Chemoenzymatic synthesis of macrocyclic peptides and polyketides via thioesterase-catalyzed macrocyclization

• Senze Qiao,
• Zhongyu Cheng and
• Fuzhuo Li

Beilstein J. Org. Chem. 2024, 20, 721–733, doi:10.3762/bjoc.20.66

• clinical trials for the treatment of non-small-cell lung cancer and platinum-resistant ovarian cancer, but was halted in phase II due to dose-limiting peripheral neuropathy and limited efficacy in vivo [80]. However, this family of depsipeptides remains of therapeutic significance and has recently been

Simulating the enzymes of ganglioside biosynthesis with Glycologue

• Andrew G. McDonald and
• Gavin P. Davey

Beilstein J. Org. Chem. 2021, 17, 739–748, doi:10.3762/bjoc.17.64

• ganglioside biosynthesis, and altered ganglioside status in cancer, and the effects on network structure are predicted. The simulator is available at the Glycologue website, https://glycologue.org/. Keywords: gangliosides; Glycologue; glycosyltransferases; neuropathy; Svennerholm nomenclature; Introduction

What contributes to an effective mannose recognition domain?

• Christoph P. Sager,
• Deniz Eriş,
• Martin Smieško,
• Rachel Hevey and
• Beat Ernst

Beilstein J. Org. Chem. 2017, 13, 2584–2595, doi:10.3762/bjoc.13.255

• carbohydrate-based drugs. One such example of a therapeutic application can be found in a recent novel approach to treating anti-myelin-associated glycoprotein (anti-MAG) neuropathy, a rare, disabling autoimmune disorder. The use of a multivalent glycopolymer mimicking the natural HNK-1 epitope proved to be a

• valid approach to selectively sequester the autoantibodies associated with anti-MAG neuropathy onset. By applying a multivalent strategy, the inhibitory potential of the monomeric carbohydrate epitope (KD 124–793 μM from individual patient sera) could be improved by up to a factor of 230,000 in the

Brønsted acid-mediated cyclization–dehydrosulfonylation/reduction sequences: An easy access to pyrazinoisoquinolines and pyridopyrazines

• Ramana Sreenivasa Rao and
• Chinnasamy Ramaraj Ramanathan

Beilstein J. Org. Chem. 2017, 13, 428–440, doi:10.3762/bjoc.13.46

• active towards chronic diabetic complications including neuropathy, nephropathy, cataracts and retinopathy [13][14]. On the other hand, piperazinone condensed tetrahydroisoquinolines (THIQs) are widespread in nature with interesting biological activities [15]. They are also found to be building blocks