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David Lapinsky, Ph.D.

Associate Professor Of Medicinal Chemistry
Mylan School of Pharmacy
Pharmaceutical Sciences

Mellon 422B
Phone: 412.396.6069

Education:

Ph.D., Medicinal Chemistry, The Ohio State University, 2003
B.S., Pharmacy, Duquesne University, 1997
Research

Watch a video that explains the research done in the Lapinsky lab

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


1.) target identification of hit compounds originating from phenotypic screening campaigns,
2.) mechanism of action studies, confirmation of target engagement, or selectivity profiling (also known as Affinity-Based Protein Profiling (AfBPP)),
3.) characterizing the interactions of sterols or lipids with proteins, and
4.) determining binding sites within target proteins.

Grants/Contracts

R21MH098127 National Institute of Mental Health (NIMH) NIH Grant
Principal Investigators: M. Cascio, Ph.D. and D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, 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)
Principal Investigator: D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, Ph.D.
Non-Tropane Irreversible Dopamine Transporter Ligands
$364,182
7/1/09 to 6/30/11

Duquesne University Faculty Development Fund
Principal Investigator: D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, Ph.D.
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

R01DA026530 National Institute on Drug Abuse (NIDA) NIH Grant
Principal Investigator: C. K. Surratt, Ph.D.
Co-investigators: J. D. Madura, Ph.D. and D. J. Lapinsky, Ph.D.
Dopamine Transporter Structure and Function
$627,250
7/1/09 to 6/30/11

R01DA027806 NIDA NIH/NSF Grant
Principal Investigator: J. D. Madura, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and D. J. Lapinsky, Ph.D.
CRCNS: Computational and Experimental Study of Dopamine and Serotonin Transporters
$1,545,450
7/1/09 to 6/30/14

Hunkele Dreaded Disease Award
Principal Investigator: D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, Ph.D.
"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

Publications

Recent Developments and Applications of Clickable Photoprobes in Medicinal Chemistry and Chemical Biology. Lapinsky, David J.; Johnson, Douglas S. Future Medicinal Chemistry 2015, in press.

Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram. Kumar, Vivek; Yarravarapu, Nageswari; Lapinsky, David J.; Perley, Danielle; Felts, Bruce; Tomlinson, Michael J.; Vaughan, Roxanne A.; Henry, L. Keith; Lever, John R.; Newman, Amy Hauck. Journal of Medicinal Chemistry 2015, 58(14), 5609-5619.

(±)-2-(N-tert-Butylamino)-3'-[125I]-iodo-4'-azidopropiophenone: A dopamine transporter and nicotinic acetylcholine receptor photoaffinity ligand based on bupropion (Wellbutrin, Zyban). Lapinsky, David J.; Aggarwal, Shaili; Nolan, Tammy L.; Surratt, Christopher K.; Lever, John R.; Acharya, Rejwi; Vaughan, Roxanne A.; Pandhare, Akash; Blanton, Michael P. Bioorganic & Medicinal Chemistry Letters 2012, 22(1), 523-526.

Bupropion Binds to Two Sites in the Torpedo Nicotinic Acetylcholine Receptor Transmembrane Domain: A Photoaffinity Labeling Study with the Bupropion Analogue [125I]-SADU-3-72. Pandhare, Akash; Hamouda, Ayman K.; Staggs, Brandon; Aggarwal, Shaili; Duddempudi, Phaneendra K.; Lever, John R.; Lapinsky, David J.; Jansen, Michaela; Cohen, Jonathan B.; Blanton, Michael P. Biochemistry 2012, 51(12), 2425-2435.

Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (±)-threo-Methylphenidate. Lapinsky, David J.; Yarravarapu, Nageswari; Nolan, Tammy L.; Surratt, Christopher K.; Lever, John R.; Tomlinson, Michael; Vaughan, Roxanne A.; Deutsch, Howard M. ACS Medicinal Chemistry Letters 2012, 3(5), 378-382.

Structural and functional interaction of (±)-2-(N-tert-butylamino)-3'-iodo-4'-azidopropiophenone, a photoreactive bupropion derivative, with nicotinic acetylcholine receptors. Arias, Hugo R.; Feuerbach, Dominik; Targowska-Duda, Katarzyna M.; Aggarwal, Shaili; Lapinsky, David J.; Jozwiak, Krzysztof. Neurochemistry International 2012, 61(8), 1433-1441.

Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry. Lapinsky, David J. Bioorganic & Medicinal Chemistry 2012, 20(21), 6237-6247.

Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling. Lapinsky, David J.; Velagaleti, Ranganadh; Yarravarapu, Nageswari; Liu, Yi; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Acharya, Rejwi; Vaughan, Roxanne A.; et al. Bioorganic & Medicinal Chemistry 2011, 19(1), 504-512.

Identification of a Novel Selective Serotonin Reuptake Inhibitor by Coupling Monoamine Transporter-Based Virtual Screening and Rational Molecular Hybridization. Nolan, Tammy L.; Lapinsky, David J.; Talbot, Jeffery N.; Indarte, Martin; Liu, Yi; Manepalli, Sankar; Geffert, Laura M.; Amos, Mary Ellen; Taylor, Phillip N.; Madura, Jeffry D.; et al. ACS Chemical Neuroscience 2011, 2(9), 544-552.

A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone. Lapinsky, David J.; Aggarwal, Shaili; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Vaughan, Roxanne A. Bioorganic & Medicinal Chemistry 2009, 17(11), 3770-3774.

Presentations

Binding ensemble profiling with (f)photoaffinity labeling (BEProFL): Mapping the binding sites and poses of metabotropic glutamate receptor type 2 (mGlu2) positive allosteric modulators (PAMs). Aggarwal, Shaili; Lapinsky, David J.; Gregory, Karen J. Abstracts of Papers, 246th ACS National Meeting & Exposition, Indianapolis, IN, United States, September 8-12, 2013, MEDI-236.

Binding ensemble profiling with (f)photoaffinity labeling (BEProFL): Development of clickable GBR-12909 photoprobes for dopamine transporter (DAT) structure-function studies. Velagaleti, Ranganadh; Lapinsky, David J. Abstracts of Papers, 244th ACS National Meeting & Exposition, Philadelphia, PA, United States, August 19-23, 2012, MEDI-360.

Binding ensemble profiling with (f)photoaffinity labeling (BEProFL): Mapping the binding sites and poses of Bupropion within the dopamine transporter (DAT) and nicotinic acetylcholine receptors (nAChRs). Aggarwal, Shaili; Lapinsky, David J.; Nolan, Tammy; Surratt, Christopher K.; Lever, John R.; Vaughan, Roxanne A.; Blanton, Michael. 244th ACS National Meeting & Exposition, Philadelphia, PA, United States, August 19-23, 2012, MEDI-362.

Binding ensemble profiling with (f)photoaffinity labeling (BEProFL): Mapping the binding sites and poses of selective serotonin reuptake inhibitors (SSRIs) within the serotonin transporter (SERT). Yarravarapu, Nageswari; Lapinsky, David J.; Nolan, Tammy; Surratt, Christopher K.; Cascio, Michael. 244th ACS National Meeting & Exposition, Philadelphia, PA, United States, August 19-23, 2012, MEDI-361.

Structure-based virtual screening for monoamine transporter inhibitors. Madura, Jeffry D.; Manepalli, Sankar; Nolan, Tammy; Geffert, Laura; Lapinsky, David J.; Surratt, Christopher K. 243rd ACS National Meeting & Exposition, San Diego, CA, United States, March 25-29, 2012, COMP-627.

Development of novel photoaffinity ligands for the dopamine transporter based on pyrovalerone. Aggarwal, Shaili; Lapinsky, David J.; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Vaughan, Roxanne A.; Manepalli, Sankar; Madura, Jeffry D. 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009, MEDI-325.

Elucidation of binding profile similarities across structurally diverse ligands using a 3D dopamine transporter model. Manepalli, Sankar; Madura, Jeffry D.; Lapinsky, David J.; Surratt, Christopher K. 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009, COMP-235.

Courses

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