PMID: 20547819; PMCID: PMC2916317.
    55. Hawtin RE, Stockett DE, Byl JA, McDowell RS, Nguyen T, Arkin MR, Conroy A, Yang W, Osheroff N, Fox JA. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One. 2010 Apr 15; 5(4):e10186. PMID: 20419121; PMCID: PMC2855444.
    56. Mott BT, Ferreira RS, Simeonov A, Jadhav A, Ang KK, Leister W, Shen M, Silveira JT, Doyle PS, Arkin MR, McKerrow JH, Inglese J, Austin CP, Thomas CJ, Shoichet BK, Maloney DJ. Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem. 2010 Jan 14; 53(1):52-60. PMID: 19908842; PMCID: PMC2804034.
    57. Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin MR, McKerrow JH, Brinen LS, Renslo AR. Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. Bioorg Med Chem Lett. 2009 Nov 01; 19(21):6218-21. PMID: 19773167; PMCID: PMC3760505.
    58. McKerrow JH, Doyle PS, Engel JC, Podust LM, Robertson SA, Ferreira R, Saxton T, Arkin M, Kerr ID, Brinen LS, Craik CS. Two approaches to discovering and developing new drugs for Chagas disease. Mem Inst Oswaldo Cruz. 2009 Jul; 104 Suppl 1:263-9. PMID: 19753483; PMCID: PMC4156466.
    59. Arkin MR, Whitty A. The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions. Curr Opin Chem Biol. 2009 Jun; 13(3):284-90. PMID: 19553156.
      View in: PubMed
    60. Rubio BK, Tenney K, Ang KH, Abdulla M, Arkin M, McKerrow JH, Crews P. The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness. J Nat Prod. 2009 Feb 27; 72(2):218-22. PMID: 19159277; PMCID: PMC2880650.
    61. Conroy A, Stockett DE, Walker D, Arkin MR, Hoch U, Fox JA, Hawtin RE. SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep; 64(4):723-32. PMID: 19169685.
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    62. Arkin M, Moasser MM. HER-2-directed, small-molecule antagonists. Curr Opin Investig Drugs. 2008 Dec; 9(12):1264-76. PMID: 19037833; PMCID: PMC3031872.
    63. Choong IC, Serafimova I, Fan J, Stockett D, Chan E, Cheeti S, Lu Y, Fahr B, Pham P, Arkin MR, Walker DH, Hoch U. A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. Bioorg Med Chem Lett. 2008 Nov 01; 18(21):5763-5. PMID: 18842409.
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    64. Arkin M. Protein-protein interactions and cancer: small molecules going in for the kill. Curr Opin Chem Biol. 2005 Jun; 9(3):317-24. PMID: 15939335.
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    65. Waal ND, Yang W, Oslob JD, Arkin MR, Hyde J, Lu W, McDowell RS, Yu CH, Raimundo BC. Identification of nonpeptidic small-molecule inhibitors of interleukin-2. Bioorg Med Chem Lett. 2005 Feb 15; 15(4):983-7. PMID: 15686897.
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    66. Raimundo BC, Oslob JD, Braisted AC, Hyde J, McDowell RS, Randal M, Waal ND, Wilkinson J, Yu CH, Arkin MR. Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions. J Med Chem. 2004 Jun 03; 47(12):3111-30. PMID: 15163192.
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    67. Arkin MR, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov. 2004 Apr; 3(4):301-17. PMID: 15060526.
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    68. Hyde J, Braisted AC, Randal M, Arkin MR. Discovery and characterization of cooperative ligand binding in the adaptive region of interleukin-2. Biochemistry. 2003 Jun 03; 42(21):6475-83. PMID: 12767230.
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    69. Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC. Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 2003 Apr 02; 125(13):3714-5. PMID: 12656598.
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    70. Arkin MR, Randal M, DeLano WL, Hyde J, Luong TN, Oslob JD, Raphael DR, Taylor L, Wang J, McDowell RS, Wells JA, Braisted AC. Binding of small molecules to an adaptive protein-protein interface. Proc Natl Acad Sci U S A. 2003 Feb 18; 100(4):1603-8. PMID: 12582206; PMCID: PMC149879.
    71. Wells J, Arkin M, Braisted A, DeLano W, McDowell B, Oslob J, Raimundo B, Randal M. Drug discovery at signaling interfaces. Ernst Schering Res Found Workshop. 2003; (42):19-27. PMID: 12664533.
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    72. Arkin M, Lear JD. A new data analysis method to determine binding constants of small molecules to proteins using equilibrium analytical ultracentrifugation with absorption optics. Anal Biochem. 2001 Dec 01; 299(1):98-107. PMID: 11726190.
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    73. Arkin MR, Wells JA. Probing the importance of second sphere residues in an esterolytic antibody by phage display. J Mol Biol. 1998 Dec 11; 284(4):1083-94. PMID: 9837728.
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