selected publications
- Small-molecule inhibition of SARS-CoV-2 NSP14 RNA cap methyltransferase. Nature. 2024 Academic Article GET IT
- Indazole to 2-cyanoindole scaffold progression for mycobacterial lipoamide dehydrogenase inhibitors achieves extended target residence time and improved antibacterial activity. Angewandte Chemie (International ed. in English). 2024 Academic Article GET IT
- Nesprin-2 is a novel scaffold protein for telethonin and FHL-2 in the cardiomyocyte sarcomere. The Journal of biological chemistry. 2024 Academic Article GET IT
- Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055. ACS medicinal chemistry letters. 2024 Academic Article GET IT
- Addition to "Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation". 2024 GET IT
- Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation. Journal of chemical information and modeling. 2023 Academic Article GET IT
-
On-demand male contraception via acute inhibition of soluble adenylyl cyclase.
Nature communications.
2023
Academic Article
GET IT
Times cited: 42 - Structure-Activity Relationship Studies of Antimalarial Plasmodium Proteasome Inhibitors─Part II. Journal of medicinal chemistry. 2023 Academic Article GET IT
-
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Journal of medicinal chemistry.
2022
Academic Article
GET IT
Times cited: 10 -
Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential.
Frontiers in physiology.
2022
Academic Article
GET IT
Times cited: 6 - Small-molecule inhibition of the acyl-lysine reader ENL as a strategy against acute myeloid leukemia. Cancer discovery. 2022 Academic Article GET IT
- Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors. Journal of medicinal chemistry. 2022 Academic Article GET IT
- Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9). Bioorganic & medicinal chemistry letters. 2022 Academic Article GET IT
- Transforming Academic Drug Discovery. Chembiochem : a European journal of chemical biology. 2022 Review GET IT
- A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors. ACS medicinal chemistry letters. 2022 Academic Article GET IT
-
Soluble adenylyl cyclase inhibition prevents human sperm functions essential for fertilization.
Molecular human reproduction.
2021
Academic Article
GET IT
Times cited: 35 -
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
ACS medicinal chemistry letters.
2021
Academic Article
GET IT
Times cited: 18 -
Macrocyclic Peptides that Selectively Inhibit the Mycobacterium tuberculosis Proteasome.
Journal of medicinal chemistry.
2021
Academic Article
GET IT
Times cited: 11 -
Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice.
Angewandte Chemie (International ed. in English).
2021
Academic Article
GET IT
Times cited: 23 - Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules. Cancer research. 2021 Academic Article GET IT
- Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions. ACS infectious diseases. 2021 Academic Article GET IT
-
Optimization of lead compounds into on-demand, nonhormonal contraceptives: leveraging a public-private drug discovery institute collaboration†.
Biology of reproduction.
2020
Academic Article
GET IT
Times cited: 15 -
Selective Phenylimidazole-Based Inhibitors of the Mycobacterium tuberculosis Proteasome.
Journal of medicinal chemistry.
2019
Academic Article
GET IT
Times cited: 15 -
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.
Bioorganic & medicinal chemistry letters.
2019
Academic Article
GET IT
Times cited: 38 -
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Nature communications.
2019
Academic Article
GET IT
Times cited: 170 -
Improvement of Asparagine Ethylenediamines as Anti-malarial Plasmodium-Selective Proteasome Inhibitors.
Journal of medicinal chemistry.
2019
Academic Article
GET IT
Times cited: 29 -
Development of a New Structural Class of Broadly Acting HCV Non-Nucleoside Inhibitors Leading to the Discovery of MK-8876.
ChemMedChem.
2017
Academic Article
GET IT
Times cited: 8 -
Thiazomycin, nocathiacin and analogs show strong activity against clinical strains of drug-resistant Mycobacterium tuberculosis.
The Journal of antibiotics.
2017
Academic Article
GET IT
Times cited: 2 -
Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
GET IT
Times cited: 10 -
In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.
Antimicrobial agents and chemotherapy.
2016
Academic Article
GET IT
Times cited: 22 -
Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
GET IT
Times cited: 7 -
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
GET IT
Times cited: 13 -
Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
GET IT
Times cited: 11 -
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
GET IT
Times cited: 12 -
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
GET IT
Times cited: 17 -
Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
GET IT
Times cited: 14 -
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
GET IT
Times cited: 19 -
Design, synthesis, structure-function relationship, bioconversion, and pharmacokinetic evaluation of ertapenem prodrugs.
Journal of medicinal chemistry.
2014
Academic Article
GET IT
Times cited: 10 -
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
ACS medicinal chemistry letters.
2014
Academic Article
GET IT
Times cited: 70 -
Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity.
ChemMedChem.
2013
Academic Article
GET IT
Times cited: 174 -
Design, synthesis, and evaluation of prodrugs of ertapenem.
ACS medicinal chemistry letters.
2013
Academic Article
GET IT
Times cited: 7 -
Synthesis and antibacterial activity of novel water-soluble nocathiacin analogs.
Bioorganic & medicinal chemistry letters.
2012
Academic Article
GET IT
Times cited: 15 -
Novel transcriptome profiling analyses demonstrate that selective peroxisome proliferator-activated receptor γ (PPARγ) modulators display attenuated and selective gene regulatory activity in comparison with PPARγ full agonists.
Molecular pharmacology.
2012
Academic Article
GET IT
Times cited: 9 -
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
Journal of medicinal chemistry.
2011
Academic Article
GET IT
Times cited: 41 -
Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3).
ChemMedChem.
2011
Academic Article
GET IT
Times cited: 48 -
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Bioorganic & medicinal chemistry letters.
2009
Academic Article
GET IT
Times cited: 51 -
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Journal of medicinal chemistry.
2009
Academic Article
GET IT
Times cited: 20 -
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma and extracellular fluid volume.
Journal of medicinal chemistry.
2009
Academic Article
GET IT
Times cited: 44 -
Discovery of the development candidate N-tert-butyl nodulisporamide: a safe and efficacious once monthly oral agent for the control of fleas and ticks on companion animals.
Journal of medicinal chemistry.
2009
Academic Article
GET IT
Times cited: 25 -
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Bioorganic & medicinal chemistry letters.
2009
Academic Article
GET IT
Times cited: 23 -
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Bioorganic & medicinal chemistry letters.
2008
Academic Article
GET IT
Times cited: 14 -
Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.
Diabetes.
2008
Academic Article
GET IT
Times cited: 154 -
A novel selective peroxisome proliferator-activator receptor-gamma modulator-SPPARgammaM5 improves insulin sensitivity with diminished adverse cardiovascular effects.
European journal of pharmacology.
2008
Academic Article
GET IT
Times cited: 30 -
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Bioorganic & medicinal chemistry letters.
2008
Academic Article
GET IT
Times cited: 137 -
The differential interactions of peroxisome proliferator-activated receptor gamma ligands with Tyr473 is a physical basis for their unique biological activities.
Molecular pharmacology.
2007
Academic Article
GET IT
Times cited: 57 -
Conversion of nocathiacin I to nocathiacin acid by a mild and selective cleavage of dehydroalanine.
The Journal of organic chemistry.
2007
Academic Article
GET IT
Times cited: 18 -
A series of novel, potent, and selective histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters.
2006
Academic Article
GET IT
Times cited: 73 -
Design and synthesis of potent and subtype-selective PPARalpha agonists.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
GET IT
Times cited: 18 -
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
GET IT
Times cited: 58 -
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Journal of medicinal chemistry.
2005
Academic Article
GET IT
Times cited: 92 -
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
GET IT
Times cited: 20 -
Selective PPARgamma modulators with improved pharmacological profiles.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
GET IT
Times cited: 67 -
PPARs: therapeutic targets for metabolic disease.
Trends in pharmacological sciences.
2005
Information Resource
GET IT
Times cited: 572 -
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
GET IT
Times cited: 25 -
PPAR ligands: potential therapies for metabolic syndrome.
Current diabetes reports.
2005
Information Resource
GET IT
Times cited: 52 -
A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.
Biochemistry.
2004
Academic Article
GET IT
Times cited: 33 -
Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump.
The Journal of biological chemistry.
2003
Academic Article
GET IT
Times cited: 197 -
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.
Bioorganic & medicinal chemistry letters.
2003
Academic Article
GET IT
Times cited: 10 -
Side-chain homologation of nodulisporic acid: synthesis of potent new dienyl derivatives.
Bioorganic & medicinal chemistry letters.
2002
Academic Article
GET IT
Times cited: 8 -
Nodulisporic acid: its chemistry and biology.
Current topics in medicinal chemistry.
2002
Information Resource
GET IT
Times cited: 24 -
Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity.
The Journal of biological chemistry.
2002
Academic Article
GET IT
Times cited: 145 -
Ivermectin and nodulisporic acid receptors in Drosophila melanogaster contain both gamma-aminobutyric acid-gated Rdl and glutamate-gated GluCl alpha chloride channel subunits.
Biochemistry.
2002
Academic Article
GET IT
Times cited: 82 -
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Bioorganic & medicinal chemistry letters.
2002
Academic Article
GET IT
Times cited: 233 -
Synthesis of side chain truncated 3"-aldehyde, 3"-carboxylic acid, and 1"-aldehyde from nodulisporic acid A.
Organic letters.
2002
Academic Article
GET IT
Times cited: 9 -
Comparison of nodulisporic acid analogs in a Lucilia sericata in vitro assay and a Ctenocephalides felis membrane feeding system.
The Journal of parasitology.
2002
Academic Article
GET IT
Times cited: 6 -
Recent advances in the modulation of voltage-gated ion channels for the treatment of epilepsy.
Current drug targets. CNS and neurological disorders.
2002
Information Resource
GET IT
Times cited: 26 -
Synthesis of nodulisporic acid 2' '-oxazoles and 2' '-thiazoles.
Organic letters.
2001
Academic Article
GET IT
Times cited: 14 -
Systemic efficacy of nodulisporamides against fleas on dogs.
The Journal of parasitology.
2001
Academic Article
GET IT
Times cited: 15 -
Systemic activity of the avermectins against the cat flea (Siphonaptera: Pulicidae).
Journal of medical entomology.
2001
Academic Article
GET IT
Times cited: 22 -
Comparison of ivermectin, doramectin, selamectin, and eleven intermediates in a nematode larval development assay.
The Journal of parasitology.
2001
Academic Article
GET IT
Times cited: 31 -
Systemic efficacy of nodulisporic acid against fleas on dogs.
The Journal of parasitology.
2001
Academic Article
GET IT
Times cited: 40 -
Perspectives in animal health: old targets and new opportunities.
Journal of medicinal chemistry.
2001
Information Resource
GET IT
Times cited: 34 -
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1.
Bioorganic & medicinal chemistry letters.
2001
Academic Article
GET IT
Times cited: 71 -
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
Bioorganic & medicinal chemistry letters.
2001
Academic Article
GET IT
Times cited: 58 -
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.
Journal of medicinal chemistry.
2000
Academic Article
GET IT
Times cited: 59 -
Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor.
The Journal of pharmacology and experimental therapeutics.
2000
Academic Article
GET IT
Times cited: 98 -
Chemical modification of nodulisporic acid A: preliminary structure-activity relationships.
Bioorganic & medicinal chemistry letters.
2000
Academic Article
GET IT
Times cited: 20 -
Nodulisporic acid opens insect glutamate-gated chloride channels: identification of a new high affinity modulator.
Biochemistry.
2000
Academic Article
GET IT
Times cited: 61 -
Synthesis of gem-difluoro-avermectin derivatives: potent anthelmintic and anticonvulsant agents.
Bioorganic & medicinal chemistry letters.
1998
Academic Article
GET IT
Times cited: 10 - Synthesis of 1,19-Aza-1,19-desoxy-avermectin B(1a): The First Avermectin Macrolactam. The Journal of organic chemistry. 1998 Academic Article GET IT
-
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.
Proceedings of the National Academy of Sciences of the United States of America.
1996
Academic Article
GET IT
Times cited: 539 -
Affinity probes for the avermectin binding proteins.
Journal of medicinal chemistry.
1992
Academic Article
GET IT
Times cited: 18 -
Photoaffinity labeling of avermectin binding sites from Caenorhabditis elegans and Drosophila melanogaster.
Proceedings of the National Academy of Sciences of the United States of America.
1992
Academic Article
GET IT
Times cited: 41