Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Patrick B. Mullins"'
Autor:
Anthony D. Keefe, Jeremy S. Disch, Jennifer Duffy, Esther C. Lee, Diana Gikunju, Betty Chan, Benjamin D. Levin, Michael I. Monteiro, Sarah A. Talcott, Anthony Lau, Fei Zhou, Anton Kozhushnyan, Neil E. Westlund, Patrick B. Mullins, Yan Yu, Moritz von Rechenberg, Junyi Zhang, Yelena Arnautova, Yanbin Liu, Ying Zhang, Andrew J. McRiner, Anna Kohlmann, Matthew A. Clark, John W. Cuozzo, Christelle Huguet, Shilpi Arora
Publikováno v:
Cancer Research. 83:5346-5346
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast cancer. Information from DNA-encoded chemical library screening provides a me
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c39832f0b4b2f727dd1b73c76bcc701c
https://doi.org/10.1158/1538-7445.am2023-5346
https://doi.org/10.1158/1538-7445.am2023-5346
Autor:
Diana Gikunju, John W. Cuozzo, Yelena A Arnautova, Sarah A Talcott, Neil Westlund, Andrew J. McRiner, Anthony D. Keefe, Yan Yu, Christelle Huguet, Moritz von Rechenberg, Fei Zhou, Jennifer M Duffy, Shilpi Arora, Esther C.Y. Lee, Ying Zhang, Benjamin Levin, Matthew A. Clark, Jeremy S. Disch, Junyi Zhang, Yanbin Liu, Anton Kozhushnyan, Betty Chan, Anthony C Lau, Michael I Monteiro, Patrick B. Mullins, Anna Kohlmann
Publikováno v:
Journal of Medicinal Chemistry. 64:5049-5066
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast cancer. Information from DNA-encoded chemical library (DECL) screening provid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef7302cad9922daa210279c4d6224ee0
https://doi.org/10.1021/acs.jmedchem.1c00127
https://doi.org/10.1021/acs.jmedchem.1c00127
Autor:
Chakrapani Subramanyam, Gregory W. Kauffman, Patrick B. Mullins, Longfei Xie, Stefanus J. Steyn, John M. Humphrey, Eddie Yang, Patrick Robert Verhoest, Beth C. Vetelino, Tuan P. Tran, Butler Todd W, Benjamin Adam Fish, Martin Pettersson, Kelly R. Bales, Antonia F. Stepan, Christopher J. O’Donnell, Cory Michael Stiff, Kathleen M. Wood, Michael Eric Green, Douglas S. Johnson, Leslie R. Pustilnik, Christopher W. am Ende
Publikováno v:
ACS Medicinal Chemistry Letters. 6:596-601
Herein we describe the design and synthesis of a series of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) for Alzheimer's disease (AD) that achieve good alignment of potency, metabolic stability, and low MDR efflux ratios, while also maintai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf675492957abbcaed313fb175f827aa
https://doi.org/10.1021/acsmedchemlett.5b00070
https://doi.org/10.1021/acsmedchemlett.5b00070
Publikováno v:
Organic Letters. 15:642-645
A facile one-pot synthesis of 3,4-dihydro-1H-pyrido[1,2-a]pyrazine-1,6(2H)-diones (pyridopyrazine-1,6-diones) has been developed which employs a sequential coupling/cyclization reaction of 6-hydroxypicolinic acids and β-hydroxylamines. The transform
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78eb03e19989d9c92b8561808da3a04f
https://doi.org/10.1021/ol303463e
https://doi.org/10.1021/ol303463e
Autor:
Chris Limberakis, David W. Piotrowski, Patrick B. Mullins, Allyn T. Londregan, Kathleen A. Farley
Publikováno v:
Organic Letters. 14:2890-2893
A new and useful procedure for the macrocyclization of linear peptides is described. The natural amino acid side chains of tyrosine (phenol), lysine (alkylamine), and histidine (imidazole) react in an intramolecular fashion with a pendent pyridine-N-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29f6c78c71b0771eca3bf0845777ae08
https://doi.org/10.1021/ol301173m
https://doi.org/10.1021/ol301173m
Autor:
Benjamin Adam Fish, Patrick B. Mullins, Christopher W. am Ende, Thayalan Navaratnam, Tuan P. Tran, Michael Eric Green, Chakrapani Subramanyam, Martin Pettersson, Christopher J. O’Donnell, Kathleen M. Wood, Longfei Xie, Liming Zhang, Douglas S. Johnson, Leslie R. Pustilnik, Kelly R. Bales, Subas M. Sakya, Gregory W. Kauffman, Cory Michael Stiff, Beth C. Vetelino, Ricardo Lira
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2906-2911
We report the discovery and optimization of a novel series of dihydrobenzofuran amides as γ-secretase modulators (GSMs). Strategies for aligning in vitro potency with drug-like physicochemical properties and good microsomal stability while avoiding
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e165d1fced0c65a288f1c260e2c8c06
https://doi.org/10.1016/j.bmcl.2012.02.059
https://doi.org/10.1016/j.bmcl.2012.02.059
Autor:
John N. Freskos, Yvette M. Fobian, Timothy E. Benson, Michael J. Bienkowski, David L. Brown, Thomas L. Emmons, Robert Heintz, Alice Laborde, Joseph J. McDonald, Brent V. Mischke, John M. Molyneaux, Joseph B. Moon, Patrick B. Mullins, D. Bryan Prince, Donna J. Paddock, Alfredo G. Tomasselli, Gregory Winterrowd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:73-77
We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48e643373fd67faba63c23379fdd0447
https://doi.org/10.1016/j.bmcl.2006.09.092
https://doi.org/10.1016/j.bmcl.2006.09.092
Publikováno v:
Organic Process Research & Development. 6:539-546
Penicillin amidohydrolase [EC 3.5.1.11] was used to resolve stereoisomers of a β-amino acid ester (ethyl 3-amino-5-(tri-methylsilyl)-4-pentynoate) by phenylacetylation. After screening commercially available sources of the immobilized enzyme, one wa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4f431b128a95569e8692768c5217f617
https://doi.org/10.1021/op0255130
https://doi.org/10.1021/op0255130
Autor:
James R. Kiefer, Barta Thomas E, Heintz Robert M, Yvette M. Fobian, Daniel P. Becker, Grace E. Munie, Patrick B. Mullins, John M. Molyneaux, Brent V. Mischke, Darren J. Kassab, Louis J. Bedell, John N. Freskos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2823-2825
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d64fc828c6eacfa443f80cdc71c9f154
https://doi.org/10.1016/j.bmcl.2011.03.095
https://doi.org/10.1016/j.bmcl.2011.03.095
Autor:
Chakrapani Subramanyam, Kelly R. Bales, Thayalan Navaratnam, Gregory W. Kauffman, Cory Michael Stiff, Patrick Robert Verhoest, Benjamin Adam Fish, Beth C. Vetelino, Michael Eric Green, Tuan P. Tran, Longfei Xie, Douglas S. Johnson, Leslie R. Pustilnik, Nikolay Pozdnyakov, Christopher W. am Ende, Kathleen M. Wood, Martin Pettersson, Patrick B. Mullins, Christopher J. O’Donnell, Liming Zhang, Subas M. Sakya
Publikováno v:
Journal of medicinal chemistry. 57(3)
Herein we describe the design and synthesis of a novel series of γ-secretase modulators (GSMs) that incorporates a pyridopiperazine-1,6-dione ring system. To align improved potency with favorable ADME and in vitro safety, we applied prospective phys
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b3cdd40c6f74cd4cce9371d25fddf55
https://pubmed.ncbi.nlm.nih.gov/24428186
https://pubmed.ncbi.nlm.nih.gov/24428186