breast cancer

Breastcancertargeting peptide 18–4 is a keratin 1 (KRT1) receptor-targeting peptide with a dissociation constant (Kd) of 0.98 μM. Its amino acid sequence is WxEAAYQrFL, and it is an analogue of the P160 peptide. When covalently bonded with the anticancer peptide MccJ25, it significantly enhances MccJ25 uptake in breast cancer cells and boosts its anticancer efficacy. The IC50 values for this covalent compound are 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR, respectively.

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

Echinomycin (Quinomycin A) is an antitumor antibiotic secondary metabolite isolated from Streptomyces, a quinoxaline antibiotic, a DNA doubly intercalating peptide, and inhibits hypoxia-inducible factor-1 (HIF-1) DNA binding activity. Echinomycin has potential anticancer activity and can be used to study triple-negative breast cancer.

Triptorelin acetate(57773-63-4 free base) (CL 118,532) is used as a GnRH agonist. It decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by causing constant stimulation of the pituitary. Triptorelin acetate(57773-63-4 free base) may be used in the treatment of hormone-responsive cancers such as breast cancer or prostate cancer, precocious puberty, estrogen-dependent conditions, and assisted reproduction.

PMX-53 is a Mas-related gene 2 (MrgX2) agonist and C5aR(CD88) antagonist. PMX-53 reduces atherosclerotic lesions in a mouse model of atherosclerosis, inhibits lung metastasis in a mouse breast cancer model, inhibits C5a-induced hypernociception in rats.

Nelipepimut-S, as an immunogenic peptide from the HER2 protein, is highly expressed in breast cancer.

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Goserelin is a gonadotropin-releasing hormone (GnRH/LHRH) deceptide-like agent that acts as a GnRH agonist. It is suitable for hormone therapy of prostate cancer, premenopausal and perimenopausal breast cancer, endometriosis.

Goserelin acetate (Fertilan) is a synthetic long-acting agonist of gonadotropin-releasing hormone, used in treatments of cancer.

ND1-YL2 is a peptide-based PROTAC®Degrader of steroid receptor co-activator 1 (SRC-1; also known as nuclear receptor coactivator 1, NCOA1). ND1-YL2 is composed of a stapled peptide that binds SRC-1 (YL2) joined by a linker to a tetrapeptide that binds UBR box domains. Upon ternary complex formation, SRC-1 is polyubiquitinated and subsequently degraded via the N-degron pathway. This Degrader induces dose-dependent degradation of SRC-1 in the MDA-MB-231 triple negative breast cancer cell line (DC50 = 10 μM), and binds to the PAS-B domain of SRC-1 (Ki = 320 nM). ND1-YL2 inhibits MDA-MB-231 cell migrationin vitro, and suppresses metastasis of MDA-MB-231 cellsin vivo.

SOR-C13 TFA, a truncated carboxy-terminal peptide, serves as a potent TRPV6 antagonist, demonstrating high affinity with an IC 50 value of 14 nM. TRPV6, a non-voltage-gated calcium channel linked to malignancy and poor prognosis in breast cancer, is effectively targeted by SOR-C13 TFA, indicating its anticancer activity [1].

Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is a luteinizing hormone-releasing hormone (LHRH) analogue with antineoplastic properties, characterized by the peptide sequence KFAKFAKKFAKFAKKFAKQHWSYGLRPG. It is effective in inhibiting breast, ovarian, and prostate cancer xenografts in mouse models [1] [2].

DOTA-CXCR4-L, a peptide targeting the CXCR4 receptor, is utilized in cancer research, notably in the contexts of glioblastoma and triple-negative breast cancer [1].

Azurin (50-77) is a peptide fragment derived from the copper-containing bacterial protein azurin, present in P. aeruginosa. It exhibits properties that regulate the cell cycle, inhibit cancer proliferation, and manage angiogenesis, proving its potential as an anticancer agent. Specifically, this compound acts as a VEGFR2 inhibitor with an IC20 of approximately 10.7 µM. At a concentration of 20 µM, it effectively induces cell cycle arrest at the G2/M phase in MCF-7 breast cancer cells, while a higher concentration of 50 µM significantly reduces the proliferation of both MCF-7 and ZR-75-1 breast cancer cell lines. Furthermore, Azurin (50-77) impedes VEGF-A-induced capillary tube formation with an IC50 of 12 µM, and alters the cellular and extracellular levels of critical signaling and structural proteins such as F-actin, focal adhesion kinase (FAK), paxillin, and platelet endothelial cell adhesion molecule-1 (PECAM-1) in human umbilical vein endothelial cells (HUVECs) at a concentration of 25 µM. Demonstrating its efficacy in vivo, Azurin (50-77) administered at 10 mg/kg per day notably reduces tumor volume in an MCF-7 mouse xenograft model, highlighting its therapeutic potential.

A20FMDV2, a peptide derived from the α-helical RGD cell-interacting domain of the VP1 capsid protein of foot-and-mouth disease virus (FMDV) serotype O, targets and binds αVβ6 integrin. It effectively disrupts αVβ6 integrin-mediated cell adhesion in H357 tongue squamous cell carcinoma cells that exhibit human αVβ6, with an inhibitory concentration (IC50) of 1.2 µM. Additionally, when labeled with 111indium-DTPA, A20FMDV2 (20 MBq) specifically attaches to αVβ6 integrin in a breast cancer mouse xenograft model using MCF10CA1a cells, facilitating targeted radiation imaging analysis.

TC 14012, a peptidomimetic compound, acts as both an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and as an agonist for CXCR7, effectively recruiting β-arrestin in HEK293T cells that express CXCR7 (EC50 = 350 nM). Moreover, it demonstrates significant antiviral activity by reducing the cytopathic effects of HIV in MT-4 cells with an EC50 value of 0.4 nM and inhibiting HIV entry in vitro through a CXCR4-dependent pathway (IC50 = 19.3 nM). Additionally, TC 14012 suppresses chemokine (C-X-C motif) ligand 12 (CXCL12)-induced migration in MDA-MB-231 breast cancer and human umbilical vein endothelial cells (HUVECs) within the 10 to 1,000 nM concentration range. In a mouse model, administration of TC 14012 at 10 mg/kg significantly reduced infarct size following acute myocardial infarction induced by ligation of the left anterior descending (LAD) coronary artery.

Z-VAD is an irreversible pan-caspase inhibitor capable of suppressing multiple caspases including caspase-3, -6, -7, -8, and -9. Z-VAD induces autophagy and necrosis in tumour cells, delays tumour growth, exhibits anti-angiogenic activity, and enhances the sensitivity of breast and lung cancer cells to radiotherapy.

KKI-5 (TFA) is a specific tissue kallikrein inhibitor.Kki-5 (TFA) can reduce breast cancer cell infiltration.

Hemorphin-7 binds to the angiotensin IV receptor, triggering multiple effects including cellular proliferation and memory enhancement. Hemorphins are endogenous peptides belonging to the family of atypical opioid peptides released from hydrolyzed hemoglob

Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cance

FKBPL (FK506-binding protein like)-based peptide. Binds to and upregulates expression of CD44. Inhibits breast cancer stem cell (BCSC) growth. Decreases pluripotency markers and promotes differentiation of BCSCs. Also inhibits endothelial cell migration a

Tumor protein p53 binding protein (53BP1) has been identified in a yeast two-hybrid screen as a protein that interacts with the central DNA–binding domain of p532. Similar to breast cancer susceptibility gene 13, 4 (BRCA1; 53BP1 enhances p53-dependent tra

CBP-1018 is a peptide-drug conjugate (PDC) composed of a dual-targeting ligand for FRα/TRPV6, linked to Monomethylauristatin E. It holds promise for research in the field of breast cancer.