Transbilayer phospholipids molecular imaging

EJNMMI Research

Table 1 Phosphatidylserine-based radiolabelled molecular imaging probes

Molecular target	Molecular probes	AA	MW (kDa)	Affinity (M)	Biological functions	Isotopes	Imaging techniques
PS ^a	annexin V	319	36	10^-9	apoptosis, necrosis, thrombosis	^99mTc, ¹²³I, ¹¹¹In, ⁶⁷Ga, ¹⁸F, ⁶⁸Ga, ¹²⁴I, ⁶⁴Cu, ^94mTc	SPECT(CT), PET(CT)
PS	C2A domain of synaptotagmin I	128	12	10^-9	apoptosis, necrosis	^99mTc	SPECT(CT)
						¹⁸F	PET(CT)
PS ^b	bavituximab chimeric antibody	-	145.3	10^-9	tumour endothelium vasculature imaging	⁷⁴As ^c	PET(CT)
					tumour endothelium vasculature therapy	⁷⁷As ^d	SPECT(CT)
PS	hypericin	-	0.504	-	necrosis	^99mTc, ¹²³I, ¹³¹I ⁶⁴Cu ^e	SPECT(CT) PET(CT)
PS	lactadherin	364	47 - 50	10^-9	apoptosis	^99mTc ^f	SPECT(CT)
PS	PSBP-6	14	1.623	10^-9	apoptosis, necrosis	^99mTc ^g	SPECT(CT)

^a Various linkers have been used for the radiolabelling of annexin V [26]. HYNIC is the most used bifunctional chelating agent in preclinical and clinical research. ^b β2 glycoprotein I domain of phosphatidylserine. ^{c 74}As, β + emitter (T _1/2 = 17.8 days). ^{d 77}As, β- emitter (T _1/2 = 1.6 days). ^e Bis-DOTA has been used as a bifunctional chelating agent for radiolabelling of hypericin. ^f HYNIC has been used as a bifunctional chelating agent for radiolabelling of lactadherin. ^g SAAC has been used as a single amino acid chelator for radiolabelling of PSBP-6. AA, amino acids; MW, molecular weight; PET(CT), positron emission tomography (computed tomography); PS, phosphatidylserine; PSBP-6, PS-binding peptide-6; SPECT(CT), single-photon emission computed tomography (computed tomography).