LTYQDLLQLQYr

Product Name
VEGF-IQ: Ac-LTYQDLLQLQY-{D-Arg}-NH2, Related products Ac-KLTWQELYQLKYKGI-NH2; Ac-KQLLWIRSGDRPWYTS-NH2
Product Quantity
4mg
Catalog Number
LT8211
Molecular Weight
1594.81
Sequence
Ac- LTYQDLLQLQY-{D-Arg}-NH2
Product Description

The ability to control angiogenesis using chemical tools has important applications in various scientific fields. In the search for new proangiogenic molecules, researchers found that a sequence of amino acids in the IQGAP1 protein has similarities to a well-known proangiogenic peptide called the QK peptide. They analyzed a synthetic peptide derived from IQGAP1, Ac-LTYQDLLQLQY-{D-Arg}-NH2, and found it to have biological activity similar to that of VEGF, making it a potential tool for promoting reparative angiogenesis.

Developing molecules that can modulate the VEGF-dependent angiogenic response is crucial for treating diseases related to excessive or insufficient blood vessel formation. Various types of molecules, including antibodies, small organic molecules like tyrosine kinase inhibitors (TKIs), and peptide-like molecules, have been proposed to modulate angiogenesis.

Research on novel peptides for modulating the VEGF/VEGFR molecular system has been active in recent years: Ac-KLTWQELYQLKYKGI-NH2, Ac-LTYQDLLQLQY-{D-Arg}-NH2 and Ac-KQLLWIRSGDRPWYTS-NH2. Different approaches, such as screening of protein sequences and structure-based design, have been used to develop peptides mimicking VEGF/VEGFR binding epitopes.

The VEGF/VEGFR molecular system has been a focus of drug discovery, leading to the development of molecules that can interact with either partner, including antibodies, small organic molecules, and more recently, peptides. The design and characterization of peptides mimicking the VEGF/VEGFR binding interface have deepened our understanding of the molecular recognition involved. It is expected that the design of more sophisticated peptides will lead to valuable drug candidates for biomedical applications in the near future.

Structure-based designed peptides targeting VEGF/VEGFRs.

Peptide Sequence Target Mimicking  Affinity Ref.
- NGIDFNRDKFLFL VEGF VEGFR-2 - []
α/β-VEGF-1 V(β-Val)NK(β3-Phe)NKE(ACPC)CN
(APC)RAIE(Aib)ALDPNL NDQQFH
(Aib)KIW(APC)II(APC)DC 
VEGF Z-VEGF
(VEGF affibody)
Ki = 0.11 μM []
- YY(Abu)AARAWSPYSSTVDAGDFRYWGQ-amide  VEGF Nd42 (anti-VEGF nanobody) KA = 51 × 109 M []
Aib2 V(Aib)PNCDIHV(nL)WEWECFERL  VEGF V114* peptide KD = 4 nM []
Kv114* K(Aib)KKCDIHV(nL)WEWECFERL  VEGF V114* peptide KD = 540 nM []
QK Ac-KLTWQELYQLKYKGI-amide VEGFR1/R2 α1 VEGF-A KD = 64 μM []
MA Ac-KLTWMELYQLAYKGI-amide VEGFR1/R2 α1 VEGF-A KD = 46 μM []
#29 Ac-SSEEFARNWAAIN-amide VEGFR1 α1 VEGF-A IC50 = 0.05 μM []
VGB1 CSWIDVYTRATCQPRPL VEGFR1/R2 α1 VEGF-B - []
Vefin7 KAVSWVDVYTAAT-scaffold  VEGFR1 α1 VEGF-B KD = 0.167 μM []
#16 Ac-EV-cycle(NHCO)3,7[EKFM(O2) K]
VYQRSY-amide
VEGFR1 α1 Vammin IC50 = 36 μM []
#5 Ac-W(αMeAsp)N(αMeAsp)WR(Api)TW-amide  VEGFR1/R2 α1 VEGF-C - []
#6 Ac-(Api)WDN (αMeAsp)WR(Api)TW-amide  VEGFR1/R2 α1 VEGF-C - []
#14 CFQEYPDEIEYICK-amide VEGFR1 L1 VEGF-A IC50 = 50.4 μM []
#18 Ac-CTVELMGTVAKQLVPC-amide VEGFR1 L1 VEGF-B IC50 = 10.4 μM []
#19 CSEYPSEVEHMCS-amide VEGFR1 L1 PlGF IC50 = 56.0 μM []
#2 Ac-CNDEGLEC-amide VEGFR-1 L2 VEGF-A - []
Cyclo-VEGI Cycle(fPQIMRIKPHQGQHIGE) VEGFR1/R2 L3 VEGF-A IC50 = 0.7 μM []
#7 Ac-M-cycle(CH2NHCOCH2)2,10 [GIKPHQGQG]I-amide VEGFR1 L3 VEGF-A IC50 = 93.2 μM []
#8 Acetyl-M(aGly)GIKPHQQ(aGly)I-amide  VEGFR1 L3 VEGF-A IC50 = 42.3 μM []
VEGF-P3CYC Acetyl-ITMQCGIHQGQHPKIRMIC
EMSF-amide
VEGFR2 L3 VEGF-A KD = 11 nM []
HPLW KQLLWIRSGDRPWYYTS VEGFR1/R2 L3 PlGF KD = 32 μM []
HPLC KQCLWIRSGDRPWYCTS VEGFR1/R2 L3 PlGF - []
HPLW2 Ac-KQLL(Bpg)IRSGDRP(OrnN3) YWTS-amide  VEGFR1/R2 L3 PlGF - []
PLGF2 QLLKIRSHDRPSYVE-amide VEGFR1 L3 PlGF KD = 86 μM []
C1C12W3W10 CRWNPRTQSWKC VEGFR2 L3 Vammin - []
#7 c[YYDEGLEE]-amide VEGFR1 L2/α1 VEGF-A IC50 = 39.9 μM []
#3 c[YKDEGLEE]-NHCH2CH2Ph(3,4-diOH) VEGFR1 L2/α1 VEGF-A IC50 = 196 μM []
VG3F KFMDVYQRSY(Ahx)elGedncs(Ahx)ECRPK-amide  VEGFR1 α1/L2/L3 VEGF-A IC50 = 52 μM []
EP6 Ac-E(C-7Ahp-QIMRIKPHQGQHIGET
S)KFMDVYQLKYKGI-amide 
VEGFR1/R2 α1/L3 VEGF-A KD = 139 μM []
VGB CIKPHQGQHICNDE VEGFR1/R2 L2/L3 VEGF-A - []
VGB4 KQLVIKPHGQILMIRYPSSQLEM VEGFR1/R2 L1/L2 VEGF-B + L3 VEGF-A - []

Reference: Di Stasi R, De Rosa L, D'Andrea LD. Structure-Based Design of Peptides Targeting VEGF/VEGFRs. Pharmaceuticals (Basel). 2023 Jun 7;16(6):851. doi: 10.3390/ph16060851. PMID: 37375798; PMCID: PMC10302803.

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