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. Author manuscript; available in PMC: 2016 Apr 20.
Published in final edited form as: Methods Mol Biol. 2015;1324:191–203. doi: 10.1007/978-1-4939-2806-4_13

Table 1.

Pepducin applications and outcomes in diverse human diseases

Pepducin Sequence Target Outcome Ref.
PZ128
  (P1pal-7)		 pal-KKSRALF PAR1 Inhibits platelet aggregation in
  humans and arterial thrombosis
  in primate models, suppresses
  tumor growth, metastasis and
  angiogenesis in mice		 [16–18,
  23,
  44–46]
P1pal-12 pal-RCLSSSAVANRS PAR1 Inhibits platelet aggregation,
  decreases thrombin-induced
  relaxation in rat aortic rings and
  limits pulmonary fibrosis		 [18, 63,
  64]
P1pal-12S pal-RSLSSSAVANRS PAR1 Temporally modulates sepsis
  survival, vascular leakage, and
  DIC		 [33]
P1pal-13 pal-AVANRSKKSRALF PAR1 Temporally modulates sepsis
  survival, vascular leakage, and
  DIC		 [33]
P2pal-18S pal-
  RSSAMDENSEKKRKSAIK		 PAR2 Reduces acute inflammation and
  edema in skin inflammation
  models and reduces the severity
  of experimental biliary
  pancreatitis		 [27, 54]
P4pal-10 pal-SGRRYGHALR PAR4 Inhibits platelet aggregation
  and platelet deposition in guinea
  pig and baboon thrombosis
  models		 [5]
P4pal-i1 pal-ATGAPRLPST PAR4 Inhibits platelet aggregation and
  prolongs the occlusion time in
  guinea pig arterial thrombosis		 [16]
x1/2pal-i3 pal-RTLFKAHMGQKHR CXCR1
CXCR2		 Inhibits neutrophil migration
  toward interleukin-8, decreases
  transmigration of neutrophils
  into the peritoneal cavity,
  reverses the lethal sequelae of
  sepsis and improves survival in
  mice		 [26]
x4pal-i3 pal-HSKGHQKRKALK CXCR4 Completely inhibits the response
  of neutrophils toward SDF-1α		 [26]
x4pal-i1 pal-MGYQKKLRSMTD CXCR4 Completely inhibits the response
  of neutrophils toward SDF-1α,
  mobilizes leukocytes from the
  bone marrow		 [26]
ATI-2341 pal-MGYQKKLRSMTDKYRL CXCR4 Mediates release of granulocyte/
  macrophage progenitor cells
  from the bone marrow		 [29, 34]
KRX-7 myristoyl-GMRPYDANKR S1P3 Induces vasorelaxation and
  fibroblast proliferation		 [58]
Compd 16 myristoyl-GRPYDAN S1P3 Blocks KRX-725 activity [58]
F2pal-16 pal-KIHKKGMIKSSRPLRV FRP2 Activates neutrophils to produce
  superoxide		 [65]
F2Pal-10 pal-KIHKKGMIKS FRP2 Activates neutrophils to produce
  superoxide		 [65]
F2pal-12 pal-KIHKKGMIKSSR FRP2 Inhibits neutrophil chemotaxis and
  superoxide production		 [61]