Increasing space-time-yield, carbon-conversion-efficiency and carbon substrate flexibility in the production of fine chemicals

carbohydrates, ,

Fascinating discovery from BASF on increasing space-time-yield, carbon-conversion-efficiency, and carbon substrate flexibility in the production of fine chemicals. They found a positive effect of increased cAMP levels and/or manipulating the PTS system on the above characteristics achieved by de-regulating adenylate cyclase cyaa by deleting the C-terminal regulatory region leading to increased cAMP levels or deleting the Crr protein activity (carbohydrate repression resistance) which regulates the carbohydrate utilization system. Both lead to increased 2-fucosyllactoe and 6-sialyllactose production (human milk oligosaccharides) and increase carbohydrate usage.
Hartwig Schroeder; Peter Ödman]; Georg Wandrey; Christian Dietzsch; Dominik Satory; Matthew Blankschien; Jens Plassmeier et al.

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Synthesis of an amphiphilic vancomycin aglycone derivative inspired by polymyxins: overcoming glycopeptide resistance in Gram-positive and Gram-negative bacteria in synergy with teicoplanin in vitro

carbohydrates, ,

A fascinating journey in the world of novel glycopeptide antibiotics with stops such as overcoming resistance in Gram-positive and Gram-negative bacteria and combined antiviral and antibiotic effects guided by  Anikó Borbás and her group at University of Debrecen supported by several international KOLs in the field (Ilona Bakai-Bereczki, Ferenc Fenyvesi, Pal Herczegh, Eszter Ostorhazi, Henrietta Papp, Batta Gyula, Ana Mitrović, Janko Kos, István Hajdu, Dávid Bajusz, György Keseru, et al)

See the corresponding articles on nature.com:

Synthesis of an amphiphilic vancomycin aglycone derivative inspired by polymyxins: overcoming glycopeptide resistance in Gram-positive and Gram-negative bacteria in synergy with teicoplanin in vitro

Semisynthetic teicoplanin derivatives with dual antimicrobial activity against SARS-CoV-2 and multiresistant bacteria


Fucosyltransferase-specific inhibition using fucose mimetics

carbohydrates, drug discovery

Fascinating joint invention by Università degli Studi di Firenze and Florida International University – Robert Sackstein MD,PhD, Barbara Richichi, and Kyle Martin.
The specific glycomimetic fucosyltransferase inhibitors created are proposed for treatment of a variety of diseases, like acute inflammatory disease, chronic inflammatory disease, diabetes, cystic fibrosis, or a cancer via a modification of fucosylated cell surface glycoconjugates.

See the full patent here

Sugar-decorated carbon dots: a novel tool for targeting immunomodulatory receptor

carbohydrates, drug discovery,

Griffith University (Oren Cooper, Dechao Chen, Thomas Haselhorst, Joseph Tiralongo et al) and University of Bremen released common findings on creating multivalent siglec probes through the decoration of α(2,6)-sialyllactose ligands on inherently fluorescent carbon dots capable of generating a significant cytotoxic effect on Burkitt’s Lymphoma (BL) Daudi B cells.

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Prostate-specific membrane antigen (PSMA) ligands comprising an amylase cleavable linker

carbohydrates, drug discovery, ,

Using sugars in a prodrug concept is a fascinating idea as these compounds can bring so much to the table like improve stability, PK, or help in targeting. In this patent from Heidelberg University oligosaccharide conjugated prostate-specific membrane antigens are described where the bonds are cleaved by amylase in the body.

See the patent on espacenet

Locked and loaded: β-galactosidase activated photodynamic therapy agent enables selective imaging and targeted treatment of glioblastoma multiforme cancer cells

drug discovery, , ,

Our group has always been fond of photodynamic therapy, and here is a great example of why: β-galactosidase activated PDT for selective imaging and targeted treatment of glioblastoma delivered by Orta Doğu Teknik Üniversitesi / Middle East Technical University and Koç University Gorkem Gunbas Toghrul Almammadov Safacan Kölemen

Full article: https://pubs.acs.org/doi/10.1021/acsabm.2c00484