Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Rama K. Kondru"'
Autor:
Rama K. Kondru, Sung-Sau So, Andreas Kuglstatter, Yan Lou, Francisco Javier Lopez-Tapia, Christine E. Brotherton-Pleiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(9)
A seven-membered cyclic chiral analog of potent lead BTK inhibitor 1 was envisioned by structure-based design to lock the molecule into its bioactive conformation. For the elaboration of the seven-membered ring, compound 1 pyridone 6-position was sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0cd98e01670ec9b018467c9ef23adc8
https://pubmed.ncbi.nlm.nih.gov/30857747
https://pubmed.ncbi.nlm.nih.gov/30857747
Autor:
Judy M. Suh, Sandra Frauchiger, Michael Soth, Xiaochun Han, Ronald J. Hill, Buelent Kocer, Taygerly Joshua Paul Gergely, Jaehyeon Park, Hong Jun-Bae, Andreas Kuglstatter, Rama K. Kondru, Tobias Gabriel, Renee Litman, Yan Lou, Zachary Kevin Sweeney, Mcintosh Joel, Nolan James Dewdney, Dana Davis, David Michael Goldstein, Timothy D. Owens, Hasim Zecic, Keshab Sarma
Publikováno v:
Journal of Medicinal Chemistry. 58:512-516
Structure-based drug design was used to guide the optimization of a series of selective BTK inhibitors as potential treatments for Rheumatoid arthritis. Highlights include the introduction of a benzyl alcohol group and a fluorine substitution, each o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2706725af4b785142b07ad80c3bfd24
https://doi.org/10.1021/jm500305p
https://doi.org/10.1021/jm500305p
Autor:
Yonglin Ren, Ryan Craig Schoenfeld, Adrian J. Fretland, Maria E. Fuentes, Kung-Ching Chang, Yimin Qian, Rachid Hamid, Yun Chen, Achyutharao Sidduri, Matthew Michael Hamilton, Christopher S. Stevenson, Gabriel Stephen Deems, Lin Zhang, Terry Truitt, Dramane Ibrahim Laine, Arjun Narayanan, Ruoqi Peng, David C. Budd, Matthew C. Lucas, Rama K. Kondru, Ruben Alvarez Sanchez
Publikováno v:
Journal of Medicinal Chemistry. 55:7920-7939
Lysophosphatidic acid is a class of bioactive phospholipid that mediates most of its biological effects through LPA receptors, of which six isoforms have been identified. The recent results from LPA1 knockout mice suggested that blocking LPA1 signali
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2902548479e1e1e040690c9e871f2659
https://doi.org/10.1021/jm301022v
https://doi.org/10.1021/jm301022v
Autor:
Laurent Salphati, Stewart J. Baker, Steve Price, Jim Nonomiya, Matthew C. Lucas, Timothy Hancox, David Knowles, Bohdan Waszkowycz, Neil Anthony Pegg, David Chantry, Bryan K. Chan, Paul Blaney, Anthony Brown, Steven T. Staben, Jodie Pang, Paul Depledge, Rama K. Kondru, Mark Ultsch, Paul Goldsmith, Karin Reif, Angelina Bisconte, Cristina Lewis, Eileen Mary Seward, Jeremy Murray, Brian Safina, Daniel P. Sutherlin, Zachary Kevin Sweeney, Georgette Castanedo, David Michael Goldstein, Jasmit Kaur, Sukhjit Sohal, Binqing Wei, John Lesnick, Stephen J. Shuttleworth, Alan Nadin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4296-4302
A potent inhibitor of PI3Kδ that is ⩾200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structure
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92be9aea35b7ac14f79d9d789ee6948b
https://doi.org/10.1016/j.bmcl.2012.05.027
https://doi.org/10.1016/j.bmcl.2012.05.027
Publikováno v:
Journal of Chemical Information and Modeling. 52:1450-1461
A central problem in structure-based drug design is understanding protein-ligand interactions quantitatively and qualitatively. Several recent studies have highlighted from a qualitative perspective the nature of these interactions and their utility
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4b9325830f624335e59914b3a229bf9
https://doi.org/10.1021/ci300034x
https://doi.org/10.1021/ci300034x
Publikováno v:
Journal of Medicinal Chemistry. 55:4539-4550
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cabed5364c98c874c2a8787da63c6ad1
https://doi.org/10.1021/jm300035p
https://doi.org/10.1021/jm300035p
Autor:
Andreas Jekle, Pamela Berry, Rama K. Kondru, André deRosier, Changhua Ji, Gabrielle Heilek, Lijing Chen, Jutta Wanner, Remy Lemoine, David Mark Rotstein
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6802-6807
Replacement of a secondary amide with a piperidine or azetidine moiety in a series of CCR5 antagonists led to the discovery of compounds with increased intrinsic permeability. This effort led to the identification of a potent CCR5 antagonist which ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c49b8fe349098e4978d13aea1e1af53d
https://doi.org/10.1016/j.bmcl.2010.08.118
https://doi.org/10.1016/j.bmcl.2010.08.118
Autor:
David Mark Rotstein, Changhua Ji, Rama K. Kondru, Marianna Dioszegi, Surya Sankuratri, Tara Mirzadegan, Jun Zhang
Publikováno v:
Molecular Pharmacology. 73:789-800
In addition to being an important receptor in leukocyte activation and mobilization, CCR5 is the essential coreceptor for human immunodeficiency virus (HIV). A large number of small-molecule CCR5 antagonists have been reported that show potent activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ed924f54529ba393cdaa7997b6642bb
https://doi.org/10.1124/mol.107.042101
https://doi.org/10.1124/mol.107.042101
Autor:
Changhua Ji, Nick Cammack, Eileen Rao, Jun Zhang, Marianna Dioszegi, Rama K. Kondru, André deRosier, Surya Sankuratri, Michael Brandt, Stephan Schwoerer, Eva Chan
Publikováno v:
Antimicrobial Agents and Chemotherapy. 51:1386-1397
Six mouse anti-human CCR5 monoclonal antibodies (mAbs) that showed potent antiviral activities were identified from over 26,000 mouse hybridomas. The epitopes for these mAbs were determined by using various CCR5 mutants, including CCR5/CCR2B chimeras
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a10e77713ca764a1a46cc21f622da3a9
https://doi.org/10.1128/aac.01302-06
https://doi.org/10.1128/aac.01302-06
Autor:
Joseph A. DiMasi, Kathryn Twyman, Stella Stergiopoulos, Rama K. Kondru, Johannes Cornelius Hermann, Wayne R. Rackoff, Kenneth A. Getz
Publikováno v:
Clinical pharmacology and therapeutics. 98(5)
We developed an algorithm (ANDI) for predicting regulatory marketing approval for new cancer drugs after phase II testing has been conducted, with the objective of providing a tool to improve drug portfolio decision-making. We examined 98 oncology dr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d2f917fe713a51c68124347d8202718
https://pubmed.ncbi.nlm.nih.gov/26239772
https://pubmed.ncbi.nlm.nih.gov/26239772