Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Kam W. Siu"'
Autor:
Kam W. Siu, Kanak Raina, Craig M. Crews, Ann Marie Rossi, James D. Winkler, Kevin Coleman, Martha Altieri, Hanqing Dong, Andrew P. Crew, Xin Chen, Deborah M. Gordon, Jing Wang, Jing Lu, Yimin Qian
Publikováno v:
Proceedings of the National Academy of Sciences. 113:7124-7129
Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States. Although androgen deprivation can initially lead to remission, the disease often progresses
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e52c5cfa2f667176759537abdfe006d
https://doi.org/10.1073/pnas.1521738113
https://doi.org/10.1073/pnas.1521738113
Autor:
Alicia Morgan, Kevin Coleman, Dominico Vigil, Caterina Ferraro, Andrew P. Crew, Kam W. Siu, Brian D. Hamman, James D. Winkler, Jing Wang, Yevgeniy V. Serebrenik, Craig M. Crews, Yimin Qian, Taavi K. Neklesa, Kanak Raina, Hanqing Dong
Publikováno v:
Journal of medicinal chemistry. 61(2)
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e53e69a07899fd55762d8047933dd61
https://pubmed.ncbi.nlm.nih.gov/28692295
https://pubmed.ncbi.nlm.nih.gov/28692295
Autor:
David Epstein, Kam W. Siu, Earl W. May, Andrew Kleinberg, Prafulla C. Gokhale, Mark J. Mulvihill, Ryan Schulz, Jonathan A. Pachter, Meizhong Jin, Mridula Kadalbajoo, Kenneth Foreman, Jennifer Kahler, Mark Bittner, Brenda A. Petronella, Andy Cooke, Robert A. Wild
Publikováno v:
ACS Medicinal Chemistry Letters. 4:627-631
This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure–activity and structure–kinetic relationships were elucidated and guided further optimizations within t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71d0beeac5e7bcb9257a057fecc19be4
https://doi.org/10.1021/ml400160a
https://doi.org/10.1021/ml400160a
Autor:
Andrew P. Crew, Meizhong Jin, Kristen Michelle Mulvihill, Mark J. Mulvihill, David Epstein, Qun-Sheng Ji, Shripad V. Bhagwat, Mridula Kadalbajoo, Andrew Cooke, Josef A. Rechka, Jonathan A. Pachter, Mark Bittner, Kam W. Siu, Yan Yao, Jing Wang, April Thelemann, Andrew Kleinberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:979-984
This Letter describes the medicinal chemistry effort towards a series of novel imidazo[1,5-a]pyrazine derived inhibitors of ACK1. Virtual screening led to the discovery of the initial hit, and subsequent exploration of structure-activity relationship
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb66157d50668f15d12c6b4c68463b3f
https://doi.org/10.1016/j.bmcl.2012.12.042
https://doi.org/10.1016/j.bmcl.2012.12.042
Autor:
Dan Sherman, Pawan Rastogi, An-Hu Li, Andrew Kleinberg, Ti Wang, Mark J. Mulvihill, Anthony Nigro, Heather Coate, Kristen Michelle Mulvihill, Andrew P. Crew, Mridula Kadalbajoo, Kam W. Siu, Ayako Honda, Radoslaw Laufer, David J. Beard, Arno G. Steinig, Doug Werner
Publikováno v:
Synthesis. 2010:1678-1686
A highly effective one-pot Friedlander quinoline synthesisfrom O-nitroarylcarbaldehydes and ketonesor aldehydes was developed and the scope and limitations of themethod were examined. The O-nitroarylcarbaldehydeswere reduced to O-aminoarylcarbaldehyd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::08f67c0e37249d3f8abdc174bfb57b66
https://doi.org/10.1055/s-0029-1218701
https://doi.org/10.1055/s-0029-1218701
Autor:
Darlene Romashko, James G. Tarrant, Felix Weng, Keith R. Hornberger, Matthew R. Medeiros, Andrew Kleinberg, Peter Meyn, Dan Maarten Berger, Mark Albertella, William Peick, An-Hu Li, Mark Bittner, Jing Wang, Hanqing Dong, Paul Maresca, Mark J. Mulvihill, Earl W. May, Wilde Victoria Lynn, Kam W. Siu, Brianna Tokar, Michael Tanowitz, Michael J. Gray, Andrew P. Crew, Andrew Cooke
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(16)
The discovery and potency optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ∼10 nM, as exe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::539f984e43b2488a1efbebe0b4c06384
https://pubmed.ncbi.nlm.nih.gov/23850198
https://pubmed.ncbi.nlm.nih.gov/23850198
Autor:
Darla Landfair, Prafulla C. Gokhale, Qun-Sheng Ji, Robert A. Wild, Kristen Michelle Mulvihill, Meizhong Jin, Kenneth Foreman, Hanqing Dong, Gilda Mak, Andrew Kleinberg, Andy Cooke, Mark J. Mulvihill, Matthew O'Connor, Mark Bittner, Yan Yao, Kam W. Siu, Maryland Rosenfeld-Franklin, Jonathan A. Pachter
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(4)
Preclinical and emerging clinical evidence suggests that inhibiting insulin-like growth factor 1 receptor (IGF-1R) signaling may offer a promising therapeutic strategy for the treatment of several types of cancer. This Letter describes the medicinal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c89e64064f19f6bae3c17b1b2909d2d
https://pubmed.ncbi.nlm.nih.gov/21251824
https://pubmed.ncbi.nlm.nih.gov/21251824
Autor:
Andrew Kleinberg, Prafulla C. Gokhale, Kathryn M. Stolz, Yan Yao, Andy Cooke, An-Hu Li, Douglas S. Werner, Robert A. Wild, Darla Landfair, Arno G. Steinig, Earl W. May, Mark Bittner, Elizabeth Buck, Hanqing Dong, Mark J. Mulvihill, Jonathan A. Pachter, Radoslaw Laufer, Mridula Kadalbajoo, Lixin Feng, Kam W. Siu, Kenneth Foreman, Meizhong Jin
This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure−activity relationship exploration and optimizat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c753d9d6dfa51f50ae521f392bf85fd4
https://europepmc.org/articles/PMC4007908/
https://europepmc.org/articles/PMC4007908/
Autor:
Kenneth Foreman, Mark J. Mulvihill, Caroline Pirrit, Kam W. Siu, Anthony Nigro, Gilda Mak, Ayako Honda, Neil W. Gibson, Andrew Cooke, Lixin Feng, Kristen Michelle Mulvihill, Arno G. Steinig, Hanqing Dong, Matthew O'Connor, Paula A. R. Tavares, Kathryn M. Stolz, Yingchuan Sun, Qun-Sheng Ji, Heather Coate, Maryland Rosenfeld-Franklin, Yan Yao
Publikováno v:
Bioorganicmedicinal chemistry. 16(3)
A series of novel, potent quinolinyl-derived imidazo[1,5-a]pyrazine IGF-IR (IGF-1R) inhibitors--most notably, cis-3-(3-azetidin-1-ylmethylcyclobutyl)-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-ylamine (AQIP)--is described. Synthetic details, st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e22a4df4a6696ed4e73207d83c986a9d
https://pubmed.ncbi.nlm.nih.gov/17983756
https://pubmed.ncbi.nlm.nih.gov/17983756
Autor:
Kevin Coleman, Hanqing Dong, Kam W. Siu, Jing Wang, AP Crew, Ryan R. Willard, Caterina Ferraro, Deborah A. Gordon, Taavi K. Neklesa, Craig M. Crews, Xin Chen, James D. Winkler, AnnMarie K. Rossi, Meizhong Jin
Publikováno v:
Molecular Cancer Therapeutics. 14:PR08-PR08
Patients with prostate cancer who progress on therapy often have enhanced Androgen Receptor (AR) signaling due to several mechanisms: increased androgen production, increased AR expression, and/or specific AR mutations that render current therapies i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e99ce278ede08c0d79f568cd1d0ce3b1
https://doi.org/10.1158/1535-7163.targ-15-pr08
https://doi.org/10.1158/1535-7163.targ-15-pr08