Table 1.

List of CXCR4 Inhibitors

Name of CXCR4 Inhibitors or Analog Designation	Molecular Type	Amino Acid Sequences, Modification Diagrams, or Chemical Structures	Biological Activities	Stage of Development	References
1	d-Peptide	Ac-NH-(d-Arg)9-COOH	Block HIV-1 entry	Phage I	53,72,73
AMD3100	Small Orgnic Molecule		(1) Block HIV-1 entry; (2) promote stem cell migration; (3) inhibit stromal–leukemia cell interactions; and (4) anti-RA and allergic asthma activities	Approved in 2008 for patients with lymphoma and multiple myeloma as a source of hematopoietic stem cells for transplantation	57, 200,111, 117,113,125
2	Small Orgnic Molecule		CXCR4 Antagonist	Pre-clinical	77
AMD3465	Small Orgnic Molecule		Block HIV-1 entry	Pre-clinical	78
3	Small Orgnic Molecule		Block HIV-1 entry	Phase I	80
4	Small Orgnic Molecule		Block HIV-1 entry	Phase I	84
5	Small Orgnic Molecule		Block HIV-1 entry	Pre-clinical	85,86
6	Small Orgnic Molecule		Block HIV-1 entry	Pre-clinical	87
T22	Peptide		(1) Block HIV-1 entry; and (2) anti-RA activities	Pre-clinical	58
T140	Peptide		(1) Block HIV-1 entry; (2) promote stem cell migration; and (3) anti-RA activities	Pre-clinical	88,89,201
TC14012	Peptide		Block HIV-1 entry	Pre-clinical	88
7	Peptide		(1) Block HIV-1 entry; and (2) anti-RA activities	Pre-clinical	89
8	Small Orgnic Molecule		Block HIV-1 entry	Pre-clinical	93
R3G	Small Orgnic Molecule		Block HIV-1 entry	Pre-clinical	203
SDF-1α	Peptide	KPVSLSYRCPCRFFESHVARANVK HLKILNTPNCALQIVARLKNNNRQ VCIDPKLKWIQEYLEKALNK	Block HIV-1 entry	Pre-clinical	59,60,67,69
CTCE-9908	Peptide	KGVSLSYRKRYSLSVGK	Inhibit cancer growth and metastases	Phase II	128-130
vMIP-II	Peptide	LGASWHRPDKCCLGYQKRPLPQV LLSSWYPTSQLCSKPGVIFLTKRGR QVCADKSKDWVKKLMQQLPVTA R	Block HIV-1 entry	Pre-clinical	19,20
V1	Peptide	LGASWHRPDKCCLGYQ KRPLP	Block HIV-1 entry	Pre-clinical	61
DV1	d-Peptide	LGASWHRPDKCCLGYQ KRPLP	Block HIV-1 entry	Pre-clinical	64
9	d-Amino Acid Containing Peptide	LGASWHRPDKCCLGYQKRPLPQVL LSSWYPTSQLCSKPGVIFLTKRGR QVCADKSKDWVKKLMQQLPVTA R	(1) Block HIV-1 entry; and (2) inhibit stromal–leukemia cell interactions	Pre-clinical	98,99,124

^aD-amino acids are shown in italic.