[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 …
enzyme family has become one of the most important drug targets in the 21 st century. There …
A comprehensive overview of globally approved JAK inhibitors
Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …
Put a ring on it: application of small aliphatic rings in medicinal chemistry
MR Bauer, P Di Fruscia, SCC Lucas… - RSC Medicinal …, 2021 - pubs.rsc.org
Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …
Installing the “magic methyl”–C–H methylation in synthesis
D Aynetdinova, MC Callens, HB Hicks… - Chemical Society …, 2021 - pubs.rsc.org
The selective and efficient C–H methylation of sp2 and sp3 carbon centres has become a
powerful transformation in the synthetic toolbox. Due to the potential for profound changes to …
powerful transformation in the synthetic toolbox. Due to the potential for profound changes to …
Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine
The Janus tyrosine kinase (JAK) family of non-receptor tyrosine kinases includes four
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …
Efficacy and safety of abrocitinib in combination with topical therapy in adolescents with moderate-to-severe atopic dermatitis: the JADE TEEN randomized clinical trial
Importance Dupilumab subcutaneous injection is approved for treating moderate-to-severe
atopic dermatitis (AD) in adolescents, but there has been too little research on an efficacious …
atopic dermatitis (AD) in adolescents, but there has been too little research on an efficacious …
Highly selective inhibition of tyrosine kinase 2 (TYK2) for the treatment of autoimmune diseases: discovery of the allosteric inhibitor BMS-986165
ST Wrobleski, R Moslin, S Lin, Y Zhang… - Journal of Medicinal …, 2019 - ACS Publications
Small molecule JAK inhibitors have emerged as a major therapeutic advancement in
treating autoimmune diseases. The discovery of isoform selective JAK inhibitors that …
treating autoimmune diseases. The discovery of isoform selective JAK inhibitors that …
An overview of JAK/STAT pathways and JAK inhibition in alopecia areata
Alopecia Areata (AA) is a common autoimmune disease characterized by non-scarring hair
loss ranging from patches on the scalp to complete hair loss involving the entire body …
loss ranging from patches on the scalp to complete hair loss involving the entire body …
Cyclobutanes in small‐molecule drug candidates
MR van der Kolk, MACH Janssen, FPJT Rutjes… - …, 2022 - Wiley Online Library
Cyclobutanes are increasingly used in medicinal chemistry in the search for relevant
biological properties. Important characteristics of the cyclobutane ring include its unique …
biological properties. Important characteristics of the cyclobutane ring include its unique …
Oxetanes in drug discovery campaigns
JJ Rojas, JA Bull - Journal of Medicinal Chemistry, 2023 - ACS Publications
The oxetane ring is an emergent, underexplored motif in drug discovery that shows attractive
properties such as low molecular weight, high polarity, and marked three-dimensionality …
properties such as low molecular weight, high polarity, and marked three-dimensionality …