TY - JOUR

T1 - Acid-sensing ion channels as potential therapeutic targets

AU - Heusser, Stephanie A.

AU - Pless, Stephan A.

PY - 2021

Y1 - 2021

N2 - Tissue acidification is associated with a variety of disease states, and acidsensing ion channels (ASICs) that can sense changes in pH have gained traction as possible pharmaceutical targets. An array of modulators, ranging from small molecules to large biopharmaceuticals, are known to inhibit ASICs. Here, we summarize recent insights from animal studies to assess the therapeutic potential of ASICs in disorders such as ischemic stroke, various pain-related processes, anxiety, and cardiac pathologies. We also review the factors that present a challenge in the pharmacological targeting of ASICs, and which need to be taken into careful consideration when developing potent and selective modulators in the future.

AB - Tissue acidification is associated with a variety of disease states, and acidsensing ion channels (ASICs) that can sense changes in pH have gained traction as possible pharmaceutical targets. An array of modulators, ranging from small molecules to large biopharmaceuticals, are known to inhibit ASICs. Here, we summarize recent insights from animal studies to assess the therapeutic potential of ASICs in disorders such as ischemic stroke, various pain-related processes, anxiety, and cardiac pathologies. We also review the factors that present a challenge in the pharmacological targeting of ASICs, and which need to be taken into careful consideration when developing potent and selective modulators in the future.

KW - SECONDARY HYPERALGESIA

KW - INFLAMMATORY PAIN

KW - ASIC3

KW - NEUROPROTECTION

KW - MUSCLE

KW - INHIBITION

KW - VENOM

KW - PHARMACOLOGY

KW - PEPTIDE

KW - STROKE

U2 - 10.1016/j.tips.2021.09.008

DO - 10.1016/j.tips.2021.09.008

M3 - Review

C2 - 34674886

VL - 42

SP - 1035

EP - 1050

JO - Trends in Pharmacological Sciences

JF - Trends in Pharmacological Sciences

SN - 0165-6147

IS - 12

ER -