Pharmaceutical composition comprising a gamma-cyclodextrin-based polymer

drug discovery

today’s cyclodextrin:
it makes me particularly happy to post about the recent success of Heegon Kim and RENATUS, as I have known and admired Heegon’s work for a while and we share a vision of the importance of developing CD-based therapies. Renatus develops gamma-cyclodextrin-based polymer to prevent or treat cholesterol metabolism-related diseases to minimize cell membrane cholesterol extraction, thus exhibiting an excellent anti-inflammatory effect by causing no cytotoxicity and hemolytic activity, making intracellular cholesterol metabolism and release easy and effectively inhibiting the release of IL-1β, MCP-1, and TNF-α.

See the complete patent here: PHARMACEUTICAL COMPOSITION COMPRISING GAMMA-CYCLODEXTRIN POLYMER AND USE THEREOF


Discovery of potent 1,1-diarylthiogalactoside glycomimetic inhibitors of Pseudomonas aeruginosa LecA with antibiofilm properties

carbohydrates, drug discovery,

This great research team recently presented a new series of 1,1-diarylthiogalactoside for targeting the Pseudomonas aeruginosa LecA. The highest affinity (Kd = 160 nM) was obtained for a divalent ligand containing two galactoside units. A monovalent ligand displayed high affinity toward LecA (Kd = 1 μM) and strong antibiofilm activity while others induced a significant antibiofilm activity with no associated bactericidal activity.
Alexandre Bruneau, Emilie Gillon, Aurélie Furiga, Etienne BRACHET, Mouad Alami, Christine Roques, Annabelle Varrot, Anne Imberty, Samir Messaoudi 

See the full article here: Discovery of potent 1,1-diarylthiogalactoside glycomimetic inhibitors of Pseudomonas aeruginosa LecA with antibiofilm properties

Discovery of natural-product-derived sequanamycins as potent oral anti-tuberculosis agents

carbohydrates, drug discovery

Amazing research on the drug discovery of a series of macrolides called sequanamycins (bacterial ribosome inhibitors) with outstanding in vitro and in vivo activity against Mycobacterium tuberculosis (Mtb). The mechanism of action is similar to that of erythromycin and clarithromycin, but with binding characteristics that allow them to overcome the inherent macrolide resistance of Mtb. SEQ-9 was efficacious in mouse models of acute and chronic TB as a single agent, and it demonstrated bactericidal activity in a murine TB infection model in combination with other TB drugs. These results support further investigation of this series as TB clinical candidates, with potential use in new regimens against drug-susceptible and drug-resistant TB.
Sanofi, Texas A&M University, Evotec – Jidong ZHANG, Kwame Amaning, Zhicheng (Z.Chen) Cui, Scott Franzblau, Florence Bordon-Pallier, Cathy Cantalloube, Stefaan Sansen, Laurent Fraisse, Alexey Rak, Lasse Jenner, Gulnara YUSUPOVA, Junjie Zhang, Takushi Kaneko, Nader Fotouhi, Sandeep Tyagi, Fabrice B., Anna Upton, James Sacchettini and Sophie LAGRANGE, PhD

See the full article here.

Targeting galectin-driven regulatory circuits in cancer and fibrosis

carbohydrates, drug discovery,

Comprehensive summary from Gabriel Rabinovich Karina V. Marino Alejandro Cagnoni Diego Croci Russo (University of Buenos Aires) on the array of galectin-targeted strategies, including small-molecule carbohydrate inhibitors, natural polysaccharides and their derivatives, peptides, peptidomimetics, and biological agents reviewing the results of clinical trials that aim to evaluate the efficacy of galectin inhibitors in patients with idiopathic pulmonary fibrosis, nonalcoholic steatohepatitis, and cancer.

See the full article on nature.com.

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

Glycan-modified nucleic acids, methods of preparation, and therapeutic uses

drug discovery

Fantastic chemistry making glyconucleic acids, such as glycoRNA and glycoDNA using the now world-famous click chemistry to treat diseases such as inflammation disorder, an autoimmune disease, cancer, metabolic disease, clotting disease, anti-clotting disease, allergy, viral disease, and microbial infection.
Ryan Flynn; Ciaran Lawlor; Namita Bisaria, Ph.D.; Richard Cummings; Carolyn Bertozzi et al

See the full patent on Espacenet.

Using heparan sulfate octadecasaccharide (18-mer) as a multi-target agent to protect against sepsis

drug discovery,

Fascinating research from University of North Carolina at Chapel Hill, The State University of New York and Rensselaer Polytechnic Institute on using heparan sulfate octadecasaccharide (18-mer) as a multi-target agent to protect against sepsis.

Yongmei Xu, Katelyn Arnold, Fuming Zhang, Vijayakanth Pagadala, Robert Linhardt et al.

See the full article here.