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Hit-to-Lead
New horizons in small molecule solubility screening
22 October 2019 | By Halo Labs
Aqueous solubility of small molecule compounds is an essential parameter during the hit-to-lead stage of drug discovery as well as lead optimization and formulation. Low solubility can result in misleading ADMET/DMPK analyses if some fraction of a compound precipitates. Watch on-demand to find out more!
New compound keeps cells alive and functioning in a healthy state
A world-first compound that can keep cells alive and functioning in a healthy state could be revolutionary for medical emergencies.
The challenges of hit-to-lead in drug discovery
A study that identified 12 novel compounds that may prove valuable against new drug targets for leishmaniasis and Chagas disease was not without complication. Here, we discuss the findings but also the challenges the researchers reported in their hit-to-lead study.
High-throughput screening used to discover new class of antibiotics
Researchers have used a high-throughput screening method to test over 125,000 molecules and identify a new class of antibiotics.
High-throughput method used to identify cancer drug candidates
A study using high-throughput screening has revealed some promising compounds that could be used in future cancer treatments.
Drug Target Review – Issue 3 2019
This issue includes an investigation into utilising recombinant antibodies for research, a highlight on protein design using computational methods and an examination of the advances in genomic medicine. Also in the issue are articles on next generation sequencing and upstream bioprocessing.
Compound promotes healing of myelin in nervous system disorders
A compound that promotes the rebuilding of the protective sheath around nerve cells damaged in multiple sclerosis has been developed.
Potential sepsis prevention in burn patients found with novel approach
A new study has demonstrated the possibility of treating antibiotic-resistant Pseudomonas aeruginosa which causes sepsis in burn patients.
The promise and pitfalls of serial femtosecond X-ray crystallography
A report from scientists at the Moscow Institute of Physics and Technology highlights the advantages and disadvantages of serial femtosecond X-ray crystallography. This article investigates the review, focusing on its role in drug development.
Unhealthy gut microbiomes in mice remodelled into more healthy ones
Scientists have shown that there are molecules to remodel the gut microbiome and turn an unhealthful gut into a more healthful one for the first time.
Breast cancer progression may be halted with CRISPR gene editing
A tumour-targeted CRISPR gene editing system encapsulated in a nanogel could halt the growth of triple-negative breast cancer.
Researchers image structure of cancer metastasis target
The structure of a key receptor involved in tumour metastasis has been imaged in a study, providing opportunities to develop cancer treatments.
Cyclisation reaction enables screening of macrocyclic compounds libraries
Libraries of more than 9,000 macrocyclic molecules below 1 KDa have been generated, small enough to cross cell membranes and reach targets.
Osteoporosis in mice reversed with new drug target
A pharmaceutical target has been identified by Duke University that, when activated, can reverse bone degradation caused by osteoporosis.