E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

Proteostasis of islet amyloid polypeptide: a molecular perspective of risk factors and protective strategies for type II diabetes

D Milardi, E Gazit, SE Radford, Y Xu… - Chemical …, 2021 - ACS Publications
The possible link between hIAPP accumulation and β-cell death in diabetic patients has
inspired numerous studies focusing on amyloid structures and aggregation pathways of this …

DNA-encoded chemistry: enabling the deeper sampling of chemical space

RA Goodnow Jr, CE Dumelin, AD Keefe - Nature Reviews Drug …, 2017 - nature.com
DNA-encoded chemical library technologies are increasingly being adopted in drug
discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of …

Utilisation of dietary carbohydrates in farmed fishes: new insights on influencing factors, biological limitations and future strategies

BS Kamalam, F Medale, S Panserat - Aquaculture, 2017 - Elsevier
Carbohydrates are the most abundant class of energy yielding nutrients which is
economically indispensable in commercial fish feed formulations. But, the ability of farmed …

New modalities for challenging targets in drug discovery

E Valeur, SM Guéret, H Adihou… - Angewandte Chemie …, 2017 - Wiley Online Library
Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

Role of zinc homeostasis in the pathogenesis of diabetes and obesity

A Fukunaka, Y Fujitani - International journal of molecular sciences, 2018 - mdpi.com
Zinc deficiency is a risk factor for obesity and diabetes. However, until recently, the
underlying molecular mechanisms remained unclear. The breakthrough discovery that the …

Hepatic insulin clearance: mechanism and physiology

SM Najjar, G Perdomo - Physiology, 2019 - journals.physiology.org
Upon its secretion from pancreatic β-cells, insulin reaches the liver through the portal
circulation to exert its action and eventually undergo clearance in the hepatocytes. In …

RNA display methods for the discovery of bioactive macrocycles

Y Huang, MM Wiedmann, H Suga - Chemical reviews, 2018 - ACS Publications
The past two decades have witnessed the emergence of macrocycles, including macrocyclic
peptides, as a promising yet underexploited class of de novo drug candidates. Both …

Type 2 diabetes as a protein misfolding disease

A Mukherjee, D Morales-Scheihing, PC Butler… - Trends in molecular …, 2015 - cell.com
Type 2 diabetes (T2D) is a highly prevalent and chronic metabolic disorder. Recent
evidence suggests that formation of toxic aggregates of the islet amyloid polypeptide (IAPP) …

Chemical space of DNA-encoded libraries: Miniperspective

RM Franzini, C Randolph - Journal of medicinal chemistry, 2016 - ACS Publications
In recent years, DNA-encoded chemical libraries (DECLs) have attracted considerable
attention as a potential discovery tool in drug development. Screening encoded libraries …