How beyond rule of 5 drugs and clinical candidates bind to their targets

BC Doak, J Zheng, D Dobritzsch… - Journal of medicinal …, 2016 - ACS Publications
To improve discovery of drugs for difficult targets, the opportunities of chemical space
beyond the rule of 5 (bRo5) were examined by retrospective analysis of a comprehensive …

The journey of multifunctional bone scaffolds fabricated from traditional toward modern techniques

A Bigham, F Foroughi, E Rezvani Ghomi… - Bio-Design and …, 2020 - Springer
As a bone scaffold, meeting all basic requirements besides dealing with other bone-related
issues—bone cancer and accelerated regeneration—is not expected from traditional …

Nuclear receptors: from molecular mechanisms to therapeutics

DE Frigo, M Bondesson, C Williams - Essays in biochemistry, 2021 - portlandpress.com
Nuclear receptors are classically defined as ligand-activated transcription factors that
regulate key functions in reproduction, development, and physiology. Humans have 48 …

Directing evolution of novel ligands by mRNA display

G Kamalinia, BJ Grindel, TT Takahashi… - Chemical Society …, 2021 - pubs.rsc.org
mRNA display is a powerful biological display platform for the directed evolution of proteins
and peptides. mRNA display libraries covalently link the displayed peptide or protein …

Human DNA virus exploitation of the MAPK-ERK cascade

JK DuShane, MS Maginnis - International journal of molecular sciences, 2019 - mdpi.com
The extracellular signal-regulated kinases (ERKs) comprise a particular branch of the
mitogen-activated protein kinase cascades (MAPK) that transmits extracellular signals into …

Identifying ligands at orphan GPCRs: current status using structure‐based approaches

T Ngo, I Kufareva, JLJ Coleman… - British journal of …, 2016 - Wiley Online Library
GPCRs are the most successful pharmaceutical targets in history. Nevertheless, the
pharmacology of many GPCRs remains inaccessible as their endogenous or exogenous …

Why and how have drug discovery strategies in pharma changed? What are the new mindsets?

S Mignani, S Huber, H Tomás, J Rodrigues… - Drug discovery today, 2016 - Elsevier
Highlights•Economic, scientific and strategic challenges of the pharmaceutical industry are
analyzed.•New approaches to increase the output of innovative medicine are …

[HTML][HTML] Nano pharmaceutical delivery in combating colorectal cancer

SK Singh, R Solanki, S Patel - Medicine in Drug Discovery, 2024 - Elsevier
Colorectal cancer (CRC), ranking as the third most common cancer globally, is associated
with a high death rate. The colon, also known as the large intestine, is the site where …

Data sets representative of the structures and experimental properties of FDA-approved drugs

D Douguet - ACS medicinal chemistry letters, 2018 - ACS Publications
Presented here are several data sets that gather information collected from the labels of the
FDA approved drugs: their molecular structures and those of the described active …

Chronological analysis of first-in-class drugs approved from 2011 to 2022: their technological trend and origin

R Okuyama - Pharmaceutics, 2023 - mdpi.com
The discovery and development of first-in-class (FIC) drugs are becoming increasingly
important due to increasing reimbursement pressure and personalized medication. To …