A. Pinkerton

Early-stage therapeutic efficacy of TNAP inhibition using a novel milder murine model of CKD-MBD
20250 citationsauthor #3
Targeting of a Bile Acid Receptor, Takeda G Protein Receptor 5 [TGR5], by a Novel First-in-Class Competitive Antagonist, SBI-364, Diminishes Hepatic and Renal Cystogenesis in Polycystic Liver and Kidney Disease.
20250 citationsauthor #6
Neurotensin receptor 1-biased ligand attenuates neurotensin-mediated excitation of ventral tegmental area dopamine neurons and dopamine release in the nucleus accumbens.
20236 citationsauthor #7
Abstract 1626: Tumors driven by oncogene amplified extrachromosomal DNA (ecDNA) demonstrate enhanced sensitivity to cell cycle checkpoint kinase 1 (CHK1) inhibition
20234 citationsauthor #18
Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator
202255 citationsauthor #9
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
202215 citationsauthor #22
Human LMPTP in complex with inhibitor
20210 citationsauthor #13
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.
20218 citationsauthor #12
Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth
202110 citationsauthor #14
Chronic Kidney Disease-Induced Arterial Media Calcification in Rats Prevented by Tissue Non-Specific Alkaline Phosphatase Substrate Supplementation Rather Than Inhibition of the Enzyme
20219 citationsauthor #4
Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.
202112 citationsauthor #16
The Compound SBI-0090799 Inhibits Zika Virus Infection by Blocking De Novo Formation of the Membranous Replication Compartment
202117 citationsauthor #12
Discovery of DS68702229 as a Potent, Orally Available NAMPT (Nicotinamide Phosphoribosyltransferase) Activator.
202110 citationsauthor #11
Optimization of a Urea-containing Series of Nicotinamide Phosphoribosyltransferase (NAMPT) Activators.
202113 citationsauthor #1
Pharmacological TNAP inhibition efficiently inhibits arterial media calcification in a warfarin rat model but deserves careful consideration of potential physiological bone formation/mineralization impairment.
202024 citationsauthor #4
Inhibition of tissue‐nonspecific alkaline phosphatase protects against medial arterial calcification and improves survival probability in the CKD‐MBD mouse model
202060 citationsauthor #6
P1237TISSUE-NONSPECIFIC ALKALINE PHOSPHATASE, A CULPRIT DURING ARTERIAL MEDIA CALCIFICATION BUT INDISPENSABLE DURING PHYSIOLOGICAL BONE FORMATION/-MINERALIZATION IN RATS
20200 citationsauthor #3
Targeting eIF4F translation initiation complex with SBI-756 sensitises B lymphoma cells to venetoclax
202012 citationsauthor #10
The serine-threonine kinase TAO3 promotes cancer invasion and tumor growth by facilitating trafficking of endosomes containing the invadopodia scaffold TKS5α
20200 citationsauthor #14
β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors.
2020126 citationsauthor #18
1742-P: Targeting the Low Molecular Weight Protein Tyrosine Phosphatase for Obesity-Associated Diabetes Therapy
20200 citationsauthor #5
Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells.
201918 citationsauthor #14
Glucose 6-phosphate dehydrogenase 6-phosphogluconolactonase: characterization of the Plasmodium vivax enzyme and inhibitor studies
201917 citationsauthor #10
Author Correction: Arylmethylamino steroids as antiparasitic agents
20191 citationsauthor #15
Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma.
201916 citationsauthor #10
Systemic inhibition of tissue-nonspecific alkaline phosphatase alters the brain-immune axis in experimental sepsis
201928 citationsauthor #9
Crystal structure of human TAO3 kinase binding ADP
20190 citationsauthor #3
Targeting tumor phenotypic plasticity and metabolic remodeling in adaptive cross-drug tolerance
201956 citationsauthor #10
Boosting NAD+ with a small molecule that activates NAMPT
2019127 citationsauthor #23
Discovery of b-Arrestin Biased, Orally Bioavailable and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
201940 citationsauthor #1
Inhibition of Tissue-Nonspecific Alkaline Phosphatase Attenuates Ectopic Mineralization in the Abcc6-/- Mouse Model of PXE but Not in the Enpp1 Mutant Mouse Models of GACI.
201954 citationsauthor #3
Repurposing antimalarial aminoquinolines and related compounds for treatment of retinal neovascularization
201815 citationsauthor #15
Accelerated Aging and Clearance of Host Anti-inflammatory Enzymes by Discrete Pathogens Fuels Sepsis.
201847 citationsauthor #7
819 Inhibition of tissue-nonspecific alkaline phosphatase prevents ectopic mineralization in the Abcc6-/- mouse model of PXE
20180 citationsauthor #3
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
201836 citationsauthor #1
Diabetes reversal by inhibition of the low molecular weight tyrosine phosphatase
201766 citationsauthor #22
Characterization of the Zika virus two‐component NS2B‐NS3 protease and structure‐assisted identification of allosteric small‐molecule antagonists
2017110 citationsauthor #9
TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling
201756 citationsauthor #11
Accelerated bottom-up drug design platform enables the discovery of novel stearoyl-CoA desaturase 1 inhibitors for cancer therapy
201737 citationsauthor #9
Overexpression of tissue-nonspecific alkaline phosphatase (TNAP) in endothelial cells accelerates coronary artery disease in a mouse model of familial hypercholesterolemia
201742 citationsauthor #14
Arylmethylamino steroids as novel antiparasitic agents
20170 citationsauthor #15
Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.
2017135 citationsauthor #16
Arylmethylamino steroids as antiparasitic agents
201742 citationsauthor #15
A screen for inducers of bHLH activity identifies pitavastatin as a regulator of p21, Rb phosphorylation and E2F target gene expression in pancreatic cancer
201715 citationsauthor #8
TGR 5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases via cAMP / G α s signaling Short title : TGR 5 in hepatic cystogenesis
20170 citationsauthor #11
High‐throughput screening and bioinformatic analysis to ascertain compounds that prevent saturated fatty acid‐induced &bgr;‐cell apoptosis
201719 citationsauthor #5
Abstract 426: Overexpression of Tissue-nonspecific Alkaline Phosphatase (TNAP) Accelerates Coronary Artery Disease in the Setting of Hypercholesterolemia in Mice
20170 citationsauthor #10
Ectopic calcification in pseudoxanthoma elasticum responds to inhibition of tissue-nonspecific alkaline phosphatase
2017102 citationsauthor #10
PPARδ repression in Huntington’s disease and its essential role in CNS translate into a potent agonist therapy
201620 citationsauthor #21
ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse.
201642 citationsauthor #15
Figure 3, Stability of ML401 in 1×
20150 citationsauthor #18
Figure 1, Structure of ML400
20150 citationsauthor #23
Abstract 4459: Accelerated drug discovery platform yields synthesis of novel stearoyl-CoA desaturase 1 inhibitors that demonstrate anti-tumor efficacy in several models of aggressive cancer
20150 citationsauthor #8
Figure 7, ML400 Prevents Adipogenesis in 3T3-L1 Cells
20150 citationsauthor #23
PPARδ repression in Huntington’s disease and its essential role in CNS translate into a potent agonist therapy
201581 citationsauthor #21
Figure 4.1.1, Structures for Compounds Reported to inhibit the mtPTP
20150 citationsauthor #7
SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex.
201534 citationsauthor #2
Aberrant lipid metabolism in anaplastic thyroid carcinoma reveals stearoyl CoA desaturase 1 as a novel therapeutic target.
2015146 citationsauthor #3
Pathophysiological Role of Vascular Smooth Muscle Alkaline Phosphatase in Medial Artery Calcification
2015182 citationsauthor #12
Table 3, Probe and Analog Submissions to MLSMR (Evotec) for TAG inhibitors
20150 citationsauthor #18
Table 4, Summary of in vitro ADME Properties of selected LMPTP inhibitors
20150 citationsauthor #23
Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.
201512 citationsauthor #10
Figure 2, Stability of ML377 in 1× PBS at RT
20150 citationsauthor #18
Allosteric Small Molecule Inhibitors of LMPTP
20152 citationsauthor #23
Table 1, Potency and selectivity characteristics for probe ML400
20150 citationsauthor #23
Scheme1, Synthesis of ML401, conditions: a. CDI, THF 2 to 3 hrs at RT (79%); b. DCM, TFA 0 °C; c. 4-Cl benzyl bromide, K2CO3, Acetone, 50°C 2 hours (58%)
20150 citationsauthor #18
Scheme 1, Synthesis of ML400, conditions: a. 4-Methoxybenzoyl chloride, DIPEA, DCM, 0°C to RT, overnight (80%); b. t-BuOK, t-BuOH, 75°C, overnight (84%); c. POCl3, 90°C, overnight (61%); d. 3-(Piperidin-1-yl)propan-1-amine, t-BuOK 10%, Dry DMA, 135°C, overnight, nitrogen atmosphere (57%)
20150 citationsauthor #23
Table 4, Summary of in vitro ADME Properties of TAG inhibitor probe ML377
20150 citationsauthor #18
Table 5, Summary of in vitro ADME Properties of EBI2 inhibitor probe ML401 (MLS-0472527)
20150 citationsauthor #18
Scheme 1, Synthesis of ML377
20150 citationsauthor #18
Figure 1, EBI2 antagonist GSK682753
20150 citationsauthor #18
Figure 3, Potency of ML377 inhibition for triacylglycerol accumulation in both H9c2 cells and differentiated human skeletal myotubes
20150 citationsauthor #18
Inhibitors of Myocyte Triacylglyceride Accumulation
20150 citationsauthor #18
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
2015140 citationsauthor #28
Figure 6, Eurofins Panel for ML401
20150 citationsauthor #18
Table 3, Probe and Analog Submissions to MLSMR (Evotec) for Small Molecule Inhibitors of LMPTP
20150 citationsauthor #23
Figure 2, Stability of ML400 in 1× PBS and 1:1 PBS:ACN at RT
20150 citationsauthor #23
Small Molecules Targeting the Mitochondrial Permeability Transition
201514 citationsauthor #7
Figure 1, Structure of ML377
20150 citationsauthor #18
Figure 5, Potency of ML401 inhibition in EBI2 beta-arrestin and RS11846 cell chemotaxis assays
20150 citationsauthor #18
Functional Antagonists of EBI-2
20155 citationsauthor #18
Table 7, SAR Around Scaffolds C, D, E and F
20140 citationsauthor #8
Benzodiazepinone Derivatives Protect against Endoplasmic Reticulum Stress-Mediated Cell Death in Human Neuronal Cell Lines
201413 citationsauthor #8
Table 7, Summary of in vitro ADME Properties of Gli-Sufu Antagonists Probe CID6538918
20140 citationsauthor #19
Figure 2, Prior Art compounds described in Patent for UBC13/UEV
20140 citationsauthor #8
Figure 3, Structure of ML307
20140 citationsauthor #8
Table 5, Potencies of key screening hit scaffolds
20140 citationsauthor #20
Figure 6a, Stability of ML262 in 50% acetonitrile: 1X PBS
20140 citationsauthor #20
Scheme 1, Synthesis of ML307, conditions
20140 citationsauthor #8
Figure 1, Overview of fatty liver disease
20140 citationsauthor #20
Small-molecule antagonists of Gli function
20143 citationsauthor #19
A high throughput screen for inhibitors of nematode detoxification genes
20142 citationsauthor #18
Table 6, SAR Around Scaffold B
20140 citationsauthor #8
[Table, Identification of 7, 8, 9, 10-tetrahydro-6H-azepino[1,2-e]purine Scaffolds].
20140 citationsauthor #8
Figure 2, Synthesis of triglycerides and lipid droplets
20140 citationsauthor #20
Table 5, Summary of Gli-antagonist (Sufu-KO-LIGHT) HTS Performance
20140 citationsauthor #19
Table 6, SAR elucidation of thieno[3,2-b]pyrrole series A and B
20140 citationsauthor #20
Table 4, Probe and Analog Submissions to MLSMR (BioFocus DPI) for Gli-Sufu Antagonist ML340
20140 citationsauthor #19
Figure 6b, Stability of ML262 in 50% acetonitrile: water
20140 citationsauthor #20
Figure 3, Structure of ML340
20140 citationsauthor #19

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