The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.
ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.
The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.
 Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
 Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.
Ziele für Signaling Pathways
- MAPK Signaling(26)
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- DNA Damage/DNA Repair(45)
- PI3K/Akt/mTOR Signaling(36)
- Microbiology & Virology(42)
- Cell Cycle/Checkpoint(154)
- Ubiquitination/ Proteasome(21)
- JAK/STAT Signaling(9)
- TGF-β / Smad Signaling(12)
- GPCR/G protein(3)
- Stem Cell(17)
- Membrane Transporter/Ion Channel(161)
- Cancer Biology(336)
- Endocrinology and Hormones(119)
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- Other Signal Transduction(86)
- Vitamin D Related(0)
- Antibody-drug Conjugate/ADC Related(0)
- Ox Stress Reagents(22)
Produkte für Signaling Pathways
- Bestell-Nr. Artikelname Informationen
- GC19566 N-Nitrosodiethylamine
NLRP3 inflammasome inhibitor
- GC63267 α-Chaconine
α,β-Methyleneadenosine 5'-triphosphate (sodium salt)
α,β-Methyleneadenosine 5'-triphosphate (αβ-methylene ATP) is a phosphonic analog of ATP that is characterized by the replacement of the bridging oxygen atom between the α- and β-phosphate groups with methylene.
Bacteria synthesize the cellular growth factor putrescine through a number of pathways.
- GC65446 α-Amyrin acetate
- GC63268 α-Amyrin palmitate
- GC63269 α-Conotoxin PIA TFA
- GC63723 α-Conotoxin PnIA TFA
- GC39464 α-Cyclodextrin
α-Ecdysone is a prohormone of 20-hydroxy ecdysone, an insect-molting, ecdysteroid hormone.
- GC38042 α-Factor Mating Pheromone, yeast (TFA)
α-GalCer analog 8
α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide.
- GC45207 α-hydroxy Farnesyl Phosphonic Acid α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase).
- GC45208 α-hydroxy Metoprolol α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol.
- GC45210 α-Linolenic Acid (sodium salt) α-Linolenic acid (ALA) is an essential fatty acid found in leafy green vegetables.
- GC45601 α-Linolenic Acid ethyl ester-d5
- GC45602 α-Linolenic Acid-d5 MaxSpec• Standard
- GC63749 α-Lipoic Acid-d5
- GC64563 α-Methylserotonin
- GC45213 α-NETA Choline acetyltransferase (ChAT) mediates the synthesis of the neurotransmitter acetylcholine from acetyl-CoA and choline.
- GC38287 α-Pyridone
- GC63941 α-Solanine
- GC63615 α-Thujone
- GC37980 α-Tocopherol phosphate
α-Truxillic acid can be formed by the dimerization of two molecules of α-trans-cinnamic acid.
- GC38873 α2β1 Integrin Ligand Peptide TFA
- GC62380 αvβ1 integrin-IN-1
- GC62566 αvβ1 integrin-IN-1 TFA
- GC64932 αvβ5 integrin-IN-1
- GC49467 β-Aescin A triterpenoid saponin with diverse biological activities
- GC63273 β-Amyloid (1-14),mouse,rat
- GC63274 β-Amyloid (1-42), (rat/mouse) (TFA)
- GC37984 β-Amyloid (1-42), rat
- GC61394 β-Amyloid (1-42), rat TFA
- GC37991 β-Amyloid 15-21
- GC45603 β-Amyrin
- GC45225 β-Apooxytetracycline β-Apooxytetracycline is a potential impurity found in commercial preparations of oxytetracycline.
- GC60391 β-Casomorphin, bovine TFA
- GC61484 β-Casomorphin, human TFA
- GC62432 β-catenin-IN-2
- GC63275 β-Cryptoxanthin
- GC63276 β-Cyclocitral
- GC45228 β-Cyclodextrin β-Cyclodextrin (β-CD) is a cyclic oligosaccharide that contains seven D-(+)-glucopyranose units and has been used to improve the aqueous solubility of various compounds, especially those containing a phenyl group.
- GC63277 β-Cyclogeraniol
- GC45232 β-D-Glucosamine Pentaacetate β-D-Glucosamine pentaacetate is an N-acetylglucosamine derivative that has been shown to promote hyaluronic acid production.
- GC63278 β-D-Glucose pentaacetate
- GC45230 β-Defensin-3 (human) (trifluoroacetate salt) β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.
- GC45231 β-Defensin-4 (human) (trifluoroacetate salt) β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.
- GC45234 β-Endorphin (1-27) (human) (trifluoroacetate salt) β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors).
- GA24007 β-Endorphin (30-31) (bovine, camel, mouse, ovine) The dipeptide Gly-Gln, which is naturally derived from the posttranslational processing of β-endorphin, exhibited an inhibitory action on cell firing when applied iontophoretically to brainstem neurons in the rat. Moreover, it seems to be a neurotrophic regulator of acetylcholinesterase in the mammalian sympathetic ganglion. Gly-Gln suppressed morphine withdrawal symptoms in rats. Gly-Gln has found use as a Gln source in parenteral nutrition, see also G-1210.
- GC45236 β-Endorphin (rat) β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities.
- GC38030 β-Endorphin, equine (TFA)
- GC64430 β-Glucuronidase-IN-1
- GC62551 β-Hydroxypropiovanillone
- GC49647 β-Hyodeoxycholic Acid (hydrate) A 3β epimer of hyodeoxycholic acid
- GC64619 β-Ionone
- GC62235 β-Lactamase-IN-2
- GC38007 β-Melanocyte Stimulating Hormone (MSH), human TFA
- GC45604 β-Rubromycin
- GC38008 β-Zearalenol
- GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide
- GC38010 γ-Aminobutyric acid
- GC64508 γ-Aminobutyric acid-d6
- GC63279 γ-Glu-Gly TFA
- GC63280 γ-Hexalactone
- GC45238 δ14-Triamcinolone acetonide δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide.
- GC45239 δ4-Abiraterone δ4-Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone.
- GC62708 σ1 Receptor antagonist-1
- GC62067 ω-Conotoxin GVIA TFA
- GA24016 ω-Conotoxin MVIIA ω-Conotoxin MVIIA, originally isolated from the venom of the fish-hunting cone snail Conus magus, is a blocker of voltage-sensitive Ca²? channels in neurons. The peptide has been used to identify different Ca²? channel subtypes in amphibian brain.
- GC64899 ω-Conotoxin MVIIC TFA
- GC63281 ω-Pentadecalactone
- GC45713 (±)-α-Tocopherol Acetate
- GC52010 (±)-10-hydroxy-12(Z),15(Z)-Octadecadienoic Acid An oxylipin gut microbiota metabolite
- GC52013 (±)-10-hydroxy-12(Z)-Octadecenoic Acid An oxylipin and metabolite of linoleic acid
- GC38194 (±)-10-Hydroxycamptothecin
- GC62726 (±)-Amiflamine
- GC34961 (±)-BI-D
- GC60394 (±)-Duloxetine hydrochloride
- GC49515 (±)-Ibuprofen-d3 (sodium salt) An internal standard for the quantification of (±)-ibuprofen
- GC45985 (±)-Indoxacarb
- GC45278 (±)-Ketoprofen-d3
- GC38369 (±)-Leucine
- GC65599 (±)-Leucine-d10
- GC45968 (±)-Liquiritigenin
- GC50708 (±)-ML 209
- GC39271 (±)-Naringenin
- GC49482 (±)-Nornicotine-d4 An internal standard for the quantification of (±)-nornicotine
- GC62727 (±)-Penbutolol-d9 hydrochloride
- GC46008 (±)-Thalidomide-d4
- GC45618 (±)-trans-GK563
- GC64007 (±)-U-50488 hydrate hydrochloride
- GC45269 (±)10(11)-DiHDPA (±)10(11)-DiHDPA is produced from cytochrome P450 epoxygenase action on docosahexaenoic acid.
- GC45270 (±)10(11)-EDP Ethanolamide (±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively).
- GC46000 (•)-Drimenol
- GA20003 ((R)-4-Hydroxy-4-methyl-Orn(FITC)⁷)-Phalloidin Fluorophore-labeled phalloidin used for visualizing the actin cytoskeleton.
- GC45890 (+)-Abscisic Acid-d6
- GC39795 (+)-Afzelechin