[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 …

Phenotypic drug discovery: recent successes, lessons learned and new directions

F Vincent, A Nueda, J Lee, M Schenone… - Nature Reviews Drug …, 2022 - nature.com
Many drugs, or their antecedents, were discovered through observation of their effects on
normal or disease physiology. For the past generation, this phenotypic drug discovery …

QSAR without borders

EN Muratov, J Bajorath, RP Sheridan… - Chemical Society …, 2020 - pubs.rsc.org
Prediction of chemical bioactivity and physical properties has been one of the most
important applications of statistical and more recently, machine learning and artificial …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

R Roskoski Jr - Pharmacological research, 2020 - Elsevier
Because genetic alterations including mutations, overexpression, translocations, and
dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this …

Antipsychotic drug efficacy correlates with the modulation of D1 rather than D2 receptor-expressing striatal projection neurons

S Yun, B Yang, JD Anair, MM Martin, SW Fleps… - Nature …, 2023 - nature.com
Elevated dopamine transmission in psychosis is assumed to unbalance striatal output
through D1-and D2-receptor-expressing spiny-projection neurons (SPNs). Antipsychotic …

[HTML][HTML] Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

FS Willard, JD Douros, MBN Gabe, AD Showalter… - JCI insight, 2020 - ncbi.nlm.nih.gov
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for
the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis …

Properties of FDA-approved small molecule protein kinase inhibitors

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …

[HTML][HTML] Structural insights into the human D1 and D2 dopamine receptor signaling complexes

Y Zhuang, P Xu, C Mao, L Wang, B Krumm, XE Zhou… - Cell, 2021 - cell.com
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …

Revealing the structure of pharmacobehavioral space through motion sequencing

AB Wiltschko, T Tsukahara, A Zeine, R Anyoha… - Nature …, 2020 - nature.com
Understanding how genes, drugs and neural circuits influence behavior requires the ability
to effectively organize information about similarities and differences within complex …

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 …