Anthony Pinkerton, Ph.D.

Anthony Pinkerton

Anthony Pinkerton, Ph.D.

Anthony Pinkerton's Research Focus

Drug Discovery, Medicinal Chemistry, Synthetic Chemistry, Pharmacogenomics, Pharmacokinetics, Synthetic Organic Chemistry, Pharmacodynamics, Chemistry, Medicinal Chemistry, Pharmacology, Combinatorial Chemistry, Drug Delivery, Fragment-Based Drug Design, Mass Spectrometry, Nuclear Magnetic Resonance Spectroscopy (NMR), Rational Drug Design
Neurological and Psychiatric Disorders, Structural Biology

Dr. Pinkerton is currently leading the chemistry efforts on a broad range of targets across multiple therapeutic areas at SBP. Some recent examples of programs underway include tissue nonspecific alkaline phosphatase (TNAP) inhibitors in collaboration with Jose Luis Millan (SBP) and pharmaceutical industry partners, selective neurotensin receptor 1 (NTR1) modulators in collaboration with Marc Caron and Larry Barak (Duke University), and selective inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) in collaboration with Nunzio Bottini and Stephanie Stanford (UCSD).

Anthony Pinkerton's Research Report


“Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor” Pinkerton, A.B.; Sergienko, E.; Bravo, Y.; Dahl, R.; Ma, C.-T.; Sun, Q.; Jackson, M. R.; Cosford, N. D. P.; Millan, J.-L. Bioorg. Med. Chem. Letters 2018, 28, 31-34.

“Overexpression of Tissue-nonspecific Alkaline Phosphatase (TNAP) in Endothelial Cells Accelerates Coronary Artery Disease in a Mouse Model of Familial Hypercholesterolemia”Romanelli, F.; Corbo, A.; Salehi, M.; Yadav, M. C.; Salman, S.; Petrosian, D.; Rashidbaigi, O.J.; Chait, J.; Kuruvilla, J.; Plummer, M.; Radichev, I.; Margulies, K. B.; Gerdes, A. M.; Pinkerton, A. B.; Millan, J.L.; Savinov, A. Y.; Savinova, O. V. PLOS One 2017, 12(10): e0186426.

“Ectopic calcification in pseudoxanthoma elasticum responds to inhibition of tissue non-specific alkaline phosphatase” Ziegler, S.; Chew, E.; Dietz, H.; Millan, J.-L.; Pinkerton, A. B.; Gahl, W.; Ferreira, C.; MacFarlane, E.; Riddle, R.; Tomlinson, R.; Martin, L.; Ma, C.-T.; Sergienko, E. Science Translational Medicine 2017, 9(393). doi: 10.1126/scitranslmed.aal1669

“Pathophysiological role of vascular smooth muscle alkaline phosphatase in medial artery calcification” Sheen, C. R.; Kuss, P.; Narisawa, S.; Yadav, M. C.; Nigro, J.; Wang, W.; Chhea, T. N.; Sergienko, E. A.; Kapoor, K.; Jackson, M. R.; Hoylaerts, M. F.; Pinkerton, A. B.; O’Neill, W. C.; Millan, J. L. Journal of Bone and Mineral Research2015, 30 (5), 824-836

“Inhibitors of Tissue-Nonspecific Alkaline Phosphatase (TNAP): From Hits to Leads” Teriete, P.; Pinkerton, A. B.; Cosford, N. D. P., Methods in Molecular Biology,2013, 1053, 85-101

PCT WO 2016054056 “Methods of treating disorders characterized by medial vascular calcification with an inhibitor of tissue-nonspecific alkaline phosphatase” Gahl, W. A.; Ziegler, S. G.; Dietz, H. C.; Pinkerton, A. B.; Millan, J. L

PCT WO 2013126608 “Preparation of pyridinylsulfonamidedervatives for use as TNAP inhibitor” Pinkerton, A. B.; Dahl, R.; Cosford, N. D. P.; Millan, J. L.


“ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse” Barak, L.S.; Bai, Y.; Peterson, S.; Evron, T.; Urs, N. M.; Peddibhotla, S.; Hedrick, M. P.; Hershberger, P.; Maloney, P. R.; Chung, T. D. Y.; Rodriguiz, R. M.; Wetsel, W. C.; Thomas, J. B.; Hanson, G. R.; Pinkerton, A. B.; Caron, M. G. ACS Chemical Biology 2016 11(7), 1880-1890. DOI:10.1021/acschembio.6b00291

“Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor” Peddibhotla, S.; Hedrick, M. P.; Hershberger, P.; Maloney, P. R.;  Li, Y.; Milewski, M.; Gosalia, P.; Gray, W.; Mehta, A.; Sugarman, E.; Hood, B; Suyama, E.; Nguyen, K.; Heynen-Genel, S.; Vasile, S.; Salaniwal, S.; Stonich, D.; Su, Y.; Mangravita-Novo, A.;  Vicchiarelli, M.; Roth, G. P.; Smith L. H.; Chung, T. D. Y; Hanson, G. R.; Thomas, J. B.; Caron, M. G.;  Barak, L. S.; Pinkerton, A. B.  (2013) ACS Medicinal Chemistry Letters, 4, 846-851.  PMCID: PMC3940307.

“Imidazole-derived agonists for the neurotensin 1 receptor” Hershberger, P. M.; Hedrick, M. P.; Peddibhotla, S.; Mangravita-Novo, A.; Gosalia, P.; Li, Y.; Gray, W.; Vicchiarelli, M.; Smith, L. H.; Chung, T. D. Y.; Thomas, J. B.; Caron, M. G.; Pinkerton, A. B.; Barak, L. S.; Roth G. P. Bioorg Med Chem Lett. 2014 Jan 1;24(1):262-7. doi: 10.1016/j.bmcl.2013.11.026. PMID: 24332089. PMCID: PMC3898338.

PCT WO 2015200534 “Preparation of substituted quinazolines as small molecule agonists of neurotensin receptor 1” Pinkerton, A. B.; Hershberger, P. M.; Peddibhotla, S.; Maloney, P. R.;  Hedrick, M. P

PCT WO 2014100501 “Preparation of piperazinylquinazolines and related compounds as agonists of neurotensin receptor 1” Pinkerton, A.; Maloney, P.; Hershberger, S.; Peddibhotla, S.; Hedrick, M.; Barak, L.; Caron, M.


“Diabetes reversal by inhibition of the low molecular weight tyrosine phosphatase” Stanford, S. M.; Aleshin, A. E.; Zhang, V.; Ardecky, R. J.; Hedrick, M.P.; Zou, J.; Ganji, S. R.; Bliss, M. R.; Yamamoto, F.; Bobkov, A. A.; Kiselar, J.; Liu, Y.; Cadwell, G. W.; Khare, S.; Yu, J.; Barquilla, A.; Chung, T. D. Y.; Mustelin, T.; Schenk, S.; Bankston, L. A.; Liddington, R. C.; Pinkerton, A. B.; Bottini, N., Nature Chemical Biology 2017, 13, 624-632. doi:10.1038/nchembio.2344

PCT WO 2016061280 “Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof” Bottini, N.; Zou, J.; Ganji, S.R.; Stanford, S.; Pinkerton, A.; Chung, T.; Hedrick, M.; Ardecky, R

Anthony Pinkerton's Bio

Dr. Pinkerton’s career in industry began as a medicinal chemist at the Merck Research Laboratories in San Diego. Over his career, Tony has worked in multiple therapeutic areas including CNS, virology, diabetes, inflammation, and oncology, with extensive experience in GPCRs. He has been both project leader and project manager for oncology, virology and diabetes targets, as well as chemistry lead for the metabolic disease therapeutic area group, in which he helped a team identify and prosecute the most promising new targets in the field. In addition, Tony has led the IP strategy around multiple chemical series and programs. Tony is an inventor or co-inventor on over 40 patents or patent applications covering small molecule therapeutics, as well as over 70 publications. During his career he has helped advance multiple compounds into clinical development.

Tony originally trained as a synthetic organic chemist in the laboratories of Dieter Seebach at ETH-Zurich (where he was a Fulbright Scholar) and Barry Trost at Stanford University, where he earned his Ph.D. in chemistry in 2001. While at Stanford he developed new metal catalyzed reactions and completed the total synthesis of several natural products.

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ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse.

Barak LS, Bai Y, Peterson S, Evron T, Urs NM, Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Chung TD, Rodriguiz RM, Wetsel WC, Thomas JB, Hanson GR, Pinkerton AB, Caron MG

ACS Chem Biol 2016 Jul 15 ;11(7):1880-90

PPAR-δ is repressed in Huntington's disease, is required for normal neuronal function and can be targeted therapeutically.

Dickey AS, Pineda VV, Tsunemi T, Liu PP, Miranda HC, Gilmore-Hall SK, Lomas N, Sampat KR, Buttgereit A, Torres MJ, Flores AL, Arreola M, Arbez N, Akimov SS, Gaasterland T, Lazarowski ER, Ross CA, Yeo GW, Sopher BL, Magnuson GK, Pinkerton AB, Masliah E, La Spada AR

Nat Med 2016 Jan ;22(1):37-45

Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.

Ardecky RJ, Bobkova EV, Kiffer-Moreira T, Brown B, Ganji S, Zou J, Pass I, Narisawa S, Iano FG, Rosenstein C, Cheltsov A, Rascon J, Hedrick M, Gasior C, Forster A, Shi S, Dahl R, Vasile S, Su Y, Sergienko E, Chung TDY, Kaunitz J, Hoylaerts MF, Pinkerton AB, Millán JL

Bioorg Med Chem Lett 2014 Feb 1 ;24(3):1000-1004

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An Optimized Dihydrodibenzothiazepine Lead Compound (SBI-0797750) as a Potent and Selective Inhibitor of Plasmodium falciparum and P. vivax Glucose 6-Phosphate Dehydrogenase 6-Phosphogluconolactonase.

Berneburg I, Peddibhotla S, Heimsch KC, Haeussler K, Maloney P, Gosalia P, Preuss J, Rahbari M, Skorokhod O, Valente E, Ulliers D, Simula LF, Buchholz K, Hedrick MP, Hershberger P, Chung TDY, Jackson MR, Schwarzer E, Rahlfs S, Bode L, Becker K, Pinkerton AB

Antimicrob Agents Chemother 2022 Apr 19 ;66(4):e0210921

Discovery of DS68702229 as a Potent, Orally Available NAMPT (Nicotinamide Phosphoribosyltransferase) Activator.

Akiu M, Tsuji T, Iida K, Sogawa Y, Terayama K, Yokoyama M, Tanaka J, Asano D, Honda T, Sakurai K, Pinkerton AB, Nakamura T

Chem Pharm Bull (Tokyo) 2021 ;69(11):1110-1122

The Compound SBI-0090799 Inhibits Zika Virus Infection by Blocking De Novo Formation of the Membranous Replication Compartment.

Riva L, Goellner S, Biering SB, Huang CT, Rubanov AN, Haselmann U, Warnes CM, De Jesus PD, Martin-Sancho L, Terskikh AV, Harris E, Pinkerton AB, Bartenschlager R, Chanda SK

J Virol 2021 Oct 27 ;95(22):e0099621

Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.

Stanford SM, Diaz MA, Ardecky RJ, Zou J, Roosild T, Holmes ZJ, Nguyen TP, Hedrick MP, Rodiles S, Guan A, Grotegut S, Santelli E, Chung TDY, Jackson MR, Bottini N, Pinkerton AB

J Med Chem 2021 May 13 ;64(9):5645-5653

Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.

Akiu M, Tsuji T, Sogawa Y, Terayama K, Yokoyama M, Tanaka J, Asano D, Sakurai K, Sergienko E, Sessions EH, Gardell SJ, Pinkerton AB, Nakamura T

Bioorg Med Chem Lett 2021 Jul 1 ;43:128048

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