The Therapeutic Utility of Targeting Cav2 Channels

Cohen, Charles J.; Kraus, Richard L.

doi:10.1007/978-1-4419-9254-3_3

Cited by 1 publication

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References 157 publications

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“…This lack of success conforms to the general decrease in productivity of the drug discovery industry over the past decade. 28,29 The discovery of channel mutants and the availability of transgenic mice may aid in efforts to validate targets, although both of these approaches suffer from limitations due to compensation of loss (or gain) of function by compensating pathways [30][31][32] (Table 2). With a better understanding of both channel properties and localization, the search for specific small molecule drugs should become both more rational and more directed; however, success is probably not imminent.…”

Section: Voltage-gated Calcium Channels As New Drug Targetsmentioning

confidence: 99%

Drug Targets in the Voltage-Gated Calcium Channel Family: Why Some Are and Some Are Not

Triggle

2003

ASSAY and Drug Development Technologies

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The L-type calcium channel antagonists have been, and continue to be, a very successful group of therapeutic agents targeted at cardiovascular disorders, notably angina and hypertension. The discovery that the voltage-gated calcium channels are a large and widely distributed family with important roles in both the peripheral and central nervous systems has initiated a major search for drugs active at other calcium channel types directed at disorders of the central nervous system, including pain, epilepsy, and stroke. These efforts have not been therapeutically successful thus far, and small molecule equivalents of the L-type blockers nifedipine, diltiazem, and verapamil directed at non-L-type channels have not been found. The underlying reasons for this are discussed together with suggestions for new directions, including fertility control, oxygen-sensitive channels, and calcium channel activators.

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Section: Voltage-gated Calcium Channels As New Drug Targetsmentioning

confidence: 99%

Drug Targets in the Voltage-Gated Calcium Channel Family: Why Some Are and Some Are Not

Triggle

2003

ASSAY and Drug Development Technologies

View full text Add to dashboard Cite

show abstract

The Therapeutic Utility of Targeting Cav2 Channels

Cited by 1 publication

References 157 publications

Drug Targets in the Voltage-Gated Calcium Channel Family: Why Some Are and Some Are Not

Drug Targets in the Voltage-Gated Calcium Channel Family: Why Some Are and Some Are Not

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