公开(公告)号：US20190167604A1

公开(公告)日：2019-06-06

申请号：US16243761

申请日：2019-01-09

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Jie LI ,  Zilei LIU ,  Suhua LI ,  Peng WU ,  K. Barry SHARPLESS

IPC分类号： A61K31/05 ,  A61K47/54 ,  A61K31/136 ,  C07C305/26 ,  C07K1/113 ,  C07K1/02 ,  A61K51/04 ,  A61K38/31 ,  A61K31/7048 ,  A61K31/70 ,  A61K31/655 ,  A61K31/65 ,  A61K31/56 ,  A61K31/5513 ,  A61K31/53 ,  A61K31/515 ,  A61K31/505 ,  A61K31/485 ,  A61K31/4745 ,  A61K31/473 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/439 ,  A61K31/4353 ,  A61K31/4245 ,  A61K31/4168 ,  A61K31/407 ,  A61K31/4045 ,  A61K31/40 ,  A61K31/397 ,  A61K31/198 ,  A61K31/197 ,  A61K31/14 ,  C07K2/00 ,  C07D295/26 ,  C07D295/185 ,  C07D295/088 ,  C07D277/82

摘要： Arylfluorosulfate compounds derived from anticancer drugs are disclosed herein, which exhibit improved anti-cancer cell proliferation activities compared to their phenolic drug precursors. Among these compounds, the fluorosulfate derivative of fulvestrant showed significantly enhanced activity to down-regulate estrogen receptor (ER) expression in ER+ breast cancer cell line MCF-7, and oral availability in vivo; the fluorosulfate derivative of combretastatin A4 exhibited a 70-fold increase in potency in the drug resistant colon cancer cell line HT-29; and the fluorosulfate derivative of ABT-751 showed enhanced activity relative to ABT-751.

公开(公告)号：US20200268683A1

公开(公告)日：2020-08-27

申请号：US16871902

申请日：2020-05-11

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Jie LI ,  Zilei LIU ,  Suhua LI ,  Peng WU ,  K. Barry SHARPLESS

IPC分类号： A61K31/05 ,  A61K31/136 ,  C07C305/26 ,  C07K1/113 ,  C07K1/02 ,  A61K51/04 ,  A61K38/31 ,  A61K31/7048 ,  A61K31/70 ,  A61K31/655 ,  A61K31/65 ,  A61K31/56 ,  A61K31/5513 ,  A61K31/53 ,  A61K31/515 ,  A61K31/505 ,  A61K31/485 ,  A61K31/4745 ,  A61K31/473 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/439 ,  A61K31/4353 ,  A61K31/4245 ,  A61K31/4168 ,  A61K31/407 ,  A61K31/4045 ,  A61K31/40 ,  A61K31/397 ,  A61K31/198 ,  A61K31/197 ,  A61K31/14 ,  C07K2/00 ,  C07D295/26 ,  C07D295/185 ,  C07D295/088 ,  C07D277/82 ,  A61K47/54

摘要： A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO2F2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilyl chloride to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.

公开(公告)号：US20230348846A1

公开(公告)日：2023-11-02

申请号：US18327110

申请日：2023-06-01

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Peng WU ,  Jie LI ,  Yiran ZHOU ,  Mingkuan CHEN

IPC分类号： A61P35/00 ,  C12N5/0784 ,  C12N5/00 ,  A61K47/68 ,  C07K16/28 ,  C07K16/32 ,  C12N5/0783 ,  C12N9/10 ,  C12N5/10 ,  A61K47/54 ,  A61K47/69

CPC分类号： C12N5/0006 ,  A61K47/549 ,  A61K47/6849 ,  A61K47/6855 ,  A61K47/6901 ,  A61P35/00 ,  C07K16/2827 ,  C07K16/2854 ,  C07K16/32 ,  C12N5/0636 ,  C12N5/0639 ,  C12N5/0646 ,  C12N5/10 ,  C12N9/1051 ,  C07K2317/55 ,  C07K2317/622

摘要： Provided herein are engineered cells, comprising: a chemical or biological moiety covalently bound to a cell surface glycan, wherein the chemical or biological moiety is selected from the group consisting of small molecule, polynucleotide, polypeptide, and antibody. Also provided are compositions comprising these engineered cells and methods of making and using the same.