Literature DB >> 30139550

Nav1.7 inhibitors for the treatment of chronic pain.

Steven J McKerrall1, Daniel P Sutherlin2.   

Abstract

The voltage gated sodium channel Nav1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive efforts to discover potent, selective, and efficacious Nav1.7 inhibitors for the treatment of chronic pain. This digest will introduce the structure and function of Nav1.7 and highlight the wealth of recent developments on a diverse array of Nav1.7 inhibitors, including optimization of their potency, selectivity, and PK/PD relationships.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Na(v)1.7; Pain; SCN9A; Voltage gated sodium channel

Mesh：

Substances：

Year:  2018        PMID： 30139550     DOI： 10.1016/j.bmcl.2018.08.007

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study in Healthy Volunteers.

Authors:  Michael E Rothenberg; Michael Tagen; Jae H Chang; Janel Boyce-Rustay; Michel Friesenhahn; David H Hackos; Avis Hains; Dan Sutherlin; Michael Ward; William Cho
Journal:  Clin Drug Investig       Date:  2019-09       Impact factor: 2.859

2.  Mapping the Molecular Surface of the Analgesic NaV1.7-Selective Peptide Pn3a Reveals Residues Essential for Membrane and Channel Interactions.

Authors:  Alexander Mueller; Zoltan Dekan; Quentin Kaas; Akello J Agwa; Hana Starobova; Paul F Alewood; Christina I Schroeder; Mehdi Mobli; Jennifer R Deuis; Irina Vetter
Journal:  ACS Pharmacol Transl Sci       Date:  2020-02-19

Review 3.  Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform NaV1.7.

Authors:  John V Mulcahy; Hassan Pajouhesh; Jacob T Beckley; Anton Delwig; J Du Bois; John C Hunter
Journal:  J Med Chem       Date:  2019-05-07       Impact factor: 7.446

4.  Rat NaV1.7 loss-of-function genetic model: Deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers.

Authors:  B Grubinska; L Chen; M Alsaloum; N Rampal; D J Matson; C Yang; K Taborn; M Zhang; B Youngblood; D Liu; E Galbreath; S Allred; M Lepherd; R Ferrando; T J Kornecook; S G Lehto; S G Waxman; B D Moyer; S Dib-Hajj; J Gingras
Journal:  Mol Pain       Date:  2019 Jan-Dec       Impact factor: 3.395

5.  Discovery of a selective, state-independent inhibitor of NaV1.7 by modification of guanidinium toxins.

Authors:  H Pajouhesh; J T Beckley; A Delwig; H S Hajare; G Luu; D Monteleone; X Zhou; J Ligutti; S Amagasu; B D Moyer; D C Yeomans; J Du Bois; J V Mulcahy
Journal:  Sci Rep       Date:  2020-09-09       Impact factor: 4.379

6.  Lacosamide Inhibition of NaV1.7 Channels Depends on its Interaction With the Voltage Sensor Domain and the Channel Pore.

Authors:  Julie I R Labau; Matthew Alsaloum; Mark Estacion; Brian Tanaka; Fadia B Dib-Hajj; Giuseppe Lauria; Hubert J M Smeets; Catharina G Faber; Sulayman Dib-Hajj; Stephen G Waxman
Journal:  Front Pharmacol       Date:  2021-12-21       Impact factor: 5.810

7.  Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.

Authors:  Anthony J Roecker; Mark E Layton; Joseph E Pero; Michael J Kelly; Thomas J Greshock; Richard L Kraus; Yuxing Li; Rebecca Klein; Michelle Clements; Christopher Daley; Aneta Jovanovska; Jeanine E Ballard; Deping Wang; Fuqiang Zhao; Andrew P J Brunskill; Xuanjia Peng; Xiu Wang; Haiyan Sun; Andrea K Houghton; Christopher S Burgey
Journal:  ACS Med Chem Lett       Date:  2021-06-01       Impact factor: 4.632

Review 8.  Synthetic Approaches to Zetekitoxin AB, a Potent Voltage-Gated Sodium Channel Inhibitor.

Authors:  Kanna Adachi; Hayate Ishizuka; Minami Odagi; Kazuo Nagasawa
Journal:  Mar Drugs       Date:  2019-12-26       Impact factor: 5.118

9.  The Specific Effects of OD-1, a Peptide Activator, on Voltage-Gated Sodium Current and Seizure Susceptibility.

Authors:  Ming-Chi Lai; Sheng-Nan Wu; Chin-Wei Huang
Journal:  Int J Mol Sci       Date:  2020-11-04       Impact factor: 5.923
  9 in total

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