[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update

R Roskoski Jr - Pharmacological research, 2022 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21st century. There …

Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

[HTML][HTML] Payload diversification: a key step in the development of antibody–drug conjugates

L Conilh, L Sadilkova, W Viricel, C Dumontet - Journal of Hematology & …, 2023 - Springer
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that
currently combines the selectivity of monoclonal antibodies with the potency of a payload …

[HTML][HTML] PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …

[HTML][HTML] Toll-like receptor signalling in B cells during systemic lupus erythematosus

S Fillatreau, B Manfroi, T Dörner - Nature Reviews Rheumatology, 2021 - nature.com
B lymphocytes have a central role in autoimmune diseases, which are often defined by
specific autoantibody patterns and feature a loss of B cell tolerance. A prototypic disease …

[PDF][PDF] Mapping the degradable kinome provides a resource for expedited degrader development

KA Donovan, FM Ferguson, JW Bushman, NA Eleuteri… - Cell, 2020 - cell.com
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update

R Roskoski Jr - Pharmacological research, 2021 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, the
protein kinase enzyme family has become one of the most important drug targets in the 21st …

[HTML][HTML] Self-nano-emulsifying drug-delivery systems: From the development to the current applications and challenges in oral drug delivery

AB Buya, A Beloqui, PB Memvanga, V Préat - Pharmaceutics, 2020 - mdpi.com
Approximately one third of newly discovered drug molecules show insufficient water
solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems …

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European Journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …