Peptide Library

The boron atom reversibly binds the active site of the 26S proteasome (mainly the β5 "chymotrypsin-like" subunit), stopping cells from disposing of unwanted proteins; myeloma cells, which make huge amounts of antibody protein, cannot cope…

Binds selectively to glioma and several other tumour cell surfaces — the target is generally attributed to a matrix metalloproteinase-2 complex and chloride channel components — and carries whatever is attached to it (a fluorescent dye, a…

Act at the bombesin receptor family — principally GRP receptor (BB2/GRPR) and neuromedin B receptor (BB1) — which in normal physiology drives gastrin release, gut motility, satiety and itch, and which is heavily over-expressed on several…

The peptide binds somatostatin receptor subtype 2 (SSTR2) on neuroendocrine tumour cells and is internalised; Ga-68 emits positrons that a PET camera detects, while Lu-177 emits short-range beta particles that irradiate the tumour from…

Binds SSTR2 (and SSTR5 to a lesser degree) on neuroendocrine tumour cells; the attached radiometal images or irradiates them

The Glu-urea-Lys head binds the active site of PSMA, an enzyme over-expressed on the surface of most prostate cancer cells; the complex is internalised and the attached isotope images (Ga-68) or irradiates (Lu-177) the cell

Binds SSTR2 (and SSTR5) on neuroendocrine tumour cells; indium-111 gamma rays are detected by a gamma camera at 4 and 24 hours

Binds SSTR2 without activating or internalising it; because antagonists recognise many more receptor conformations than agonists, far more molecules bind per tumour cell, delivering more radiation or a brighter image

Binds FAP, a protease on the surface of cancer-associated fibroblasts in the stroma of most solid tumours (and in some fibrotic and inflamed tissues); the isotope images or irradiates the tumour's supportive tissue rather than the cancer…

RGD is the three-amino-acid sequence that extracellular-matrix proteins use to grip integrin receptors; cyclic RGD peptides bind integrin αvβ3 (and αvβ5) on tumour blood vessels and some tumour cells, either blocking them (cilengitide) or…

Binds the GLP-1 receptor, which is expressed at extremely high density on insulinomas (and on normal pancreatic beta cells), and is internalised; the isotope lets a PET or SPECT camera find tumours that are often under 1 cm and invisible to…

Tilmanocept's mannose groups bind CD206 (the mannose receptor) on macrophages and dendritic cells inside lymph nodes, so it is retained in the first ("sentinel") nodes draining a tumour

Binds the chemokine receptor CXCR4, which is over-expressed on many haematological cancers (myeloma, lymphoma, leukaemia), some solid tumours, aldosterone-producing adrenal adenomas and activated immune cells; the isotope images or…

Blocks the CXCR4 receptor on haematopoietic stem cells, breaking the CXCL12 (SDF-1) "anchor" that holds them in the bone marrow so they spill into the blood where they can be collected

Presents a melanoma-associated peptide to the immune system in a strongly adjuvanted depot so that CD8+ "killer" T cells specific for gp100-bearing melanoma cells expand

Expands HER2-specific CD8+ T cells so they can recognise and kill residual HER2-expressing breast-cancer cells after surgery and chemotherapy

Presents a telomerase fragment to helper (CD4+) T cells, which in turn support CD8+ responses against the telomerase-positive cells found in most cancers; the same peptide also has direct anti-inflammatory and cell-penetrating properties…

Raises CD8+ and CD4+ T-cell and antibody responses against survivin, a protein that blocks cell death and is strongly expressed by glioblastoma and many other cancers but almost absent from normal adult tissue

Immunises the patient against their own EGF so that antibodies mop up circulating EGF and starve EGFR-driven tumours of their growth signal — an antibody-mediated "ligand deprivation" strategy, not a T-cell vaccine

Vaccinates against many tumour antigens at once so that losing any single antigen does not allow the tumour to escape, with cyclophosphamide pre-treatment intended to deplete regulatory T cells first

Raises T cells against the specific mutated KRAS protein driving the patient's tumour — a true tumour-specific target, since the mutation does not exist in normal tissue

Vaccinates each patient against the specific mutations in their own tumour, so the targets are sequences that exist nowhere in normal tissue and against which the immune system has not been tolerised

The lipophilic peptide carries melphalan rapidly into cells, where aminopeptidases cleave it and trap a high concentration of active alkylator inside — especially in myeloma cells, which are rich in those enzymes

The Angiopep-2 peptide binds LRP1 on brain capillary endothelium and is carried across the blood-brain barrier by receptor-mediated transcytosis, taking its chemotherapy payload with it