Details of the BTS

General Information of Binding Target of SBP (BTS) (ID: ST00552)
BTS Name	Integrin alpha-v-beta-3
BTS Type	Protein
Family	Integrin alpha chain family; Integrin beta chain family
Organism	Homo sapiens (Human)
UniProt ID	P06756, P05106
UniProt Entry	ITAV_HUMAN, ITB3_HUMAN

Synthetic Binding Protein (SBP) Targeting This BTS

SBP Name	Highest Status	Mechanism	Affinity	Application	Details	Ref
Bicyclic peptide anti-Integrin BiRK-1	Research	binder	N.A.	Cancers [ICD-11: 2D4Z]	SBP Info	[1]
Bicyclic peptide anti-Integrin BiRK-2	Research	binder	N.A.	Cancers [ICD-11: 2D4Z]	SBP Info	[1]
Evibody anti-Integrin RGD-7B	Research	Binder	N.A.	Research tool	SBP Info	[2]
Fab anti-Integrin clone 9	Research	Binder	N.A.	Research tool	SBP Info	[3]
Knottin anti-Integrin 6C	Research	Binder	Kd: 15 nM	Solid tumour/cancer [ICD-11: 2A00-2F9Z]	SBP Info	[4]
Knottin anti-Integrin 7A	Research	Binder	Kd: 0.78 nM	Solid tumour/cancer [ICD-11: 2A00-2F9Z]	SBP Info	[4]
Knottin anti-Integrin 7C	Research	Binder	Kd: 2.4 nM	Solid tumour/cancer [ICD-11: 2A00-2F9Z]	SBP Info	[4]
Knottin anti-Integrin 7E	Research	Binder	Kd: 1.6 nM	Solid tumour/cancer [ICD-11: 2A00-2F9Z]	SBP Info	[4]
Knottin anti-Integrin 7J	Research	Binder	Kd: 16 nM	Solid tumour/cancer [ICD-11: 2A00-2F9Z]	SBP Info	[4]
Knottin anti-Integrin AgTx 7C	Research	Binder	N.A.	Imaging agent	SBP Info	[5]
Knottin anti-Integrin AgTx 7C(R21)	Research	Binder	N.A.	Imaging agent	SBP Info	[5]
Knottin anti-Integrin b3A	Research	Inhibitor	Kd: 20 nM	Tools as inhibitors of platelet aggregation	SBP Info	[6]
Knottin anti-Integrin b3I	Research	Inhibitor	Kd: 30 nM	Tools as inhibitors of platelet aggregation	SBP Info	[6]
Knottin anti-Integrin EETI-1.5B	Research	Binder	N.A.	Cancers [ICD-11: 2D4Z]	SBP Info	[7]
Knottin anti-Integrin EETI-2.5D	Research	Binder	N.A.	Cancers [ICD-11: 2D4Z]	SBP Info	[7]
Knottin anti-Integrin EETI-2.5F	Research	Binder	N.A.	Glioma [ICD-11: 2A00.0]	SBP Info	[7]
Macrocyclic peptide anti-Integrin ALOS4	Research	Inhibitor	Kd: 2550 nM	Cancers [ICD-11: 2D4Z]	SBP Info	[8]
Macrocyclic peptide anti-Integrin P5	Research	Antagonist	N.A.	Cancers [ICD-11: 2D4Z]	SBP Info	[9], [10]
Monobody anti-Integrin FNfn10-3JCLI4	Research	Binder	Kd: 0.8 nM	Cancers [ICD-11: 2D4Z]	SBP Info	[11], [12]
Tendamistat-based binder anti-Integrin variants	Research	Binder	N.A.	Research tool	SBP Info	[13]

References

1	Rational Design of a Dual-Targeting Natural Toxin-Like Bicyclic Peptide for Selective Bioenergetic Blockage in Cancer Cells. Bioconjug Chem. 2021 Oct 20;32(10):2173-2183.
2	Development and application of cytotoxic T lymphocyte-associated antigen 4 as a protein scaffold for the generation of novel binding ligands. FEBS Lett. 2000 Jun 23;475(3):225-31.
3	Integrin alphaIIbbeta3-specific synthetic human monoclonal antibodies and HCDR3 peptides that potently inhibit platelet aggregation. FASEB J. 2004 Feb;18(2):361-3.
4	Engineered cystine-knot peptides that bind alpha(v)beta(3) integrin with antibody-like affinities. J Mol Biol. 2009 Jan 30;385(4):1064-75.
5	Engineering agatoxin, a cystine-knot peptide from spider venom, as a molecular probe for in vivo tumor imaging. PLoS One. 2013;8(4):e60498.
6	Cystine-knot peptides engineered with specificities for (IIb)(3) or (IIb)(3) and (v)(3) integrins are potent inhibitors of platelet aggregation. J Mol Recognit. Jan-Feb 2011;24(1):127-35.
7	Engineered cystine knot peptides that bind alphavbeta3, alphavbeta5, and alpha5beta1 integrins with low-nanomolar affinity. Proteins. 2009 Nov 1;77(2):359-69.
8	Novel synthetic cyclic integrin v3 binding peptide ALOS4: Antitumor activity in mouse melanoma models. Oncotarget. 2016 Sep 27;7(39):63549-63560.
9	Crystal structure of the extracellular segment of integrin alpha Vbeta3 in complex with an Arg-Gly-Asp ligand. Science. 2002 Apr 5;296(5565):151-5.
10	N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists. J Med Chem. 1999 Aug 12;42(16):3033-40.
11	Fibronectin type III domain based monobody with high avidity. Biochemistry. 2007 Nov 6;46(44):12656-64.
12	Engineered fibronectin type III domain with a RGDWXE sequence binds with enhanced affinity and specificity to human alphavbeta3 integrin. J Mol Biol. 2003 Mar 7;326(5):1475-88.
13	Use of phage display to probe the evolution of binding specificity and affinity in integrins. Protein Eng. 2003 Jan;16(1):65-72.