Zobrazeno 1 - 10
of 63
pro vyhledávání: '"Shawn J. Stachel"'
Autor:
Chuan Hong, Noel J. Byrne, Beata Zamlynny, Srivanya Tummala, Li Xiao, Jennifer M. Shipman, Andrea T. Partridge, Christina Minnick, Michael J. Breslin, Michael T. Rudd, Shawn J. Stachel, Vanessa L. Rada, Jeffrey C. Kern, Kira A. Armacost, Scott A. Hollingsworth, Julie A. O’Brien, Dawn L. Hall, Terrence P. McDonald, Corey Strickland, Alexei Brooun, Stephen M. Soisson, Kaspar Hollenstein
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Agonists of the orexin receptor 2 (OX2R) show promise in the treatment of narcolepsy. Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both rec
Externí odkaz:
https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
Autor:
Yuan Tian, Yi Wang, Angela M. Jablonski, Yinghui Hu, Jonathan A. Sugam, Markus Koglin, Shawn J. Stachel, Heather Zhou, Jason M. Uslaner, Sophie Parmentier-Batteur
Publikováno v:
Neurobiology of Disease, Vol 161, Iss , Pp 105548- (2021)
TDP-43 pathology is a hallmark of Amyotrophic Lateral Sclerosis (ALS) and Frontotemporal lobar degeneration (FTLD). Namely, both diseases feature aggregated and phosphorylated TDP-43 containing inclusions in the cytoplasm and a loss of nuclear TDP-43
Externí odkaz:
https://doaj.org/article/10127822ae8a4b869c780c0f430e8e11
Autor:
Corey Strickland, Christina Minnick, Michael J. Breslin, Srivanya Tummala, Kaspar Hollenstein, Alexei Brooun, Vanessa L. Rada, Shawn J. Stachel, Beata Zamlynny, Kira A. Armacost, Dawn L. Hall, Li Xiao, Terrence P. McDonald, Chuan Hong, Kern Jeffrey, Scott A. Hollingsworth, Stephen M. Soisson, Julie A. O'Brien, Andrea T. Partridge, Jennifer M. Shipman, Michael T. Rudd, Noel Byrne
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Nature Communications
Nature Communications
Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain’s ability to control sleep-wake cycles. Current therapies are limited to the management of symptoms with modest effectiveness and substantial adverse effects. Agonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e52de5a726dc2d15e8ae787fb1b0817
https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
https://doaj.org/article/71020c0fdeec442e80fbd53a66967a19
Autor:
Mary Wolf, Idriss Bennacef, Hyking Haley, Terence G. Hamill, G Wesolowski, Shawn J. Stachel, Le T. Duong, Mangay Williams, Diane J. Posavec, Mona Purcell, Eric D. Hostetler, Jeffrey L. Evelhoch, Marie A. Holahan, Daniel Rubins, Laura S. Lubbers, Kerry Riffel
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 64:159-167
The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1d62580f174113b1cfb6b8736aeffe3e
https://doi.org/10.1002/jlcr.3896
https://doi.org/10.1002/jlcr.3896
Autor:
Jonathan A. Sugam, Jason M. Uslaner, Sophie Parmentier-Batteur, Markus Koglin, Angela Marie Jablonski, Yi Wang, Heather Zhou, Yuan Tian, Shawn J. Stachel, Yinghui Hu
Publikováno v:
Neurobiology of Disease, Vol 161, Iss, Pp 105548-(2021)
TDP-43 pathology is a hallmark of Amyotrophic Lateral Sclerosis (ALS) and Frontotemporal lobar degeneration (FTLD). Namely, both diseases feature aggregated and phosphorylated TDP-43 containing inclusions in the cytoplasm and a loss of nuclear TDP-43
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26483812e9293df7d140293b1f92c574
https://pubmed.ncbi.nlm.nih.gov/34752923
https://pubmed.ncbi.nlm.nih.gov/34752923
Autor:
Idriss, Bennacef, Daniel, Rubins, Kerry, Riffel, Mangay, Williams, Diane J, Posavec, Marie A, Holahan, Mona L, Purcell, Hyking D, Haley, Mary, Wolf, Shawn J, Stachel, Laura S, Lubbers, Gregg A, Wesolowski, Le T, Duong, Terence G, Hamill, Jeffrey L, Evelhoch, Eric D, Hostetler
Publikováno v:
Journal of labelled compoundsradiopharmaceuticalsREFERENCES. 64(4)
The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::bdb02b926f3faa356b518eec36f58133
https://pubmed.ncbi.nlm.nih.gov/33226657
https://pubmed.ncbi.nlm.nih.gov/33226657
Autor:
Pravien Abeywickrema, Shawn J. Stachel, Tamara D. Cabalu, Anthony T. Ginetti, Yili Chen, Daniel V. Paone, Michael P. Dwyer, Jonathan E. Wilson, Deping Wang, Alejandro Crespo, Jun Lu, Christopher Joseph Sinz, Gregori J. Morriello, Shimin Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 44:128082
A focused SAR study was conducted on a series of N1-substituted pyrazolopyrimidinone PDE2 inhibitors to reveal compounds with excellent potency and selectivity. The series was derived from previously identified internal leads and designed to enhance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33cfdd9f39e9f739df7e6d6ec5a403b0
https://doi.org/10.1016/j.bmcl.2021.128082
https://doi.org/10.1016/j.bmcl.2021.128082
Publikováno v:
Journal of Neuroscience Methods. 282:34-42
Background NGF signaling through TrkA triggers pathways involved in a wide range of biological effects. Clinical trials targeting either NGF or TrkA are ongoing to treat various diseases in the areas of oncology, neuroscience, and for pain, but there
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1126b00aa11229922f41fb4e04b1197
https://doi.org/10.1016/j.jneumeth.2017.03.001
https://doi.org/10.1016/j.jneumeth.2017.03.001
Autor:
Kausik K. Nanda, Yang Yuan, Celina Zerbinatti, Zhongguo Chen, Yingjie Li, Rada Vanessa L, Zhenhua Wu, Jeanine E. Ballard, Meissner Robert S, D. Jonathan Bennett, Mark T. Bilodeau, Edward J. Brnardic, Jian Li, Jill W. Maxwell, Shawn J. Stachel, Michael T. Rudd, Mali Cosden, Peter Wuelfing, Marie A. Holahan, Andrew J. Cooke, Peter Szczerba, Maria S. Michener, Jun Lu, John J. Renger, Keith Wessner, Daniel J. Klein, Victor N. Uebele, Sokreine Suon, Jason M. Uslaner, Yuntae Kim, Jillian DiMuzio, Gopal Parthasarathy, Xavier Fradera
Publikováno v:
Journal of Medicinal Chemistry. 59:3489-3498
Herein, we describe the development of a functionally selective liver X receptor β (LXRβ) agonist series optimized for Emax selectivity, solubility, and physical properties to allow efficacy and safety studies in vivo. Compound 9 showed central pha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3057877d2db1c62e1e11af7805ba877
https://doi.org/10.1021/acs.jmedchem.6b00176
https://doi.org/10.1021/acs.jmedchem.6b00176
Autor:
Sokreine Suon, Sean M. Smith, Jun Lu, Shawn J. Stachel, Anthony Ginnetti, Michael P. Dwyer, Richard A. Berger, Ashley B. Nomland, Deping Wang, Daniel V. Paone, Henry S. Lange, Jason M. Uslaner, Vanita Puri, Jason T. Drott, Jacob Marcus
[Image: see text] Herein we describe the development of a series of pyrazolopyrimidinone phosphodiesterase 2A (PDE2) inhibitors using structure-guided lead identification and design. The series was derived from informed chemotype replacement based on
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5ff29e465b3abd220abf0218e917554
https://europepmc.org/articles/PMC6088355/
https://europepmc.org/articles/PMC6088355/
