Table 1

Function and dysfunction of human serpins

Serpin
Alternative name(s)
Protease target or function
Involvement in disease

SERPINA1
Antitrypsin
Extracellular; inhibition of neutrophil elastase
Deficiency results in emphysema: polymerization and retention in the ER results in cirrhosis [14,64,65]
SERPINA2
Antitrypsin-related protein
Not characterized, probable pseudogene

SERPINA3
Antichymotrypsin
Extracellular; inhibition of cathepsin G
Deficiency results in emphysema (see [61] for a review)
SERPINA4
Kallistatin (PI4)
Extracellular, inhibition of kallikrein [68]

SERPINA5
Protein C inhibitor (PAI-3)
Extracellular; inhibition of active protein C (see [69] for a review)
Angioedema
SERPINA6
Corticosteroid-binding globulin
Extracellular; non-inhibitory; cortisol binding
Deficiency linked to chronic fatigue [83,84]
SERPINA7
Thyroxine-binding globulin
Extracellular; non-inhibitory, thyroxine binding
Deficiency results in hypothyroidism [85]
SERPINA8
Angiotensinogen
Extracellular; non-inhibitory; amino-terminal cleavage by the protease renin results in release of the decapeptide angiotensin I
Certain variants linked to essential hypertension [86]
SERPINA9
Centerin
Extracellular; maintenance of naive B cells [70]

SERPINA10
Protein Z-dependent proteinase inhibitor
Extracellular; inhibition of activated factor Z and XI
Deficiency linked to venous thromboembolic disease [87]
SERPINA11
XP_170754.3
Not characterized

SERPINA12
Vaspin
Extracellular; insulin-sensitizing adipocytokine [71]

SERPINA13
XM_370772
Not characterized

SERPINB1
Monocyte neutrophil elastase inhibitor
Intracellular; inhibition of neutrophil elastase [72]

SERPINB2
Plasminogen activator inhibitor-2 (PAI2)
Intracellular; inhibition of uPA (see [73] for a review)

SERPINB3
Squamous cell carcinoma antigen-1
Intracellular; cross-class inhibition of cathepsins L and V [6]

SERPINB4
Squamous cell carcinoma antigen-2
Intracellular; cross-class inhibition of cathepsin G and chymase [74]

SERPINB5
Maspin
Intracellular; non-inhibitory; inhibition of metastasis through uncharacterized mechanism
Downregulation and/or intracellular location linked to tumor progression and overall prognosis [10]
SERPINB6
Proteinase inhibitor-6 (PI6)
Intracellular, inhibition of cathepsin G [75]

SERPINB7
Megsin
Intracellular; megakaryocyte maturation [76]
IgA nephropathy
SERPINB8
Cytoplasmic antiproteinase 8 (PI8)
Intracellular; inhibition of furin [77]

SERPINB9
Cytoplasmic antiproteinase 9 (PI9)
Intracellular, inhibition of granzyme B [78]

SERPINB10
Bomapin (PI10)
Intracellular; inhibition of thrombin and trypsin [79]

SERPINB11
Epipin
Intracellular

SERPINB12
Yukopin
Intracellular; inhibition of trypsin [80]

SERPINB13
Headpin (PI13)
Intracellular; inhibition of cathepsins L and K

SERPINC1
Antithrombin
Extracellular; thrombin and factor Xa inhibitor
Deficiency results in thrombosis (see [88] for review)
SERPIND1
Heparin cofactor II
Extracellular; thrombin inhibitor
May contribute to thrombotic risk when combined with other deficiencies [89]
SERPINE1
Plasminogen activator inhibitor I (PAI1)
Extracellular; inhibitor of thrombin, uPA, tPA and plasmin
Abnormal bleeding [90]
SERPINE2
Protease nexin I (PI7)
Extracellular; inhibition of uPA and tPA

SERPINE3
Hs.512272
Not characterized

SERPINF1
Pigment epithelium derived factor
Non-inhibitory; potent anti-angiogenic molecule [81]

SERPINF2
Alpha-2-antiplasmin
Extracellular; plasmin inhibitor
Unrestrained fibrinolytic activity, bleeding [91]
SERPING1
C1 inhibitor
C1 esterase inhibitor
Angioedema [92]
SERPINH1
47kDa heat-shock protein
Non-inhibitory molecular Chaperone for collagens [9]

SERPINI1
Neuroserpin (PI12)
Extracellular; inhibitor of tPA, uPA and plasmin
Polymerization results in dementia [17]
SERPINI2
Myoepithelium-derived serine proteinase inhibitor (PI14)
Extracellular; inhibition of cancer metastasis [82]


Law et al. Genome Biology 2006 7:216   doi:10.1186/gb-2006-7-5-216