Cryptophycins
WebFeb 21, 2024 · The cryptophycins are a family of macrocyclic depsipeptide natural products that display exceptionally potent antiproliferative activity against drug-resistant cancers. WebFeb 21, 2024 · The cryptophycins are a family of macrocyclic depsipeptide natural products that display exceptionally potent antiproliferative activity against drug-resistant cancers.
Cryptophycins
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WebFeb 15, 2015 · Cryptophycin Antibody drug conjugates (ADCs) are currently an emerging class of treatment for targeted therapies against cancer.1, 2, 3, 4 ADCs consist of an … Cryptophycins are a family of macrolide molecules that are potent cytotoxins and have been studied for potential antiproliferative properties useful in developing chemotherapy. They are members of the depsipeptide family. See more Cryptophycins were originally discovered in 1990 in cyanobacteria of the genus Nostoc. Cryptophycins were patented as antifungal agents with an unknown mechanism of action and subsequently identified as See more Cryptophycins are potent microtubule inhibitors, with a mechanism of action similar to that of vinca alkaloids. Treatment of cells … See more Cryptophycins were first isolated from cyanobacteria but have subsequently been produced by chemical synthesis. Chemoenzymatic syntheses have also been reported. See more Members of the cryptophycin family have been studied as anti-tumor agents. Cryptophycin-52, a synthetic analog of natural product cryptophycins also known as LY355703, reached See more
WebCryptophycins were found to induce apoptosis due to inhibition of the microtubule dynamics. Consequently, cryptophycin analogues are considered as potential antitumour agents. Retrosynthetically, cryptophycins can be subdivided into four building blocks, namely units A–D, to be assembled in the total synthesis. WebCryptophycins, naturally occurring cytotoxic cyclo -depsipeptides, have been modified by total synthesis to provide analogues suitable for conjugation to peptide-based homing devices. An array of functionalized β 2 -amino acids …
WebFeb 15, 2015 · The cryptophycins are a potent class of cytotoxic agents that were evaluated as antibody drug conjugate (ADC) payloads. Free cryptophycin analog 1 displayed cell activity an order of magnitude more potent than approved ADC payloads MMAE and DM1. This potency increase was also reflected in the activity of the cryptophycin ADCs, … WebThe invention provides methods and compositions to detect expression of one or more biomarkers for identifying and treating patients having glioblastomas who are likely to be responsive to VEGF antagonist therapy. The invention also provides kits and articles of manufacture for use in the methods.
WebThis invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding …
WebSep 21, 2010 · Both new cryptophycin derivatives show high biological activity in cytotoxicity assays. Supporting Information General information, 1 H and 13 C NMR … flannel hair colorWebMar 1, 2002 · The cryptophycins are a unique family of 16‐membered macrolide antimitotic agents isolated from the cyanobacteria Nostoc sp. Their molecular target is tubulin … can school cause insanityWebOct 20, 2009 · Cryptophycins are a family of highly cytotoxic, cyclic depsipeptides. They display antitumour activity that is largely maintained for multi-drug-resistant tumour cells. … flannel guys with beardsWebcryptophycins can be divided into the four building blocks unit A–D being amino or hydroxycarboxylic acids, respectively. Unit A is an α,β-unsaturated δ-hydroxy carboxylic acid typical for cryptophycins. In cryptophycin-1, this building block contains a benzylic β-epoxide, while many cryptophycin derivatives isolated can school buses stop on the highwayWebAbstract. Cryptophycin 1 is a natural product that was initially isolated from blue-green algae which has shown potent broad spectrum antitumor activity in preclinical in vitro … flannel half bleached menWebOct 20, 2009 · Cryptophycins are a family of highly cytotoxic, cyclic depsipeptides. They display antitumour activity that is largely maintained for multi-drug-resistant tumour cells. Cryptophycins are composed of four building blocks (units A–D) that correspond to the respective amino and hydroxy acids. flannel hair scarfWebCryptophycin styrenes 7 and β-epoxides 6, bearing diverse side chains in fragment “B”, were evaluated for cytotoxic activity. β-Epoxides 6, in general, were significantly more potent than the corresponding α-epoxides 17 and styrenes 7. flannel hair images