Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Weiguo, Xiang"'
Autor:
Bo Wen, Shaomeng Wang, Duxin Sun, Miao He, Paul D. Kirchhoff, Weiguo Xiang, Chong Qin, Xin Han, Donna McEachern, Lu Wang, Hoda Metwally, Aleksas Matvekas, Lijie Zhao, Yu Wang, Bukeyan Miao
Publikováno v:
J Med Chem
We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC(50) values of ≤0.1 nM in the VCaP cell line with AR gene amplification and in t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3122d4af987b9531939410c88a01d073
https://doi.org/10.1021/acs.jmedchem.1c00900
https://doi.org/10.1021/acs.jmedchem.1c00900
Autor:
Xin Han, Aleksas Matvekas, Bukeyan Miao, Weiguo Xiang, Bo Wen, Lijie Zhao, Chong Qin, Yu Wang, Lu Wang, Hoda Metwally, Donna McEachern, Shaomeng Wang, Duxin Sun
Publikováno v:
J Med Chem
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a promising new type of therapeutic agents, but the design of PROTAC degraders with excellent oral pharmacokinetics is a major challenge. In this study, we present our st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82b5ec7f1a36d9c56757326ebe0059a4
https://doi.org/10.1021/acs.jmedchem.1c00882
https://doi.org/10.1021/acs.jmedchem.1c00882
Publikováno v:
2022 23rd International Conference on Electronic Packaging Technology (ICEPT).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e9bd8fde89d5e39f7befcbab43695af4
https://doi.org/10.1109/icept56209.2022.9873103
https://doi.org/10.1109/icept56209.2022.9873103
Autor:
Weiguo Xiang, Shaomeng Wang
Publikováno v:
Journal of medicinal chemistry. 65(13)
The androgen receptor (AR) plays a key role in the maintenance of muscle and bone and the support of male sexual-related functions, as well as in the progression of prostate cancer. Accordingly, AR-targeted therapies have been developed for the treat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe2534c8ef5e5191fb84d7510c9c01de
https://pubmed.ncbi.nlm.nih.gov/35786895
https://pubmed.ncbi.nlm.nih.gov/35786895
Autor:
Weiguo Xiang, Shaomeng Wang
Publikováno v:
Journal of medicinal chemistry. 63(23)
Tropomyosin receptor kinases (TRKs) are promising cancer therapeutic targets. Chen ( J. Med. Chem. 2020, DOI: 10.1021/acs.jmedchem.0c01342) report the discovery of CG416 and CG428 as two potent small-molecule proteolysis-targeting chimera (PROTAC) de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ab5974303129460eb4ca12c195b72ee
https://pubmed.ncbi.nlm.nih.gov/33206509
https://pubmed.ncbi.nlm.nih.gov/33206509
Publikováno v:
OncoTargets and therapy
Myeloid cell leukemia-1 (MCL-1), a member of antiapoptotic BCL-2 family proteins, is a key regulator of mitochondrial homeostasis. Frequent overexpression of MCL-1 in human primary and drug-resistant cancer cells makes it an attractive cancer therape
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc9120b37ea8fe07f32d6f43c3056c1a
http://europepmc.org/articles/PMC6205821
http://europepmc.org/articles/PMC6205821
Autor:
Shaomeng Wang, Tianfeng Xu, Jeanne A. Stuckey, Mi Wang, Bukeyan Miao, Weiguo Xiang, Krishnapriya Chinnaswamy, Chong Qin, Chao Yie Yang, Xin Han, Lijie Zhao
Publikováno v:
Journal of medicinal chemistry. 62(24)
Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and biological characterization of highly potent small-molecule proteolysis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25df38681368c03b6420b4f710f37ab6
https://pubmed.ncbi.nlm.nih.gov/31804827
https://pubmed.ncbi.nlm.nih.gov/31804827
Publikováno v:
2019 5th International Conference on Information Management (ICIM).
Aiming at solving the problems of low success rate and low efficiency in converting BIM models to GIS platform, this paper proposes a multi-source model integration and publishment method based on two main software, i.e., Bentley Microstation and Wei
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::20d5e7cbf60d963d5082020458a2f5d2
https://doi.org/10.1109/infoman.2019.8714651
https://doi.org/10.1109/infoman.2019.8714651
Autor:
James Delproposto, Tianfeng Xu, Jeanne A. Stuckey, Krishnapriya Chinnaswamy, Weiguo Xiang, Chong Qin, Shaomeng Wang, Lijie Zhao, Ester Fernandez-Salas, Chao Wang, Xin Han, Chao Yie Yang, Mi Wang
Publikováno v:
Journal of medicinal chemistry. 62(2)
We report herein the discovery of highly potent PROTAC degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent manne
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa48cb63c08eeff567789b50ecd723e1
https://pubmed.ncbi.nlm.nih.gov/30629437
https://pubmed.ncbi.nlm.nih.gov/30629437
Autor:
Ernest Hamel, Tasdique M. Quadery, Susan L. Mooberry, Lerin R. Luckett-Chastain, Aleem Gangjee, Michael A. Ihnat, Weiguo Xiang
Publikováno v:
Bioorg Med Chem
A series of methoxy naphthyl substituted cyclopenta[d]pyrimidine compounds, 4–10, were designed and synthesized to study the influence of the 3-D conformation on microtubule depolymerizing and antiproliferative activities. NOESY studies with the N,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::664c674b029bd9e6d81367bede98a64d
https://doi.org/10.1016/j.bmc.2020.115887
https://doi.org/10.1016/j.bmc.2020.115887