Research Summary

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 co-Director of the Small Molecule Discovery Center, a collaborative research and core lab that includes a high-throughput screening facility and medicinal chemistry (smdc.ucsf.edu).

Education

1990, Bryn Mawr College, Bryn Mawr, PA, B.A., Chemistry
1997, California Institute of Technology, Pasadena, CA, Ph.D., Chemistry
1999, Genentech, Inc, South San Francisco, CA and Sunesis Pharmaceuticals, Redwood City, CA, Postdoctoral fellowship, Protein Engineering

Honors & Awards

  • 1990    
    European Traveling Fellowship    Bryn Mawr College
  • 1991    
    Blodgett Fellowship    General Electric Foundation
  • 1992    
    Predoctoral Fellowship    National Science Foundation
  • 1995    
    Traineeship    National Institutes of Health
  • 1997    
    Postdoctoral Fellowship    Damon Runyon Cancer Research Foundation 
  • 2014    
    Finalist    SLAS Innovation Award
  • 2018    
    Breakthrough Chemical Biology Awardee    Ono Pharma Foundation     
  • 2018    
    Webster-Sibilsky Keynote Lecture    University of Illinois, Chicago    
  • 2019    
    Briggs Lecture    University of Texas Health San Antonio    
  • 2021    
    Fellow    Society for Laboratory Automation and Screening    
  • 2024    
    Cope Scholar    American Chemical Society, Organic Division    
  • 2024    
    Gordon Hammes Lectureship    American Chemical Society, Biochemisty    

Selected Publications

  1. Arkin MR, Dickinson BC, Winter GE. Mapping and Rewiring Biology via Proximity Induction. Acc Chem Res. 2026 Feb 17; 59(4):541-542. View on PubMed
  2. Konstantinidou M, Vickery HR, Pennings MAM, Virta JM, Luo SY, Visser EJ, Bannier SD, Srikanth M, Cismoski SZ, Young LC, van den Oetelaar MCM, McCormick F, Ottmann C, Brunsveld L, Arkin MR. Modulation of the 14-3-3σ/C-RAF "Auto"inhibited Complex by Molecular Glues. J Am Chem Soc. 2026 Feb 11; 148(5):4951-4965. View on PubMed
  3. Twigg DG, Arai K, Arkin MR, Erlanson DA, de Esch IJP, Farkaš B, Fesik SW, Jahnke W, Johnson CN, Schroeder M. Correction to "Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective". J Med Chem. 2026 Feb 12; 69(3):3639-3640. View on PubMed
  4. Twigg DG, Arai K, Arkin MR, Erlanson DA, de Esch IJP, Farkaš B, Fesik SW, Jahnke W, Johnson CN, Schroeder M. Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective. J Med Chem. 2025 Dec 11; 68(23):24830-24847. View on PubMed
  5. Konstantinidou M, Virta JM, Arkin MR. Stabilization of Native Protein-Protein Interactions with Molecular Glues: A 14-3-3 Case Study. Acc Chem Res. 2025 Sep 16; 58(18):2840-2851. View on PubMed
  6. Konstantinidou M, Vickery HR, Pennings MAM, Virta JM, Visser EJ, Bannier SD, Srikanth M, Cismoski SZ, Young LC, van den Oetelaar MCM, McCormick F, Ottmann C, Brunsveld L, Arkin MR. Modulation of the 14-3-3σ/C-RAF "auto"inhibited complex by molecular glues. bioRxiv. 2025 Jul 31. View on PubMed
  7. Konstantinidou M, Zingiridis M, Pennings MAM, Fragkiadakis M, Virta JM, Revalde JL, Visser EJ, Ottmann C, Brunsveld L, Neochoritis CG, Arkin MR. Scaffold-hopping for molecular glues targeting the 14-3-3/ERα complex. Nat Commun. 2025 Jul 14; 16(1):6467. View on PubMed
  8. Clelland CD, Fan L, Saloner R, Etchegaray JI, Altobelli CR, Salomonsson S, Maltos AM, Sachdev A, Zhu J, Lee SI, Li Y, Zhou Y, Le D, Wang C, Carling G, Kodama L, Sayed F, Perez-Bermejo JA, Geier EG, Yokoyama JS, Rosen H, Nana AL, Spina S, Grinberg LT, Seeley WW, Elahi F, Boxer AL, Arkin MR, Gan L. Opposing role of phagocytic receptors MERTK and AXL in Progranulin deficient FTD. Commun Biol. 2025 Jul 01; 8(1):971. View on PubMed
  9. Maciag AE, Yang Y, Sharma AK, Turner DM, DeHart CJ, Abdelkarim H, Fan L, Smith BP, Kumari V, Dyba M, Rigby M, Castillo Badillo JA, Adams L, Fornelli L, Fox S, Brafman A, Turbyville T, Gillette W, Messing S, Agamasu C, Wolfe AL, Gysin S, Chan AH, Simanshu DK, Esposito D, Chertov O, Stephen AG, Arkin M, Renslo A, Kelleher NL, Gaponenko V, Lightstone FC, Nissley DV, McCormick F. Blocking C-terminal processing of KRAS4b via a direct covalent attack on the CaaX-box cysteine. Proc Natl Acad Sci U S A. 2025 May 13; 122(19):e2410766122. View on PubMed
  10. Detomasi TC, Degotte G, Huang S, Suryawanshi RK, Diallo A, Lizzadro L, Zapatero-Belinchón FJ, Taha TY, Li J, Richards AL, Hantz ER, Alam Z, Montano M, McCavitt-Malvido M, Gumpena R, Partridge JR, Correy GJ, Matsui Y, Charvat AF, Glenn IS, Rosecrans J, Revalde JL, Anderson D, Hultquist JF, Arkin MR, Neitz RJ, Swaney DL, Krogan NJ, Shoichet BK, Verba KA, Ott M, Renslo AR, Craik CS. Structure-based discovery of highly bioavailable, covalent, broad-spectrum coronavirus MPro inhibitors with potent in vivo efficacy. Sci Adv. 2025 04 25; 11(17):eadt7836. View on PubMed
  11. Peck A, Dadi A, Yavarow Z, Alfano LN, Anderson D, Arkin MR, Chou TF, D'Ambrosio ES, Diaz-Manera J, Dudley JP, Elder AG, Ghoshal N, Hart CE, Hart MM, Huryn DM, Johnson AE, Jones KB, Kimonis V, Kiskinis E, Lee EB, Lloyd TE, Mapstone M, Martin A, Meyer H, Mozaffar T, Onyike CU, Pfeffer G, Pindon A, Raman M, Richard I, Rubinsztein DC, Schiava M, Schütz AK, Shen PS, Southworth DR, Staffaroni AM, Taralio-Gravovac M, Weihl CC, Yao Q, Ye Y, Peck N. 2024 VCP International Conference: Exploring multi-disciplinary approaches from basic science of valosin containing protein, an AAA+ ATPase protein, to the therapeutic advancement for VCP-associated multisystem proteinopathy. Neurobiol Dis. 2025 04; 207:106861. View on PubMed
  12. Chou J, Robinson TM, Egusa EA, Lodha R, Zhang M, Badura M, Mikayelyan M, Delavan HM, Swinderman J, Wilson C, Zhu J, Das R, Nguyen M, Loehr A, Golsorkhi T, Simmons A, Abida W, Chinnaiyan AM, Arkin MR, Small EJ, Quigley DA, Yang L, Kim M, Ashworth A, Feng FY. Synthetic Lethal Targeting of CDK12-Deficient Prostate Cancer with PARP Inhibitors. Clin Cancer Res. 2024 Dec 02; 30(23):5445-5458. View on PubMed
  13. Liara Rizzi, Julio C. Rojas, Andrew J. Ambrose, Marcio Luiz Figueredo Balthazar, Michelle R. Arkin, Lea T. Grinberg. D13 caspase-6-cleaved tau, a new biomarker to complement Alzheimer’s disease diagnosis. Alzheimer's & Dementia. 2024 Dec 1; 20(Suppl 8):e095421. View on PubMed
  14. Ian Michael Oh, Song Hua Li, Felipe Luiz Pereira, Prabhleen Kaur, Anya Raju, Rushil Jerfy, Claudia Kimie Suemoto, Renata Elaine Paraizo Leite, Vitor Ribeiro Paes, Roberta Diehl Rodriguez, Andrew J. Ambrose, Salvatore Spina, William W. Seeley, Bruce L. Miller, Michelle R. Arkin, Lea T. Grinberg. Truncated tau accumulates before hyperphosphorylated tau and in relatively distinct neuronal subpopulations in entorhinal cortex and inferior temporal gyrus in Alzheimer’s disease patients. Alzheimer's & Dementia. 2024 Dec 1; 20(Suppl 1):e093137. View on PubMed
  15. Gendelev L, Taylor J, Myers-Turnbull D, Chen S, McCarroll MN, Arkin MR, Kokel D, Keiser MJ. Deep phenotypic profiling of neuroactive drugs in larval zebrafish. Nat Commun. 2024 11 17; 15(1):9955. View on PubMed
  16. Theofilas P, Wang C, Butler D, Morales DO, Petersen C, Ambrose A, Chin B, Yang T, Khan S, Ng R, Kayed R, Karch CM, Miller BL, Gestwicki JE, Gan L, Temple S, Arkin MR, Grinberg LT. iPSC-induced neurons with the V337M MAPT mutation are selectively vulnerable to caspase-mediated cleavage of tau and apoptotic cell death. Mol Cell Neurosci. 2024 Sep; 130:103954. View on PubMed
  17. Somsen BA, Cossar PJ, Arkin MR, Brunsveld L, Ottmann C. 14-3-3 Protein-Protein Interactions: From Mechanistic Understanding to Their Small-Molecule Stabilization. Chembiochem. 2024 Jul 15; 25(14):e202400214. View on PubMed
  18. Vickery HR, Virta JM, Konstantinidou M, Arkin MR. Development of a NanoBRET assay for evaluation of 14-3-3σ molecular glues. SLAS Discov. 2024 07; 29(5):100165. View on PubMed
  19. Silva DB, Trinidad M, Ljungdahl A, Revalde JL, Berguig GY, Wallace W, Patrick CS, Bomba L, Arkin M, Dong S, Estrada K, Hutchinson K, LeBowitz JH, Schlessinger A, Johannesen KM, Møller RS, Giacomini KM, Froelich S, Sanders SJ, Wuster A. Haploinsufficiency underlies the neurodevelopmental consequences of SLC6A1 variants. Am J Hum Genet. 2024 06 06; 111(6):1222-1238. View on PubMed
  20. Konstantinidou M, Arkin MR. Molecular glues for protein-protein interactions: Progressing toward a new dream. Cell Chem Biol. 2024 Jun 20; 31(6):1064-1088. View on PubMed

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