Loading...

Michelle Arkin, PhD

TitleAssociate Professor
SchoolUCSF School of Pharmacy
DepartmentPharmaceutical Chemistry
Address1700 4th St
San Francisco CA 94158
Phone415-514-4313
vCardDownload vCard

    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: 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. 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 Feb 28. PMID: 28246293.
      View in: PubMed
    2. Visperas PR, Wilson CG, Winger JA, Yan Q, Lin K, Arkin M, Weiss A, Kuriyan J. Identification of Inhibitors of the Association of ZAP-70 with the T Cell Receptor by High-Throughput Screen. J Biomol Screen. 2016 Dec 08. PMID: 27932698.
      View in: PubMed
    3. 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
    4. Gallagher CM, Garri C, Cain EL, Ang KK, Wilson CG, Chen S, Hearn BR, Jaishankar P, Aranda-Diaz A, Arkin M, Renslo AR, Walter P. Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6a branch. Elife. 2016; 5. PMID: 27435960.
      View in: PubMed
    5. Hallenbeck KK, Turner DM, Renslo AR, Arkin M. Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery. Curr Top Med Chem. 2016 Jul 19. PMID: 27449257.
      View in: PubMed
    6. Bulfer SL, Chou TF, Arkin M, et al. p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein-Protein Interactions. ACS Chem Biol. 2016 Jun 13. PMID: 27267671.
      View in: PubMed
    7. 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
    8. 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 M, 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.
      View in: PubMed
    9. 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; 4. PMID: 26653140.
      View in: PubMed
    10. Visscher M, Arkin M, Dansen TB. Covalent targeting of acquired cysteines in cancer. Curr Opin Chem Biol. 2016 Feb; 30:61-7. PMID: 26629855.
      View in: PubMed
    11. Alverez C, Arkin M, 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.
      View in: PubMed
    12. Frye SV, Arkin M, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS. Tackling reproducibility in academic preclinical drug discovery. Nat Rev Drug Discov. 2015 Nov; 14(11):733-4. PMID: 26388229.
      View in: PubMed
    13. Khare S, Roach SL, Barnes SW, Hoepfner D, Walker JR, Chatterjee AK, Neitz RJ, Arkin M, 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.
    14. 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 Jun; 9(6):e0003878. PMID: 26114876; PMCID: PMC4482694.
    15. Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin M, Ellman JA, Renslo AR. Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease. Bioorg Med Chem Lett. 2015 Nov 1; 25(21):4834-7. PMID: 26144347.
      View in: PubMed
    16. 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 M, Wang Y, Chou TF. Altered cofactor regulation with disease-associated p97/VCP mutations. Proc Natl Acad Sci U S A. 2015 Apr 7; 112(14):E1705-14. PMID: 25775548; PMCID: PMC4394316.
    17. Tran K, Arkin M, Beal PA. Tethering in RNA: an RNA-binding fragment discovery tool. Molecules. 2015; 20(3):4148-61. PMID: 25749683.
      View in: PubMed
    18. 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.
    19. Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin M, 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
    20. Pfaff SJ, Chimenti MS, Kelly MJ, Arkin M. Biophysical methods for identifying fragment-based inhibitors of protein-protein interactions. Methods Mol Biol. 2015; 1278:587-613. PMID: 25859978.
      View in: PubMed
    21. Visperas PR, Winger JA, Horton TM, Shah NH, Aum DJ, Tao A, Barros T, Yan Q, Wilson CG, Arkin M, 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 1; 465(1):149-61. PMID: 25287889; PMCID: PMC4410814.
    22. Rettenmaier TJ, Sadowsky JD, Thomsen ND, Chen SC, Doak AK, Arkin M, 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.
    23. 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
    24. Arkin M, 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.
    25. Dar RD, Hosmane NN, Arkin M, 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.
    26. Chou TF, Bulfer SL, Weihl CC, Li K, Lis LG, Walters MA, Schoenen FJ, Lin HJ, Deshaies RJ, Arkin M. 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.
    27. Arkin M, 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
    28. Flygare JA, Arkin M. Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases. Curr Top Med Chem. 2014; 14(3):319-25. PMID: 24283214.
      View in: PubMed
    29. Wilson CG, Arkin M. Probing structural adaptivity at PPI interfaces with small molecules. Drug Discov Today Technol. 2013 Dec; 10(4):e501-8. PMID: 24451641.
      View in: PubMed
    30. 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 M, 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
    31. 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.
    32. Sun Y, Dong Z, Jin T, Ang KH, Huang M, Haston KM, Peng J, Zhong TP, Finkbeiner S, Weiss WA, Arkin M, Jan LY, Guo S. Imaging-based chemical screening reveals activity-dependent neural differentiation of pluripotent stem cells. Elife. 2013; 2:e00508. PMID: 24040509; PMCID: PMC3771564.
    33. Bagriantsev SN, Ang KH, Gallardo-Godoy A, Clark KA, Arkin M, 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.
    34. 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 M, Renslo AR, Sonenberg N, Walter P. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013; 2:e00498. PMID: 23741617; PMCID: PMC3667625.
    35. Choy JW, Bryant C, Calvet CM, Doyle PS, Gunatilleke SS, Leung SS, Ang KK, Chen S, Gut J, Oses-Prieto JA, Johnston JB, Arkin M, 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.
    36. 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 M. Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6. PLoS One. 2012; 7(12):e50864. PMID: 23227217; PMCID: PMC3515450.
    37. Wu VM, Chen SC, Arkin M, 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.
    38. Gunatilleke SS, Calvet CM, Johnston JB, Chen CK, Erenburg G, Gut J, Engel JC, Ang KK, Mulvaney J, Chen S, Arkin M, McKerrow JH, Podust LM. Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51. PLoS Negl Trop Dis. 2012; 6(7):e1736. PMID: 22860142; PMCID: PMC3409115.
    39. 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.
    40. Rogers KE, Keränen H, Durrant JD, Ratnam J, Doak A, Arkin M, 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.
    41. 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 M, 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.
    42. Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J, Arkin M, 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 8; 3(3):203-6. PMID: 24900456; PMCID: PMC4025648.
    43. 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.
    44. Tang Y, Wells JA, Arkin M. 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.
    45. De Muylder G, Ang KK, Chen S, Arkin M, 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.
    46. Ang KK, Ratnam J, Gut J, Legac J, Hansell E, Mackey ZB, Skrzypczynska KM, Debnath A, Engel JC, Rosenthal PJ, McKerrow JH, Arkin M, Renslo AR. Mining a cathepsin inhibitor library for new antiparasitic drug leads. PLoS Negl Trop Dis. 2011; 5(5):e1023. PMID: 21572521; PMCID: PMC3086806.
    47. 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
    48. Gut J, Ang KK, Legac J, Arkin M, 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
    49. Wilson CG, Arkin M. 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
    50. Zhong M, Hanan EJ, Shen W, Bui M, Arkin M, 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 1; 21(1):307-10. PMID: 21109434.
      View in: PubMed
    51. Zhong M, Shen W, Barr KJ, Arbitrario JP, Arkin M, 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 1; 20(17):5269-73. PMID: 20655213.
      View in: PubMed
    52. Engel JC, Ang KK, Chen S, Arkin M, 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.
    53. Hawtin RE, Stockett DE, Byl JA, McDowell RS, Nguyen T, Arkin M, Conroy A, Yang W, Osheroff N, Fox JA. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One. 2010; 5(4):e10186. PMID: 20419121; PMCID: PMC2855444.
    54. Mott BT, Ferreira RS, Simeonov A, Jadhav A, Ang KK, Leister W, Shen M, Silveira JT, Doyle PS, Arkin M, 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.
    55. Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin M, 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 1; 19(21):6218-21. PMID: 19773167; PMCID: PMC3760505.
    56. 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.
    57. Arkin M, 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
    58. 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.
    59. Conroy A, Stockett DE, Walker D, Arkin M, 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.
      View in: PubMed
    60. Arkin M, Moasser MM. HER-2-directed, small-molecule antagonists. Curr Opin Investig Drugs. 2008 Dec; 9(12):1264-76. PMID: 19037833; PMCID: PMC3031872.
    61. Choong IC, Serafimova I, Fan J, Stockett D, Chan E, Cheeti S, Lu Y, Fahr B, Pham P, Arkin M, Walker DH, Hoch U. A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. Bioorg Med Chem Lett. 2008 Nov 1; 18(21):5763-5. PMID: 18842409.
      View in: PubMed
    62. 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.
      View in: PubMed
    63. Waal ND, Yang W, Oslob JD, Arkin M, 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.
      View in: PubMed
    64. Raimundo BC, Oslob JD, Braisted AC, Hyde J, McDowell RS, Randal M, Waal ND, Wilkinson J, Yu CH, Arkin M. 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 3; 47(12):3111-30. PMID: 15163192.
      View in: PubMed
    65. Arkin M, 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.
      View in: PubMed
    66. Hyde J, Braisted AC, Randal M, Arkin M. Discovery and characterization of cooperative ligand binding in the adaptive region of interleukin-2. Biochemistry. 2003 Jun 3; 42(21):6475-83. PMID: 12767230.
      View in: PubMed
    67. Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin M, Raimundo BC. Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 2003 Apr 2; 125(13):3714-5. PMID: 12656598.
      View in: PubMed
    68. Arkin M, 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.
    69. 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.
      View in: PubMed
    70. 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 1; 299(1):98-107. PMID: 11726190.
      View in: PubMed
    71. Arkin M, 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.
      View in: PubMed
    72. Arkin M, Stemp ED, Pulver SC, Barton JK. Long-range oxidation of guanine by Ru(III) in duplex DNA. Chem Biol. 1997 May; 4(5):389-400. PMID: 9195873.
      View in: PubMed
    73. Arkin M, Stemp ED, Holmlin RE, Barton JK, Hörmann A, Olson EJ, Barbara PF. Rates of DNA-mediated electron transfer between metallointercalators. Science. 1996 Jul 26; 273(5274):475-80. PMID: 8662532.
      View in: PubMed
    74. Murphy CJ, Arkin M, Ghatlia ND, Bossmann S, Turro NJ, Barton JK. Fast photoinduced electron transfer through DNA intercalation. Proc Natl Acad Sci U S A. 1994 Jun 7; 91(12):5315-9. PMID: 8202486; PMCID: PMC43985.
    75. Murphy CJ, Arkin M, Jenkins Y, Ghatlia ND, Bossmann SH, Turro NJ, Barton JK. Long-range photoinduced electron transfer through a DNA helix. Science. 1993 Nov 12; 262(5136):1025-9. PMID: 7802858.
      View in: PubMed
    Michelle's Networks
    Concepts
    Derived automatically from this person's publications.
    _
    Co-Authors
    People in Profiles who have published with this person.
    _
    Related Authors
    People who share related concepts with this person.
    _
    Back to TOP