Peptide Information

General Information of This Peptide
Peptide ID
PEP00054
Peptide Name
pHLIP (GGEQ)
Structure
Sequence
H2N-GGEQNPIYWARYADWLFTTPLLLLDLALLVDADEGTCG
Peptide Type
Linear
PDC Transmembrane Types Cell-penetrating peptides (CPPs)
Distribution
Acidity is produced not only by cancerous tissue, but also by any tissue that is experiencing hypoxia: the lack of oxygen in the tissue triggers cells to switch to a high rate of the anaerobic, glycolytic energy production pathway, consequently resulting in acidification. pHLIPs have been shown to target infections in lungs, inflammatory arthritis, and ischemic myocardium, a consequence of heart disease, and could be used for diagnosis and treatment thereof. It is also possible that pHLIPs could be used as targeted treatment in ischemic strokes. In contrast to diseased tissue, healthy tissue is typically not associated with increased acidity except in the gastrointestinal tract and kidney, the pHs of which might be regulated by the implementation of a special diet or supplementary drinks if their acidity proves problematic.
Formula
C194H290N46O57S
Isosmiles
[H]NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)N[H])C(=O)N[C@@H](CC(=O)N[H])C(=O)N1CCC[C@H]1C(=O)N[C@]([H])(C(=O)N[C@@H](Cc1ccc(O[H])cc1)C(=O)N[C@@H](Cc1cn([H])c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](Cc1ccc(O[H])cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cn([H])c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@]([H])(C(=O)N[C@]([H])(C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)N[C@]([H])(C(=O)N[C@@H](CS[H])C(=O)NCC(N)=O)[C@@H](C)O[H])C(C)C)[C@@H](C)O[H])[C@@H](C)O[H])[C@@H](C)CC
InChI
InChI=1S/C194H290N46O57S/c1-28-99(20)156(236-187(291)142-47-37-63-239(142)192(296)139(78-144(197)247)232-168(272)121(56-59-143(196)246)214-167(271)120(58-61-150(254)255)211-147(250)87-204-146(249)83-195)189(293)230-131(75-109-50-54-113(245)55-51-109)179(283)226-133(76-110-84-202-116-43-34-32-41-114(110)116)171(275)209-100(21)160(264)212-118(45-36-62-201-194(199)200)166(270)224-130(74-108-48-52-112(244)53-49-108)170(274)208-102(23)162(266)217-137(81-153(260)261)182(286)227-134(77-111-85-203-117-44-35-33-42-115(111)117)180(284)222-126(69-94(10)11)176(280)225-132(73-107-39-30-29-31-40-107)185(289)237-158(105(26)242)191(295)238-159(106(27)243)193(297)240-64-38-46-141(240)186(290)229-128(71-96(14)15)178(282)221-125(68-93(8)9)175(279)219-124(67-92(6)7)174(278)220-127(70-95(12)13)177(281)228-138(82-154(262)263)183(287)218-122(65-90(2)3)169(273)207-101(22)161(265)215-123(66-91(4)5)173(277)223-129(72-97(16)17)184(288)235-155(98(18)19)188(292)231-135(79-151(256)257)172(276)210-103(24)163(267)216-136(80-152(258)259)181(285)213-119(57-60-149(252)253)164(268)206-88-148(251)234-157(104(25)241)190(294)233-140(89-298)165(269)205-86-145(198)248/h29-35,39-44,48-55,84-85,90-106,118-142,155-159,202-203,241-245,298H,28,36-38,45-47,56-83,86-89,195H2,1-27H3,(H2,196,246)(H2,197,247)(H2,198,248)(H,204,249)(H,205,269)(H,206,268)(H,207,273)(H,208,274)(H,209,275)(H,210,276)(H,211,250)(H,212,264)(H,213,285)(H,214,271)(H,215,265)(H,216,267)(H,217,266)(H,218,287)(H,219,279)(H,220,278)(H,221,282)(H,222,284)(H,223,277)(H,224,270)(H,225,280)(H,226,283)(H,227,286)(H,228,281)(H,229,290)(H,230,293)(H,231,292)(H,232,272)(H,233,294)(H,234,251)(H,235,288)(H,236,291)(H,237,289)(H,238,295)(H,252,253)(H,254,255)(H,256,257)(H,258,259)(H,260,261)(H,262,263)(H4,199,200,201)/t99-,100-,101-,102-,103-,104+,105+,106+,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,155-,156-,157-,158-,159-/m0/s1
InChIKey
FJDWZOCTTHZENZ-PQUDPETMSA-N
Pharmaceutical Properties
Molecule Weight
4210.786
Polar area
1635.34
Complexity
4208.092868
xlogp Value
-11.0925
Heavy Count
298
Rot Bonds
136
Hbond acc
54
Hbond Donor
55
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
pHLIP-PAMAM-DOX [Investigative]
 PDC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
15%
Administration Time 72 h
Administration Dosage 10 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
20%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
20%
Administration Time 72 h
Administration Dosage 5.0 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
90%
Administration Time 72 h
Administration Dosage 0.16 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
90%
Administration Time 72 h
Administration Dosage 0.31 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
90%
Administration Time 72 h
Administration Dosage 1.3 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 7 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
95%
Administration Time 72 h
Administration Dosage 0.63 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 8 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
98%
Administration Time 72 h
Administration Dosage 10 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 9 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 10 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 5.0 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
pHLIP-S-S-DOX [Investigative]
 PDC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 18 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
18%
Administration Time 72 h
Administration Dosage 10 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 16 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
20%
Administration Time 72 h
Administration Dosage 1.3 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 13 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
22%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 14 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
22%
Administration Time 72 h
Administration Dosage 5.0 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 15 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
30%
Administration Time 72 h
Administration Dosage 0.31 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
30%
Administration Time 72 h
Administration Dosage 0.63 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 7 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
30%
Administration Time 72 h
Administration Dosage 1.3 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 8 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
38%
Administration Time 72 h
Administration Dosage 0.16 µM
Evaluation Method MTS assay
Description
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).

   Click to Show/Hide
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 9 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
42%
Administration Time 72 h
Administration Dosage 0.63 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 12 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 10 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
45%
Administration Time 72 h
Administration Dosage 0.31 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 11 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 11 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
50%
Administration Time 72 h
Administration Dosage 0.16 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 10 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 12 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
90%
Administration Time 72 h
Administration Dosage 0.63 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 19 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 13 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
95%
Administration Time 72 h
Administration Dosage 0.16 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 17 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 14 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
98%
Administration Time 72 h
Administration Dosage 0.31 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 18 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 15 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
99%
Administration Time 72 h
Administration Dosage 10 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 23 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 16 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 1.3 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 20 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 17 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 21 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 18 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 5.0 µM
Evaluation Method MTS assay
Description
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 22 μM.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
pHLIP-M-DOX [Investigative]
 PDC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
97%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
97%
Administration Time 72 h
Administration Dosage 10 µM
Evaluation Method MTS assay
Description
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
98%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
99%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Cell viability
100%
Administration Time 72 h
Administration Dosage 2.5 µM
Evaluation Method MTS assay
Description
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
In Vitro Model Endocervical adenocarcinoma HeLa cell CVCL_0030
References
Ref 1 Cellular delivery of doxorubicin mediated by disulfide reduction of a peptide-dendrimer bioconjugate. Int J Pharm. 2018 Jul 10;545(1-2):64-73. doi: 10.1016/j.ijpharm.2018.04.027. Epub 2018 Apr 27.