Table 1 The uPAR-targeted peptides, small-molecule inhibitors and ligand-targeted toxins

AE105

D-Cha-F-s-r-Y-L-W-S

uPA/uPAR

[102]

AE120

[D-Cha-F-s-r-Y-L-W-S]2-βA-K

uPA/uPAR

[102]

Å6

Ac-KPSSPPEE-Am

uPA/uPAR

[103]

ATF

An amino-terminal fragment of urokinase with EGF-like domain and kringle domain

uPA/uPAR

[104]

U11

VSNKYFSNIHW

uPA/uPAR

[105]

A stable disulfide-bridged cyclic form of the linear peptide uPA_19–31

cyclo^19,31uPA_19–31

uPA/uPAR

[106]

A peptide variant of cyclo^19,31uPA_19–31

cyclo^19,31[D-Cys¹⁹]-uPA_19–31

uPA/uPAR

[107]

WX-360

cyclo^21,29[D-Cys21]-uPA_21–30[S21C;H29C]

uPA/uPAR

[108]

WX-360-Nle

cyclo^21,29[D-Cys21]-uPA_21–30[S21C;K23Nle;H29C]

uPA/uPAR

[108]

M25

PRYQHIGLVAMFRQNTG

uPAR/β1-integrins

[109]

α325

PRHRHMGAVFLLSQEAG

uPAR/Vn

[110]

p25

AESTYHHLSLGYMYTLN-NH₂

uPAR-integrin

uPAR/Vn

[111]

m.P243-251

TASWCQGSH

uPAR/integrin α5β1

[112]

D2A-Ala

IQEGAAGRPKDDR

uPAR/integrin avβ3/a5β1

[113]

PEGylated D2A-Ala

PEG-D2A-Ala

uPAR/integrin avβ3/a5β1

[114]

pERERY-NH₂

Pyro glutamic acid (pGlu)-Arg-Glu-Arg-Tyr-NH₂

fMLF/FPR

[115]

RERF

Ac-Arg-Glu-Arg-Phe-NH₂

SRSRY/FPR

fMLF/FPR

[116]

UPARANT

Ac-L-Arg-Aib-L-Arg-D-Ca(Me)Phe-NH₂

fMLF/FPR

[117]

cyclic SRSRY peptide ([SRSRY])

[Ser-Arg-Ser-Arg-Tyr]^§

SRSRY/FPR1 fMLF/FPR1

[118]

RI-3

Ac-(D)-Tyr-(D)-Arg-Aib-(D)-Arg-NH₂

fMLF/FPR1

[119]

huPA1-48 and muPA1-48

The growth factor domains of human and murine urokinase

Tumour stromal cell uPAR dependent plasminogen activation

[120]

huPA1-48Ig and muPA1-48Ig

Modify huPA1-48 and muPA1-48 with the constant region of human IgG₁

Tumour stromal cell uPAR dependent plasminogen activation

[120]

PEGh1-48 and PEGhm1-48

Human and mouse pegylated uPA1-48

Tumour stromal cell uPAR dependent plasminogen activation

[121]

IPR-456

uPA/uPAR

[122]

IPR-803

uPA/uPAR

[123]

IPR-3011

uPA/uPAR

[124]

IPR-3577

uPA/uPAR

[125]

7

uPAR/uPA_ATF

uPAR/Vn

[126]

LLL-1fsi

uPA/uPAR

[127]

MS#479 [2-(Pyridin-2-ylamino)-quinolin-8-ol]

uPAR/integrin

[128]

MS#305 [2,2′-(methylimino)di (8-quinolinol)]

〹

uPAR/integrin

[128]

Compounds 6

uPAR/Vn

uPAR/FPR

[129]

Compounds 37

uPAR/Vn

uPAR/FPR

[129]

Docosahexaenoic acid (DHA)

suppress uPAR expression

[130]

DTAT

DT and ATF

uPAR

[131, 132]

DTATEGF

ATF, EGF and DT

uPAR, EGFR

[133]

DTAT13

ATF, IL-13 and DT

uPAR, IL-13 receptors

[134, 135]

eBAT (EGFATFKDEL 7mut)

ATF, EGF, truncated PE38 with a terminal lysyl-aspartyl-glutamyl-leucine (KDEL) sequence and eight amino acids representing the seven major epitopes on PE38 were mutated

uPAR, EGFR

[136,137,138,139,140,141]

ATF-SAP

ATF and SAP

uPAR

[142, 143]

PAI-2-N-AIE

PAI-2 and N-AIE

uPAR

[144]

DTU2GMCSF

DT, GM-CSF and uPA

uPAR, GM-CSF receptor

[145]

ATF-PE38

ATF and PE38

uPAR

[146]

ATF-PE38KDEL

ATF and PE38 with a terminal KDEL sequence

uPAR

[146]