Results 211 to 220 of about 9,275 (242)

Scorpion Venom Neurotoxins: Molecular Diversity, Mechanisms, and Drug Scaffolds. [PDF]

Toxins (Basel)
Huang Y, Kamau PM, Wang J, Gao M, Li B.
europepmc   +1 more source

Refining the Na_V1.7 pharmacophore of a class of venom-derived peptide inhibitors via a combination of in silico screening and rational engineering. [PDF]

FEBS Lett
Sharma G, Deuis JR, Jia X, Crawford T, Rahnama S, Undheim EAB, Vetter I, Chin YK, Mobli M.   +8 more
europepmc   +1 more source

Inhibiting Nav1.8 for pain: Lessons from patients and from neurons. [PDF]

Proc Natl Acad Sci U S A
Waxman SG, Vasylyev DV.
europepmc   +1 more source

Carriers ofSCN9Avariants linked to inherited and acquired pain syndromes show no alteration in the prevalence of pain or analgesic usage in the UK Biobank cohort

Newton GW, Charman C, Nickerson AP, Phillips KG, Kless A, Dunham JP, Pickering AE.   +6 more
europepmc   +1 more source

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NaV1.7: A central role in pain

Neuron, 2023
Loss of function of sodium channel NaV1.7 produces pain insensitivity. In this issue, Deng et al.1 show that analgesia after NaV1.7 removal or pharmacological blockade is not driven by enkephalin overexpression. These results underscore the essential role, independent of endogenous opioids, of NaV1.7 for nociceptor firing and pain.
Stephen G. Waxman, Sulayman D. Dib-Hajj
openaire   +2 more sources

Discovery of Pyridyl Urea Sulfonamide Inhibitors of Nav1.7

SSRN Electronic Journal, 2022
NaV1.7 is an actively pursued, genetically validated, target for pain. Recently reported quinolinone sulfonamide inhibitors displayed promising selectivity profiles as well as efficacy in preclinical pain models; however, concerns about off-target liabilities associated with this series resulted in an effort to reduce the lipophilicity of these ...
John R, Butler, Gwenaella, Rescourio, Benjamin C, Milgram, Robert S, Foti, Thomas, Kornecook, Joseph, Ligutti, Bryan D, Moyer, Kristin, Taborn, Beth D, Youngblood, Violeta, Yu, Roman, Shimanovich, Alessandro, Boezio, Matthew, Weiss   +12 more
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Structural basis for NaV1.7 inhibition by pore blockers

Nature Structural & Molecular Biology, 2022
Voltage-gated sodium channel NaV1.7 plays essential roles in pain and odor perception. NaV1.7 variants cause pain disorders. Accordingly, NaV1.7 has elicited extensive attention in developing new analgesics. Here we present cryo-EM structures of human NaV1.7/β1/β2 complexed with inhibitors XEN907, TC-N1752 and NaV1.7-IN2, explaining specific binding ...
Jiangtao Zhang, Yiqiang Shi, Zhuo Huang, Yue Li, Bei Yang, Jianke Gong, Daohua Jiang   +6 more
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Interplay of Nav1.8 and Nav1.7 channels drives neuronal hyperexcitability in neuropathic pain

The Journal of General Physiology
Vasylyev et al. show that the Na+ channel Nav1.8 amplifies DRG neuron excitability close to the activation potential threshold, while Nav1.7 acts closer to resting potential.
D. Vasylyev, P. Zhao, Betsy R. Schulman, S. Waxman   +3 more
semanticscholar   +1 more source

Discovery of Novel Nav1.7-Selective Inhibitors with the 1H-Indole-3-Propionamide Scaffold for Effective Pain Relief

Research
Nav1.7 is considered a promising target for developing next-generation analgesic drugs, given its critical role in human pain pathologies. Although most reported inhibitors with strong in vitro activity and high selectivity share the aryl sulfonamide ...
Gaoang Wang, Hang Wu, Yingying Wang, Xiangying Liu, Shuijiao Peng, Wenxing Wang, Meijing Wu, Yifei Liu, Ercheng Wang, Zhe Wang, Lei Xu, Xiaojian Wang, Wei Yang, Haiyi Chen, Xi Zhou, Tingjun Hou   +15 more
semanticscholar   +1 more source

Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2019
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led to the identification of 4 analogs with hNav1.7 IC50 values under 50 nM.
Yong-Jin, Wu, Brian, Venables, Jason, Guernon, Jie, Chen, Sing-Yuen, Sit, Ramkumar, Rajamani, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Lorin A, Thompson, Carolyn, Dzierba   +13 more
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