Contact Information

Education

  • Wiess Instructor of Chemistry, Rice University, 2004–07
  • Post-Doctoral Researcher, Johns Hopkins University, 2003–04
  • Ph.D., Medicinal Chemistry, The Ohio State University, 2003
  • B.S., Pharmacy, Â鶹ֱ²¥, 1997

Research Interests or Expertise

In the areas of chemical biology and medicinal chemistry, the Lapinsky research group primarily focuses on the rational design and synthesis of clickable covalent compounds. These are valuable compounds that can be used for:

  • Target identification of hit compounds originating from phenotypic screening campaigns
  • Mechanism of action studies, confirmation of target engagement, or selectivity profiling (also known as Affinity-Based Protein Profiling (AfBPP))
  • Characterizing the interactions of small-molecules with drug targets
  • Determining binding sites within target proteins

School

  • Â鶹ֱ²¥ Faculty Development/Robert Wintermeyer Fund
    "Tackling African Cryptosporidiosis with Chemical Probes"
    $10,000
    4/17/20 - 8/1/22
  • Neurocrine Biosciences, Inc. (Sponsored Research Agreement)
    "Drug Target Identification for CNS Disorders"
    $118,768
    1/16/19 - 1/15/20
  • Â鶹ֱ²¥ Undergraduate Summer Research Fellowship (Matthew Wolowski)
    "Confronting Cancer with Cysteine-Reactive Probes"
    $4,000
    4/16/18 - 8/25/18
  • Charles Henry Leach II Fund
    "Tackling Cancer with Fully-Functionalized Small-Molecule Probes"
    $10,000
    8/15/17 - 5/15/18
  • Hunkele Dreaded Disease Award
    "Fully Functionalized Small-Molecule Probes for Oncology Drug Discovery"
    $3,359
    1/1/17 - 12/31/18
  • Commonwealth Universal Research Enhancement (C.U.R.E.) Award
    "Fully Functionalized Small-Molecule Probes for Oncology Drug Discovery"
    $62,686
    1/1/16 - 12/31/17
  • R21MH098127 National Institute of Mental Health (NIMH) NIH Grant
    Co-Principal Investigators: M. Cascio, Ph.D. and D. J. Lapinsky, Ph.D.
    "Photoprobes for Identifying Potential Anti-Depressant and Anti-Anxiety Medications"
    $363,000
    4/17/13 - 3/31/15
  • R03DA027081 NIDA NIH Grant (Early Career Award in the Chemistry of Drug Abuse)
    Non-Tropane Irreversible Dopamine Transporter Ligands
    $364,182
    7/1/09 to 6/30/11
  • Â鶹ֱ²¥ Faculty Development Fund
    The Search for Medications to Treat Psychostimulant Dependence: Rational Drug Design by Molecular Hybridization of Modafinil and Piperazine-Based Dopamine Transporter Inhibitors
    $7,137
    5/1/09 to 6/30/11
  • Hunkele Dreaded Disease Award
    "Molecular modeling-guided discovery and design of novel irreversible ligands for the dopamine transporter, the brain's cocaine receptor"
    $10,000
    7/1/08 - 6/30/09
  • Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes.
  • Hellyer SD, Aggarwal S, Chen ANY, Leach K, Lapinsky DJ, Gregory KJ.
    ACS Chem Neurosci. 2020 Jun 3;11(11):1597-1609. doi: 10.1021/acschemneuro.0c00009. Epub 2020 May 22.
    PMID: 32396330
  • Clickable photoaffinity ligands for the human serotonin transporter based on the selective serotonin reuptake inhibitor (S)-citalopram.
    Yarravarapu N, Geffert L, Surratt CK, Cascio M, Lapinsky DJ.
    Bioorg Med Chem Lett. 2018 Nov 15;28(21):3431-3435. doi: 10.1016/j.bmcl.2018.09.029. Epub 2018 Sep 22.
    PMID: 30266542
  • Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide.
    Jackson P, Lapinsky DJ.
    J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
    PMID: 30132667
  • Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.
    Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ.
    ACS Chem Biol. 2016 Jul 15;11(7):1870-9. doi: 10.1021/acschembio.6b00026. Epub 2016 May 4.
    PMID: 27115427
  • Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram.
    Kumar V, Yarravarapu N, Lapinsky DJ, Perley D, Felts B, Tomlinson MJ, Vaughan RA, Henry LK, Lever JR, Newman AH.
    J Med Chem. 2015 Jul 23;58(14):5609-19. doi: 10.1021/acs.jmedchem.5b00682. Epub 2015 Jul 8.
    PMID: 26153715
  • Recent developments and applications of clickable photoprobes in medicinal chemistry and chemical biology.
    Lapinsky DJ, Johnson DS.
    Future Med Chem. 2015;7(16):2143-71. doi: 10.4155/fmc.15.136. Epub 2015 Oct 29.
    PMID: 26511756
  • PHBM 436 - Respiratory, Dermatology, and Ophthalmic
    Disorders Module
  • PHBM 437 - Endocrine Module
  • PHBM 441 - Hematology, Oncology, and Transplantation Module
  • GPSC 516 - Synthetic Organic Medicinal Chemistry I
  • GPSC 517 - Synthetic Organic Medicinal Chemistry II