Co-expression and purification of recombinant hOvastacin and hFetuin B in insect cell sf9

Posted onAuthorYufeng PanLeave a comment

hFetuin B(1-382)-Fc-6xHis and hOvastacin(1-431)-twinStrep purification: Nickel & Strep-Tactin®T 4Flow® high capacity FPLC column For relevant background please see relevant page: Assessing Ovastacin and Fetuin B as a Non-Hormonal Contraceptive Targets  (https://openlabnotebooks.org/assessing-ovastacin-an-fetuin-b-as-a-non-hormonal-contraceptive-targets/) Donor Plasmid: pFastBac-Dual vector was used for the dual expression of hOvastacin-twinStrep (driven by polyhedrin promoter) and hFetuin B-Fc-6xHis (driven by p10 promoter). Recombinant Read More …

One year of ABHD2 – Where are we now?

Posted onAuthorOliver ArnoldsLeave a comment

The Recap It’s been one year since the last update on the α/β hydrolase domain 2 (ABHD2) as a target for non-hormonal contraception (see my previous post here). The major challenges were the production of ABHD2 and development of a reliable activity assay to screen and quantify inhibitory compounds. At that point 14 different constructs Read More …

Efficient Synthesis of Acyclic and Cyclic Pyrazoles for Evaluation as Antiviral nsp2 Protease Inhibitors

Posted onAuthorAnirban GhoshalLeave a comment

Pyrazole (E)-vinyl sulfone 3 was identified as a potential covalent CHIKV nsp2 protease inhibitor from a high throughput screen in the READDI Antiviral Drug Discovery Center at UNC.1 Initial re-synthesis of the hit compound yielded a mixture of acyclic (3) and cyclic sulfones (4) (Scheme 1), which were identified by 1D and 2D NMR, but Read More …

AViDD Filters: Compound Filtering SOP for Hit to Lead

Posted onAuthorAnwar HossainLeave a comment

High throughput screening (HTS) is a powerful technique for identifying potential drug candidates from large libraries of compounds. However, many compounds that show activity in HTS are false positives or may not be suitable for further development. Therefore, it is important to apply various filters to eliminate compounds that have undesirable properties, such as poor Read More …

PLCζ1: a promising target for non-hormonal contraceptives

Posted onAuthorEve CarterLeave a comment

The Structural Genomics Consortium (SGC) has been funded by the Bill & Melinda Gates Foundation to research Women’s and Children’s Health, focusing on the advancement of drug discovery in reproductive biology and disease, child development, and childhood diseases. The SGC plans to generate protein reagents and chemical probes for several potential drug targets for new, Read More …

PATL2: A Potential Contraceptive Target August 2023 Update

Posted onAuthorMadison EdwardsLeave a comment

PATL2: A Potential Contraceptive Target A promising protein target for NHCs is Protein Associated with Topoisomerase II Homolog 2 (PATL2), a highly conserved, oocyte-specific mRNA-binding protein that represses translation1. For consanguineous families, the inheritance pattern for PATL2 is recessive; thus, infertility is often caused by homozygous mutations in the gene2. Although some mutations in PATL2 Read More …

GRC Poster: Identification of SARS-CoV-2 helicase inhibitors by large-scale virtual screening

Posted onAuthorAnwar HossainLeave a comment

by Mohammad Anwar Hossain1, Konstantin Popov2, Sumera Perveen3, Kesatebrhan Haile Asressu1, Kenneth Hugh Pearce Jr.2, Cheryl Arrowsmith3, Peter Brown1, Alexander Tropsha4, Tim Willson1 1Structural Genomics Consortium, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA; 2CICBDD, UNC Eshelman School of Pharmacy; 3The Structural Genomics Consortium, University of Toronto, Canada; 4CBMC, UNC Eshelman Read More …