The Review

What is Dolastatins (Dolastatin 10 and Dolastatin 15)?

Structure of Dolastatin 10 Dolastatin 10 Systematic name: N,N-Dimethyl-L-valyl-N-amino}propyl]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-L -valinamide Molecular Formula: C42H68N6O6S Molecular weight 785.09092 g/mol Average mass: 785.091 Da Monoisotopic mass: 784.492126 DaStructure of Dolastatin 15 Dolastatin...

What is Centanamycin (ML-970; Indolecarboxamide)?

Chemical name: N--5,6,7-trimethoxy-1H-indole-2-carboxamideCentanamycin, also known as  ML-970, AS-I-145 and NSC 716970, is an indolecarboxamide synthesized as a less toxic analog...

Calicheamicin and DNA-cleaving

Calicheamicins, isolated from Micromonospora echinospora ssp. calichensis, combine unprecedented and extraordinary chemical and biological properties.  This includes activity in the biochemical...
Calicheamicin

What is Calicheamicin?

Calicheamicin (also known as LL-E33288 antibiotics) was first discovered in the mid-1980s by a scientist from American Cyanamid Company’s medical research division, Lederle...

Cytotoxic Agents and Antibody-drug Conjugates

Drug name  Target  Mode of Action  ExampleAuristatins α-Tubulin Prevent tubulin polymerizationMonomethyl Auristatin E (MMAE) Monomethyl Auristatin F (MMAF)Maytansinoids α-Tubulin Prevent tubulin polymerizationCalicheamicins Sequence-specific minor groove of...

What is Cryptophcin analog?

The cryptophycins are a group of cyanobacterial depsipeptides with a remarkable biological activity against multi-drug-resistant(MDR) cancer cells. As a potent...

What is Alpha-Amanitin?

Fig 1.0 Structure of α-Amanitin Systematic name: (cyclic(L)-asparaginyl-4-hydroxy-L-proly-(R)-4,5-dihydroxy-L-isoleucyl-6-hydroxy-2-mercapto-L-tryptophylglycyl-L-isoleucylglycyl-L-cysteinyl) cyclic (4 → 8)-sulfide(R)-S-oxide. Molecular Formula: C39H54N10O14S Molecular weight: 918.97 g/mol Average mass: 918.970 Da Monoisotopic mass: 918.354187 Da CAS Registry: 23109-05-9 Solubility: Soluble in...
Featured Image: Cancer cell Courtesy: © 2018. Fotolia. Used with permission.

What are Cytotoxic Agents?

In this section:Highly potent cytotoxic anticancer agents Mechanism of Toxicity Use in Antibody-drug ConjugatesAuristatins Tubulin polymerase inhibitorMaytansines Tubulin depolymerisationCalicheamicins DNA cleavageDuocarymycins DNA...

What are PEG Peptides?

PEG Peptides are a featured class of PEG-linked peptides which can be used in antibody-drug conjugation (ADC).

What are PEG Linkers?

Hydrophilic poly(ethylene glycol) or PEG-linkers are particularly attractive as a linker for conjugation. Water solubility, lack of toxicity; low immunogenicity...