Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Vajira Weerasena"'
Autor:
Heather B. Miller, Dandepally Srinivasa Reddy, Nagaswamy Kumaragurubaran, Gerald Koelsch, Xiao Ming Xu, Jordan Tang, Lin Hong, Arun K. Ghosh, Robert T. Turner, Sarang Kulkarni, Wanpin Chang, Vajira Weerasena
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1031-1036
Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic beta-secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef874ac124046e9e81fbdc7b40bdb747
https://doi.org/10.1016/j.bmcl.2007.12.028
https://doi.org/10.1016/j.bmcl.2007.12.028
Autor:
Thippeswamy Devasamudram, Christopher B. DeZutter, Vajira Weerasena, Lin Hong, Jordan Tang, Gerald Koelsch, Geoffrey Bilcer, Xiaoming Xu, Arun K. Ghosh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:15-20
A series of novel macrocyclic amide-urethanes was designed and synthesized based upon the X-ray crystal structure of our lead inhibitor (1, OM99-2 with eight residues) bound to memapsin 2. Ring size and substituent effects have been investigated. Cyc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d5f5d5d592fdf40726ab8abaf39068d
https://doi.org/10.1016/j.bmcl.2004.10.084
https://doi.org/10.1016/j.bmcl.2004.10.084
Autor:
Sarang S Kulkarni, Xiaoming Xu, Arun K. Ghosh, Geoffrey Bilcer, Wanpin Chang, Nagaswamy Kumaragurubaran, Gerald Koelsch, Vajira Weerasena, Robert T. Turner, Lin Hong, Jordan Tang
Publikováno v:
Journal of medicinal chemistry. 50(10)
Structure-based design and synthesis of a number of potent and selective memapsin 2 inhibitors are described. These inhibitors were designed based upon the X-ray structure of memapsin 2-bound inhibitor 3 that incorporates methylsulfonyl alanine as th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac03b68b6495efc403a8c0ece140f3a8
https://pubmed.ncbi.nlm.nih.gov/17432843
https://pubmed.ncbi.nlm.nih.gov/17432843
Autor:
Stephen Wong, Jordan Tang, Arun K. Ghosh, Geoffrey Bilcer, Thippeswamy Devasamudram, Gerald Koelsch, Wan-Pin Chang, Huining Da, Brian Gordon, Deborah Downs, Vajira Weerasena
Publikováno v:
Journal of neurochemistry. 89(6)
We have previously reported structure-based design of memapsin 2 (beta-secretase) inhibitors with high potency. Here we show that two such inhibitors covalently linked to a "carrier peptide" penetrated the plasma membrane in cultured cells and inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63088b9973d6629225c4cf0f0b9366ab
https://pubmed.ncbi.nlm.nih.gov/15189343
https://pubmed.ncbi.nlm.nih.gov/15189343
Autor:
Arun K. Ghosh, Geoffrey Bilcer, Vajira Weerasena, Lin Hong, Nagaswamy Kumaragurubaran, Gerald Koelsch, Chun-Feng Liu, Robert T. Turner, Thippeswamy Devasamudram, Hui Lei, Khaja Azhar Hussain, Jordan Tang
Publikováno v:
Journal of the American Chemical Society. 128:5310-5311
The proteolytic enzyme memapsin 2 (β-secretase, BACE-1) has emerged as a leading target for therapeutic intervention of Alzheimer's disease (AD).1 It is one of two proteases that cleave the β-amyloid precursor protein (APP) to generate the 40/42 re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93f364b7b525d6e612801f65e15340a5
https://doi.org/10.1021/ja058636j
https://doi.org/10.1021/ja058636j
Autor:
Gerald Koelsch, Stephen Wong, Brian A. Gordon, Thippeswamy Devasamudram, Wanpin Chang, Vajira Weerasena, Geoffrey Bilcer, Jordan Tang, Arun K. Ghosh, Huining Da, Deborah Downs
Publikováno v:
Neurobiology of Aging. 25:S581
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e4d4a2faabe93cbc7be879e6949c92aa
https://doi.org/10.1016/s0197-4580(04)81932-8
https://doi.org/10.1016/s0197-4580(04)81932-8
Autor:
Arun K. Ghosh, Nagaswamy Kumaragurubaran, Lin Hong, Sarang S. Kulkarni, Xiaoming Xu, Wanpin Chang, Vajira Weerasena, Robert Turner, Gerald Koelsch, Geoffrey Bilcer, Jordan Tang
Publikováno v:
Journal of Medicinal Chemistry; May2007, Vol. 50 Issue 10, p2399-2407, 9p