S8: Subtilisin C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

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Overview

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One member of this family has garnered intense interest as a clinical drug target. As liver PCSK9 acts to maintain cholesterol homeostasis, it has become a target of intense interest for clinical drug development. Inhibition of PCSK9 can lower low-density cholesterol (LDL-C) by clearing LDLR-bound LDL particles, thereby lowering circulating cholesterol levels. It is hypothesised that this action may improve outcomes in patients with atherosclerotic cardiovascular disease [4-6]. Therapeutics which inhibit PCSK9 are viewed as potentially lucrative replacements for statins, upon statin patent expiry. Several monoclonal antibodies including alirocumab, evolocumab, bococizumab, RG-7652 and LY3015014 are under development. One RNAi therapeutic, code named ALN-PCS02, is also in development [1-3].

Enzymes

furin, paired basic amino acid cleaving enzyme Show summary » More detailed page

membrane bound transcription factor peptidase, site 1 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 1 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 2 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 4 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 5 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 6 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 7 Show summary » More detailed page

proprotein convertase subtilisin/kexin type 9 Show summary » More detailed page

tripeptidyl peptidase 2 Show summary » More detailed page

References

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How to cite this family page

Database page citation:

S8: Subtilisin. Accessed on 22/08/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=755.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.