Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H)-Reference-Cited by-同舟云学术

Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H)

Published:2019-03-01 Issue:3 Volume:67 Page:224-235
ISSN:0009-2363
Container-title:Chemical and Pharmaceutical Bulletin
language:en
Short-container-title:CHEMICAL & PHARMACEUTICAL BULLETIN

Author:

Sekimata Katsuhiko¹,Sato Tomohiro²,Sakai Naoki³,Watanabe Hisami³,Mishima-Tsumagari Chiemi³,Taguri Tomonori¹,Matsumoto Takehisa³,Fujii Yoshifumi⁴,Handa Noriko⁴,Honma Teruki²,Tanaka Akiko³,Shirouzu Mikako³,Yokoyama Shigeyuki⁴,Miyazono Kohei⁵,Hashizume Yoshinobu⁶,Koyama Hiroo¹

Affiliation:

1. Drug Discovery Chemistry Platform Unit, RIKEN Center for Sustainable Resource Science

2. Drug Discovery Computational Chemistry Platform Unit, RIKEN Center for Biosystems Dynamics Research

3. Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research

4. Crystallographic Drug Discovery Platform Unit, RIKEN Systems and Structural Biology Center

5. Department of Molecular Pathology, Graduate School of Medicine, The University of Tokyo

6. RIKEN Program for Drug Discovery and Medical Technology Platforms

Publisher

Pharmaceutical Society of Japan

Subject

Drug Discovery,General Chemistry,General Medicine

Link

https://www.jstage.jst.go.jp/article/cpb/67/3/67_c18-00598/_pdf

Reference17 articles.

1. 1) Shore E. M., Xu M., Feldman G. J., Fenstermacher D. A., Cho T. J., Choi I. H., Connor J. M., Delai P., Glaser D. L., LeMerrer M., Morhart R., Rogers J. G., Smith R., Triffitt J. T., Urtizberea J. A., Zasloff M., Brown M. A., Kaplan F. S., Nat. Genet., 38, 525–527 (2006).

2. 2) Cappato S., Giacopelli F., Ravazzolo R., Bocciardi R., Int. J. Mol. Sci., 19, 989 (2018).

3. 3) Buczkowicz P., Hoeman C., Rakopoulos P., Pajovic S., Letourneau L., Dzamba M., Morrison A., Lewis P., Bouffet E., Bartels U., Zuccaro J., Agnihotri S., Ryall S., Barszczyk M., Chornenkyy Y., Bourgey M., Bourque G., Montpetit A., Cordero F., Castelo-Branco P., Mangerel J., Tabori U., Ho K. C., Huang A., Taylor K. R., Mackay A., Bendel A. E., Nazarian J., Fangusaro J. R., Karajannis M. A., Zagzag D., Foreman N. K., Donson A., Hegert J. V., Smith A., Chan J., Lafay-Cousin L., Dunn S., Hukin J., Dunham C., Scheinemann K., Michaud J., Zelcer S., Ramsay D., Cain J., Brennan C., Souweidane M. M., Jones C., Allis C. D., Brudno M., Becher O., Hawkins C., Nat. Genet., 46, 451–456 (2014).

4. 4) Pacifici M., Shore E. M., Cytokine Growth Factor Rev., 27, 93–104 (2016).

5. 5) Mohedas A. H., Xing X., Armstrong K. A., Bullock A. N., Cuny G. D., Yu P. B., ACS Chem. Biol., 8, 1291–1302 (2013).

Cited by 11 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011–2020): Current Status and Future Prospects;Molecules;2022-01-05

2. Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva;Bioorganic & Medicinal Chemistry Letters;2021-04

3. Structural perspective of BMP ligands and signaling;Bone;2020-11

4. Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma;Journal of Medicinal Chemistry;2020-08-11

5. Structural Basis of Activin Receptor-Like Kinase 2 (R206H) Inhibition by Bis-heteroaryl Pyrazole-Based Inhibitors for the Treatment of Fibrodysplasia Ossificans Progressiva Identified by the Integration of Ligand-Based and Structure-Based Drug Design Approaches;ACS Omega;2020-05-12