Zobrazeno 1 - 10
of 99
pro vyhledávání: '"David R. Langley"'
Autor:
Yen-Ting Lai, Tao Wang, Sijy O’Dell, Mark K. Louder, Arne Schön, Crystal S. F. Cheung, Gwo-Yu Chuang, Aliaksandr Druz, Bob Lin, Krisha McKee, Dongjun Peng, Yongping Yang, Baoshan Zhang, Alon Herschhorn, Joseph Sodroski, Robert T. Bailer, Nicole A. Doria-Rose, John R. Mascola, David R. Langley, Peter D. Kwong
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-11 (2019)
Temsavir, a compound that inhibits HIV entry by binding envelope (Env), is currently in clinical development. Here, Lai et al. identify a more than 10-fold improved compound and, using lattice engineering, obtain crystal structures that give insights
Externí odkaz:
https://doaj.org/article/8c1780f80cef41df909afde553e1a2ab
Autor:
Michael A. Schmidt, Chunshan Xie, Naidu S. Chowdari, Ankita G. Niyogi, David R. Langley, Heng Cheng, Gregory D. Vite, Sivakrishna Guturi, Rajappa Vaidyanathan, Sanjeev Gangwar, Ivar M. McDonald, Kishorekumar Kanagavel, Yichen Tan, Prasanna Sivaprakasam, Souvik Rakshit, Chin Pan, Umamaheswararao Kanusu, Martin D. Eastgate, Madhura Deshpande, Somprabha Sidhar, Bin Zheng, Christiana I. Iwuagwu, Michael R. Luzung, Ganapathy Sarma, Kevin M. Peese, Thirumalai Lakshminarasimhan, Patrick G. Holder, Pina M. Cardarelli, Patricia Cho, Srikanth Kotapati, Chetana Rao
Publikováno v:
ACS Med Chem Lett
[Image: see text] A new series with the tetrahydroisoquinoline-fused benzodiazepine (TBD) ring system combined with the surrogates of (1-methyl-1H-pyrrol-3-yl)benzene (“MPB”) payloads were designed and executed for conjugation with a monoclonal a
Autor:
Tricia Protack, Michael A. Walker, Guo Li, David R. Langley, B. Narasimhulu Naidu, Nicholas A. Meanwell, George L. Trainor, Alicia Ng, Susan Jenkins, Mark Krystal, Zeyu Lin, Samuel Gerritz, Christopher Cianci, Hal A. Lewis, Kevin Kish, Javed Khan, Prasanna Sivaprakasam, Annapurna Pendri, Ira B. Dicker, Linda Discotto
Publikováno v:
Journal of Medicinal Chemistry. 63:2620-2637
The standard of care for HIV-1 infection, highly active antiretroviral therapy (HAART), combines two or more drugs from at least two classes. Even with the success of HAART, new drugs with novel mechanisms are needed to combat viral resistance, impro
Publikováno v:
ACS omega. 7(34)
Glutathione peroxidase 4 (GPX4) reduces lipid hydroperoxides in lipid membranes, effectively inhibiting iron-dependent cell death or ferroptosis. The upregulation of the enzyme by the mutations at residues D21 and D23 has been suggested to be associa
Autor:
Eilene Kwok, Derwin Daniel W, Sanjeev Gangwar, Chin Pan, Chetana Rao, David Passmore, Yichong Wang, Bilal Sufi, David R. Langley, Pina M. Cardarelli, Vangipuram S. Rangan, Shrikant Deshpande, Gregory D. Vite, Naidu S. Chowdari, Prasanna Sivaprakasam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:466-470
Uncialamycin analogs were evaluated as potential cytotoxic agents in an antibody-drug conjugate (ADC) approach to treating human cancer. These analogs were synthesized using Hauser annulations of substituted phthalides as a key step. A highly potent
Autor:
Crystal S.F. Cheung, Alon Herschhorn, Gwo-Yu Chuang, Arne Schön, Krisha McKee, Nicole A. Doria-Rose, Aliaksandr Druz, Yongping Yang, David R. Langley, Mark K. Louder, Tao Wang, Baoshan Zhang, Yen-Ting Lai, Dongjun Peng, Peter D. Kwong, Robert T. Bailer, Joseph Sodroski, Sijy O'Dell, John R. Mascola, Bob C. Lin
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-11 (2019)
Nature Communications
Nature Communications
Diverse entry inhibitors targeting the gp120 subunit of the HIV-1 envelope (Env) trimer have been developed including BMS-626529, also called temsavir, a prodrug version of which is currently in phase III clinical trials. Here we report the character
Autor:
Johnson Walter Lewis, Sung Mei-Chen, Daniel Menezes, Chin Pan, Gregory D. Vite, Yong Zhang, Shrikant Deshpande, Vangipuram S. Rangan, Madhura Deshpande, Richard Rampulla, Ganapathy Sarma, Prasanna Sivaprakasam, Arvind Rajpal, David R. Langley, Tram N. Huynh, Arvind Mathur, Ivar M. McDonald, Naidu S. Chowdari, Pina M. Cardarelli, Bethanne M. Warrack, Srikanth Kotapati, Yichong Wang, Chetana Rao, David Passmore, Robert A. Mate, Robert M. Borzilleri, Sanjeev Gangwar
Publikováno v:
Journal of medicinal chemistry. 63(22)
A series of tetrahydroisoquinoline-based benzodiazepine dimers were synthesized and tested for in vitro cytotoxicity against a panel of cancer cell lines. Structure-activity relationship investigation of various spacers guided by molecular modeling s
Autor:
Phil S. Baran, Tian Qin, Justine N. de Gruyter, Michael R. Collins, Kap Sun Yeung, Shengyang Ni, Gary M. Gallego, David R. Langley, Jennifer X. Qiao, Paul Michael Scola, James J. Mousseau, Daniel C. Schmitt, Michael A. Poss, Rohan R. Merchant, Shouliang Yang, Alberto F. Garrido-Castro
Publikováno v:
Angewandte Chemie. 130:14768-14773
The direct union of primary, secondary, and tertiary carboxylic acids with a chiral glyoxylate-derived sulfinimine provides rapid access into a variety of enantiomerically pure α-amino acids (>85 examples). Characterized by operational simplicity, t
Publikováno v:
PLoS ONE, Vol 5, Iss 2, p e9195 (2010)
BACKGROUND: Entecavir (ETV) is a deoxyguanosine analog competitive inhibitor of hepatitis B virus (HBV) polymerase that exhibits delayed chain termination of HBV DNA. A high barrier to entecavir-resistance (ETVr) is observed clinically, likely due to
Externí odkaz:
https://doaj.org/article/d3184b0376a84ea99b5bba0418792a95
Autor:
David R. Langley, Nicholas A. Meanwell, Dennis M. Grasela, Tao Wang, Beata Nowicka-Sans, John F. Kadow, David A. Conlon, Mark Krystal, Peter Timmins, Martin D. Eastgate
Publikováno v:
Journal of Medicinal Chemistry. 61:62-80
Human immunodeficiency virus-1 (HIV-1) infection currently requires lifelong therapy with drugs that are used in combination to control viremia. The indole-3-glyoxamide 6 was discovered as an inhibitor of HIV-1 infectivity using a phenotypic screen a