23953-00-6Relevant articles and documents
COMPOUNDS FOR MALT1 DEGRADATION
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Paragraph 00310, (2018/05/24)
Provided herein are bifunctional compounds that inhibit MALTl and/or promote targeted ubiquitination for the degradation of MALTl. In particular, provided are compounds that can bind MALTl, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALTl, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALTl, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
Hydrophilic Oligo(lactic acid)s Captured by a Hydrophobic Polyaromatic Cavity in Water
Kusaba, Shunsuke,Yamashina, Masahiro,Akita, Munetaka,Kikuchi, Takashi,Yoshizawa, Michito
supporting information, p. 3706 - 3710 (2018/03/05)
Biologically relevant hydrophilic molecules rarely interact with hydrophobic compounds and surfaces in water owing to effective hydration. Nevertheless, herein we report that the hydrophobic cavity of a polyaromatic capsule, formed through coordination-driven self-assembly, can encapsulate hydrophilic oligo(lactic acid)s in water with relatively high binding constants (up to Ka=3×105 m?1). X-ray crystallographic and ITC analyses revealed that the unusual host–guest behavior is caused by enthalpic stabilization through multiple CH–π and hydrogen-bonding interactions. The polyaromatic cavity stabilizes hydrolyzable cyclic di(lactic acid) and captures tetra(lactic acid) preferentially from a mixture of oligo(lactic acid)s even in water.
Chiral tetraphenylethenes as novel dopants for calamitic and discotic liquid crystals
Schreivogel, Alina,Dawin, Ute,Baro, Angelika,Giesselmannb, Frank,Laschat, Sabine
scheme or table, p. 484 - 494 (2010/04/05)
Three series of novel chiral tetraphenylethenes have been prepared: citronellyl-derived ethers 1a, b, lactate-derived ethers 2d, g, h, i and lactate-derived esters 3a-c, e-h. Helical twisting powers (HTPs) were determined for those derivatives of 1-3, whi
Syntheses of isotopically labelled L-?±-amino acids with an asymmetric centre at C-3
Harding, John R.,Hughes, Rachael A.,Kelly, Nicholas M.,Sutherland, Andrew,Willis, Christine L.
, p. 3406 - 3416 (2007/10/03)
Approaches are described to the synthesis of a series of isotopically labelled L-a-amino acids each with an asymmetric centre at C-3, including isoleucine, allo-isoleucine, threonine and allo-threonine. The methods may be simply adapted for the selective incorporation of an isotopic label at each site of L-valine including the selective labelling of either diastereotopic methyl group with carbon-13 and/or deuterium and labelling of the amine with nitrogen-15. ? The Royal Society of Chemistry 2000.
Diastereoselective Conjugate Addition to (+)-Camphorsulfonic Acid Derived Nitroalkenes: Synthesis of α-Hydroxy and α-Amino Acids
Barrett, Anthony G. M.,Braddock, D. Christopher,Christian, Paul W. N.,Pilipauskas, Daniel,White, Andrew J. P.,Williams, David J.
, p. 5818 - 5823 (2007/10/03)
Diastereoselective tandem conjugate addition of both oxygen- and nitrogen-centered nucleophiles to the novel (1S)-10-camphorsulfonic acid derived nitroalkenes 9, 10, and 11 and ozonolysis gave the α-hydroxy and α-amino thiol acid derivatives 12, 13, and 14. In all cases, the (R)-diastereomer was formed as the major component albeit with only modest levels of selectivity (33-71% de). The structures of the products and the stereochemistry of the Michael addition step were unequivocally established by X-ray crystallographic studies of nitroalkenes 9 and 10 and (2S)-12c and (2R)-13a and by alternative syntheses from (S)-alanine, (S)-valine, and ethyl (S)-lactate.
Enantioselective syntheses of α-amino-β-hydroxy acids, [15N]-L-allothreonine and [15N]-L-threonine
Sutherland, Andrew,Willis, Christine L.
, p. 1837 - 1840 (2007/10/03)
The enantioselective synthesis of [15N]-L-allothreonine from ethyl (S)-lactate via methyl (S)-3-methoxymethoxy-2-oxobutanoate 15 is described. The stereogenic centre at C-2 was established by a one-pot, dual enzyme catalysed hydrolysis of the ester (by a lipase) and reductive amination of the ketone of 15 (with leucine dehydrogenase) to give, after deprotection, [15N]-(2S,3S)-2-amino-3-hydroxybutanoic acid as a single diastereomer in 93% yield. [15N]-L-Threonine was prepared by an analogous strategy from methyl (R)-lactate using phenylalanine dehydrogenase in the reductive amination step. This approach may be simply adapted for the incorporation of deuterium and carbon-13.
Comparison of deacylation rates of chymotryptic catalysis within an enantiomeric pair of p-nitrophenyl esters
Tanizawa,Yamada,Itoh,Kanaoka
, p. 2748 - 2749 (2007/10/02)
p-Nitrophenyl esters carrying a chiral acyl group were synthesized. These compounds were shown to meet the requirements of chymotrypsin for both the specific binding and the acylation. Therefore, the behavior of p-nitrophenyl esters with chymotrypsin is c
