Joseph Ligutti

Amgen (United States) — United States

Biochemistry, Genetics and Molecular Biology · Life Sciences

18h-index910citations32works0.02yr avg
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Research Topics

Ion channel regulation and function(21), Nicotinic Acetylcholine Receptors Study(7), Receptor Mechanisms and Signaling(6), Cardiac electrophysiology and arrhythmias(5), Pain Mechanisms and Treatments(4)

Publications32 total

Discovery of pyridyl urea sulfonamide inhibitors of NaV1.7
Bioorganic & Medicinal Chemistry Letters·2022· 1 citedOpen Access
Discovery of Pyridyl Urea Sulfonamide Inhibitors of Nav1.7
SSRN Electronic Journal·2022Open Access
Discovery of a selective, state-independent inhibitor of NaV1.7 by modification of guanidinium toxins
Scientific Reports·2020· 40 citedOpen Access
Discovery of a Selective, State-Independent Inhibitor of Na <sub>V</sub> 1.7 by Modification of Guanidinium Toxins
2019· 1 citedOpen Access
CCDC 1947050: Experimental Crystal Structure Determination
The Cambridge Structural Database·2019Open Access
Engineering Na<sub>V</sub>1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics
ACS Chemical Biology·2019· 16 cited
Peptide-Membrane Interactions Affect the Inhibitory Potency and Selectivity of Spider Toxins ProTx-II and GpTx-1
ACS Chemical Biology·2018· 15 cited
Discovery of Tarantula Venom-Derived Na<sub>V</sub>1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis
Journal of Medicinal Chemistry·2018· 31 citedOpen Access
Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V
PLoS ONE·2018· 49 citedOpen Access
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition
Bioorganic & Medicinal Chemistry Letters·2018· 11 citedOpen Access
Engineering Antibody Reactivity for Efficient Derivatization to Generate Na<sub>V</sub>1.7 Inhibitory GpTx-1 Peptide–Antibody Conjugates
ACS Chemical Biology·2017· 28 cited
Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors
Bioorganic & Medicinal Chemistry Letters·2017· 8 citedOpen Access
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement
Bioorganic & Medicinal Chemistry Letters·2017· 20 citedOpen Access
Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7
Journal of Pharmacology and Experimental Therapeutics·2017· 52 cited
Sulfonamides as Selective Na<sub>V</sub>1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Journal of Medicinal Chemistry·2017· 66 citedOpen Access
Sulfonamides as Selective Na<sub>V</sub>1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Journal of Medicinal Chemistry·2017· 49 citedOpen Access
Correction to “Sulfonamides as Selective Na<sub>V</sub>1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable <i>in Vivo</i> Target Engagement”
ACS Medicinal Chemistry Letters·2017
Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent Na<sub>V</sub>1.7 inhibitors
MedChemComm·2016· 6 citedOpen Access
Sulfonamides as Selective Na<sub>V</sub>1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
ACS Medicinal Chemistry Letters·2016· 37 citedOpen Access
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective Na<sub>V</sub>1.7 Inhibitors
Journal of Medicinal Chemistry·2016· 42 citedOpen Access
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Frequent Co-authors

Bryan D. Moyer(21), Erin F. DiMauro(14), Violeta Yu(14), Thomas Kornecook(13), Matthew M. Weiss(13), R. Foti(12), Hanh Nho Nguyen(10), Anruo Zou(9), Robert T. Fremeau(9), Min-Hwa Jasmine Lin(9), Justin K. Murray(8), Stefan McDonough(8), Les P. Miranda(8), Margaret Y. Chu‐Moyer(8), Hua Gao(8), Hakan Günaydin(8), Liyue Huang(8), Daniel S. La(8), Emily A. Peterson(8), Kristin Taborn(8)