Xiaodong Cheng

Scopus Author ID ORCID

Publication Activity (10 Years)

Years Active: 2018-2024
Publications (10 Years): 53

Top Topics

Clostridium Difficile

Dna Methylation

Top Venues

Journal of medicinal chemistry

ACS chemical biology

Nucleic acids research

Science advances

This page only lists publications with an associated author ORCID identifier.

Publications

Swanand Hardikar, Ren Ren, Zhengzhou Ying, Jujun Zhou, John R Horton, Matthew D Bramble, Bin Liu, Yue Lu, Bigang Liu, Luis Della Coletta, Jianjun Shen, Jiameng Dan, Xing Zhang, Xiaodong Cheng, Jiameng Dan
The ICF syndrome protein CDCA7 harbors a unique DNA binding domain that recognizes a CpG dyad in the context of a non-B DNA. Science advances 10 (34) (2024)
Jane Skok, Catherine Do, Guimei Jiang, Giulia Cova, Christos Katsifis, Domenic Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Aristotelis Tsirigos, Faye Fara Regis, Nata Kakabadze, Elphѐge P Nora, Marcus Noyes, Xiaodong Cheng, Anders S Hansen
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. Research square (2024)
Xing Zhang, Robert M Blumenthal, Xiaodong Cheng
Keep Fingers on the CpG Islands. Epigenomes 8 (2) (2024)
Jane Skok, Catherine Do, Guimei Jiang, Giulia Cova, Christos Katsifis, Domenic Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Aristotelis Tsirigos, Faye Fara Regis, Nata Kakabadze, Elphѐge P Nora, Marcus Noyes, Xiaodong Cheng, Anders S Hansen
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. Research square (2024)
Xing Zhang, Robert M Blumenthal, Xiaodong Cheng
Keep Fingers on the CpG Islands. Epigenomes 8 (2) (2024)
Swanand Hardikar, Ren Ren, Zhengzhou Ying, Jujun Zhou, John R Horton, Matthew D Bramble, Bin Liu, Yue Lu, Bigang Liu, Luis Della Coletta, Jianjun Shen, Jiameng Dan, Xing Zhang, Xiaodong Cheng, Jiameng Dan
The ICF syndrome protein CDCA7 harbors a unique DNA binding domain that recognizes a CpG dyad in the context of a non-B DNA. Science advances 10 (34) (2024)
Catherine Do, Guimei Jiang, Giulia Cova, Christos C Katsifis, Domenic N Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Aristotelis Tsirigos, Faye Fara D Regis, Nata Kakabadze, Elphѐge P Nora, Marcus Noyes, Xiaodong Cheng, Anders S Hansen, Jane A Skok
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. Research square (2024)
Catherine Do, Guimei Jiang, Giulia Cova, Christos C Katsifis, Domenic N Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Faye Fara Regis, Nata Kakabadze, Elphege P Nora, Marcus B Noyes, Xiaodong Cheng, Anders S Hansen, Jane A Skok
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. bioRxiv : the preprint server for biology (2024)
Catherine Do, Guimei Jiang, Giulia Cova, Christos C Katsifis, Domenic N Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Faye Fara Regis, Nata Kakabadze, Elphege P Nora, Marcus B Noyes, Xiaodong Cheng, Anders S Hansen, Jane A Skok
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. bioRxiv : the preprint server for biology (2024)
Catherine Do, Guimei Jiang, Giulia Cova, Christos C Katsifis, Domenic N Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Aristotelis Tsirigos, Faye Fara D Regis, Nata Kakabadze, Elphѐge P Nora, Marcus Noyes, Xiaodong Cheng, Anders S Hansen, Jane A Skok
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. Research square (2024)
Jujun Zhou, Qin Chen, Ren Ren, Jie Yang, Bigang Liu, John R Horton, Caleb Chang, Chuxuan Li, Leora Maksoud, Yifei Yang, Dante Rotili, Xing Zhang, Robert M Blumenthal, Jiameng Dan, Yang Gao, Sergio Valente, Antonello Mai, Xiaodong Cheng
Quinoline-based compounds can inhibit diverse enzymes that act on DNA. bioRxiv : the preprint server for biology (2024)
Xing Zhang, Robert M Blumenthal, Xiaodong Cheng
Keep Fingers on the CpG Islands. Epigenomes 8 (2) (2024)
Swanand Hardikar, Ren Ren, Zhengzhou Ying, Jujun Zhou, John R Horton, Matthew D Bramble, Bin Liu, Yue Lu, Bigang Liu, Luis Della Coletta, Jianjun Shen, Jiameng Dan, Xing Zhang, Xiaodong Cheng, Jiameng Dan
The ICF syndrome protein CDCA7 harbors a unique DNA binding domain that recognizes a CpG dyad in the context of a non-B DNA. Science advances 10 (34) (2024)
Catherine Do, Guimei Jiang, Giulia Cova, Christos C Katsifis, Domenic N Narducci, Jie Yang, Theodore Sakellaropoulos, Raphael Vidal, Priscillia Lhoumaud, Aristotelis Tsirigos, Faye Fara D Regis, Nata Kakabadze, Elphege P Nora, Marcus B Noyes, Xiaodong Cheng, Anders S Hansen, Jane A Skok
Brain and cancer associated binding domain mutations provide insight into CTCF's relationship with chromatin and its ability to act as a chromatin organizer. bioRxiv : the preprint server for biology (2024)
Swanand Hardikar, Ren Ren, Zhengzhou Ying, Jujun Zhou, John R Horton, Matthew D Bramble, Bin Liu, Yue Lu, Bigang Liu, Luis Della Coletta, Jianjun Shen, Jiameng Dan, Xing Zhang, Xiaodong Cheng, Jiameng Dan
The ICF syndrome protein CDCA7 harbors a unique DNA binding domain that recognizes a CpG dyad in the context of a non-B DNA. Science advances 10 (34) (2024)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Gundeep Kaur, Ren Ren, Michal Hammel, John R Horton, Jie Yang, Yu Cao, Chenxi He, Fei Lan, Xianjiang Lan, Gerd A Blobel, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Allosteric autoregulation of DNA binding via a DNA-mimicking protein domain: a biophysical study of ZNF410-DNA interaction using small angle X-ray scattering. Nucleic acids research (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Qin Chen, Bigang Liu, Yang Zeng, Jee Won Hwang, Nan Dai, Ivan R Corrêa, Marcos R Estecio, Xing Zhang, Margarida A Santos, Taiping Chen, Xiaodong Cheng
GSK-3484862 targets DNMT1 for degradation in cells. NAR cancer 5 (2) (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Qin Chen, Bigang Liu, Yang Zeng, Jee Won Hwang, Nan Dai, Ivan R Corrêa, Marcos R Estecio, Xing Zhang, Margarida A Santos, Taiping Chen, Xiaodong Cheng
GSK-3484862 targets DNMT1 for degradation in cells. NAR cancer 5 (2) (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Gundeep Kaur, Ren Ren, Michal Hammel, John R Horton, Jie Yang, Yu Cao, Chenxi He, Fei Lan, Xianjiang Lan, Gerd A Blobel, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Allosteric autoregulation of DNA binding via a DNA-mimicking protein domain: a biophysical study of ZNF410-DNA interaction using small angle X-ray scattering. Nucleic acids research 51 (4) (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Jujun Zhou, Youchao Deng, Iredia D Iyamu, John R Horton, Dan Yu, Taraneh Hajian, Masoud Vedadi, Dante Rotili, Antonello Mai, Robert M Blumenthal, Xing Zhang, Rong Huang, Xiaodong Cheng
Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile- Specific DNA Adenine Methyltransferase. ACS chemical biology 18 (4) (2023)
Peng Huang, Scott A Peslak, Ren Ren, Eugene Khandros, Kunhua Qin, Cheryl A Keller, Belinda M Giardine, Henry William Bell, Xianjiang Lan, Malini Sharma, John R Horton, Osheiza Abdulmalik, Stella T Chou, Junwei Shi, Merlin Crossley, Ross Cameron Hardison, Xiaodong Cheng, Gerd A Blobel
Author Correction: HIC2 controls developmental hemoglobin switching by repressing BCL11A transcription. Nature genetics (2023)
Gundeep Kaur, Ren Ren, Michal Hammel, John R Horton, Jie Yang, Yu Cao, Chenxi He, Fei Lan, Xianjiang Lan, Gerd A Blobel, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Allosteric autoregulation of DNA binding via a DNA-mimicking protein domain: a biophysical study of ZNF410-DNA interaction using small angle X-ray scattering. Nucleic acids research 51 (4) (2023)
Jie Yang, John R Horton, Bin Liu, Victor G Corces, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Structures of CTCF-DNA complexes including all 11 zinc fingers. Nucleic acids research (2023)
Gundeep Kaur, Ren Ren, Michal Hammel, John R Horton, Jie Yang, Yu Cao, Chenxi He, Fei Lan, Xianjiang Lan, Gerd A Blobel, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Allosteric autoregulation of DNA binding via a DNA-mimicking protein domain: a biophysical study of ZNF410-DNA interaction using small angle X-ray scattering. Nucleic acids research 51 (4) (2023)
Qin Chen, Bigang Liu, Yang Zeng, Jee Won Hwang, Nan Dai, Ivan R Corrêa, Marcos R Estecio, Xing Zhang, Margarida A Santos, Taiping Chen, Xiaodong Cheng
GSK-3484862 targets DNMT1 for degradation in cells. NAR cancer 5 (2) (2023)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry 66 (1) (2022)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry 66 (1) (2022)
Dan Yu, Jujun Zhou, Qin Chen, Tao Wu, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Enzymatic Characterization of In Vitro Activity of RNA Methyltransferase PCIF1 on DNA. Biochemistry (2022)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry 66 (1) (2022)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry 66 (1) (2022)
Peng Huang, Scott A Peslak, Ren Ren, Eugene Khandros, Kunhua Qin, Cheryl A Keller, Belinda M Giardine, Henry William Bell, Xianjiang Lan, Malini Sharma, John R Horton, Osheiza Abdulmalik, Stella T Chou, Junwei Shi, Merlin Crossley, Ross Cameron Hardison, Xiaodong Cheng, Gerd A Blobel
HIC2 controls developmental hemoglobin switching by repressing BCL11A transcription. Nature genetics 54 (9) (2022)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry 66 (1) (2022)
Jujun Zhou, John R Horton, Martina Menna, Francesco Fiorentino, Ren Ren, Dan Yu, Taraneh Hajian, Masoud Vedadi, Giulia Mazzoccanti, Alessia Ciogli, Elmar Weinhold, Michael Hüben, Robert M Blumenthal, Xing Zhang, Antonello Mai, Dante Rotili, Xiaodong Cheng
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile- Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. Journal of medicinal chemistry (2022)
Jie Yang, John R Horton, Kadir C Akdemir, Jia Li, Yun Huang, Janani Kumar, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Preferential CEBP binding to T:G mismatches and increased C-to-T human somatic mutations. Nucleic acids research 49 (9) (2021)
Jujun Zhou, John R Horton, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Clostridioides difficile specific DNA adenine methyltransferase CamA squeezes and flips adenine out of DNA helix. Nature communications 12 (1) (2021)
Dan Yu, John R Horton, Jie Yang, Taraneh Hajian, Masoud Vedadi, Cari A Sagum, Mark T Bedford, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Human MettL3-MettL14 RNA adenine methyltransferase complex is active on double-stranded DNA containing lesions. Nucleic acids research 49 (20) (2021)
Jujun Zhou, John R Horton, Dan Yu, Ren Ren, Robert M Blumenthal, Xing Zhang, Xiaodong Cheng
Repurposing epigenetic inhibitors to target the Clostridioides difficile-specific DNA adenine methyltransferase and sporulation regulator CamA. Epigenetics (2021)
Lucia Ichino, Brandon A Boone, Luke Strauskulage, C Jake Harris, Gundeep Kaur, Matthew A Gladstone, Maverick Tan, Suhua Feng, Yasaman Jami-Alahmadi, Sascha H C Duttke, James Akira Wohlschlegel, Xiaodong Cheng, Sy Redding, Steven E Jacobsen
MBD5 and MBD6 couple DNA methylation to gene silencing through the J-domain protein SILENZIO. Science (New York, N.Y.) (2021)
Melissa B Pappalardi, Kathryn Keenan, Mark Cockerill, Wendy A Kellner, Alexandra Stowell, Christian Sherk, Kristen Wong, Sarath Pathuri, Jacques Briand, Michael Steidel, Philip Chapman, Arthur Groy, Ashley K Wiseman, Charles F McHugh, Nino Campobasso, Alan P Graves, Emma Fairweather, Thilo Werner, Ali Raoof, Roger J Butlin, Lourdes Rueda, John R Horton, David T Fosbenner, Cunyu Zhang, Jessica L Handler, Morris Muliaditan, Makda Mebrahtu, Jon-Paul Jaworski, Dean E McNulty, Charlotte Burt, H Christian Eberl, Amy N Taylor, Thau Ho, Susan Merrihew, Shawn W Foley, Anna Rutkowska, Mei Li, Stuart P Romeril, Kristin Goldberg, Xing Zhang, Christopher S Kershaw, Marcus Bantscheff, Anthony J Jurewicz, Elisabeth Minthorn, Paola Grandi, Mehul Patel, Andrew B Benowitz, Helai P Mohammad, Aidan G Gilmartin, Rabinder K Prinjha, Donald Ogilvie, Christopher Carpenter, Dirk Heerding, Stephen B Baylin, Peter A Jones, Xiaodong Cheng, Bryan W King, Juan I Luengo, Allan Michael Jordan, Ian Waddell, Ryan G Kruger, Michael T McCabe
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nature cancer 2 (10) (2021)
Swanand Hardikar, Zhengzhou Ying, Yang Zeng, Hongbo Zhao, Bigang Liu, Nicolas Veland, Kevin M McBride, Xiaodong Cheng, Jiameng Dan
The ZBTB24-CDCA7 axis regulates HELLS enrichment at centromeric satellite repeats to facilitate DNA methylation. Protein & cell 11 (3) (2020)
Janani Kumar, Gundeep Kaur, Ren Ren, Yue Lu, Kevin Lin, Jia Li, Yun Huang, Anamika Patel, Michelle Craig Barton, Todd Macfarlan, Xing Zhang, Xiaodong Cheng
KRAB domain of ZFP568 disrupts TRIM28-mediated abnormal interactions in cancer cells. NAR cancer 2 (2) (2020)
Yang Zeng, Ren Ren, Gundeep Kaur, Swanand Hardikar, Zhengzhou Ying, Lance Babcock, Esha Gupta, Xing Zhang, Taiping Chen, Xiaodong Cheng
The inactive Dnmt3b3 isoform preferentially enhances Dnmt3b-mediated DNA methylation. Genes & development 34 (21-22) (2020)
Shaobo Dai, Matthew V Holt, John R Horton, Clayton B Woodcock, Anamika Patel, Xing Zhang, Nicolas L Young, Alex W Wilkinson, Xiaodong Cheng
Characterization of SETD3 methyltransferase-mediated protein methionine methylation. The Journal of biological chemistry 295 (32) (2020)
Shaobo Dai, John R Horton, Clayton B Woodcock, Alex W Wilkinson, Xing Zhang, Or Gozani, Xiaodong Cheng
Structural basis for the target specificity of actin histidine methyltransferase SETD3. Nature communications 10 (1) (2019)
John R Horton, Clayton B Woodcock, Sifa B Opot, Norbert O Reich, Xing Zhang, Xiaodong Cheng
The cell cycle-regulated DNA adenine methyltransferase CcrM opens a bubble at its DNA recognition site. Nature communications 10 (1) (2019)
John R Horton, Clayton B Woodcock, Qin Chen, Xu Liu, Xing Zhang, John Shanks, Ganesha Rai, Bryan T Mott, Daniel J Jansen, Stephen C Kales, Mark J Henderson, Matthew Cyr, Katherine Pohida, Xin Hu, Pranav Shah, Xin Xu, Ajit Jadhav, David J Maloney, Matthew D Hall, Anton Simeonov, Haian Fu, Paula M Vertino, Xiaodong Cheng
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. Journal of medicinal chemistry 61 (23) (2018)
John R Horton, Xu Liu, Lizhen Wu, Kai Zhang, John Shanks, Xing Zhang, Ganesha Rai, Bryan T Mott, Daniel J Jansen, Stephen C Kales, Mark J Henderson, Katherine Pohida, Yuhong Fang, Xin Hu, Ajit Jadhav, David J Maloney, Matthew D Hall, Anton Simeonov, Haian Fu, Paula M Vertino, Qin Yan, Xiaodong Cheng
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A. Journal of medicinal chemistry 61 (7) (2018)