saquinavir and Lupus-Erythematosus--Systemic

saquinavir has been researched along with Lupus-Erythematosus--Systemic* in 1 studies

Other Studies

1 other study(ies) available for saquinavir and Lupus-Erythematosus--Systemic

Article	Year
A structural investigation of FISLE-412, a peptidomimetic compound derived from saquinavir that targets lupus autoantibodies. Bioorganic & medicinal chemistry letters, 2017, 10-15, Volume: 27, Issue:20 FISLE-412 is the first reported small molecule peptidomimetic that neutralizes anti-dsDNA autoantibodies associated with systemic lupus erythematosus (SLE) pathogenesis. FISLE-412 is a complex small molecule that involves a challenging synthesis scheme, but has attractive pharmacological activities as a potential small molecule therapeutic in lupus. Therefore, we initiated a Structure-Activity Relationship study to simplify the complexity of FISLE-412. We synthesized a small library of mimetopes around the FISLE-412 structure and identified several analogues which could neutralize anti-DNA lupus antibodies in vitro and ex vivo. Our strategies reduced the structural complexity of FISLE-412 and provide important information that may guide development of potential autoantibody-targeted lupus therapeutics. Topics: Antibodies, Antinuclear; Drug Design; Humans; Inhibitory Concentration 50; Kidney; Lupus Erythematosus, Systemic; Peptidomimetics; Polyamines; Quinolines; Saquinavir; Structure-Activity Relationship	2017

Article

Year

A structural investigation of FISLE-412, a peptidomimetic compound derived from saquinavir that targets lupus autoantibodies.

Bioorganic & medicinal chemistry letters, 2017, 10-15, Volume: 27, Issue:20

FISLE-412 is the first reported small molecule peptidomimetic that neutralizes anti-dsDNA autoantibodies associated with systemic lupus erythematosus (SLE) pathogenesis. FISLE-412 is a complex small molecule that involves a challenging synthesis scheme, but has attractive pharmacological activities as a potential small molecule therapeutic in lupus. Therefore, we initiated a Structure-Activity Relationship study to simplify the complexity of FISLE-412. We synthesized a small library of mimetopes around the FISLE-412 structure and identified several analogues which could neutralize anti-DNA lupus antibodies in vitro and ex vivo. Our strategies reduced the structural complexity of FISLE-412 and provide important information that may guide development of potential autoantibody-targeted lupus therapeutics.

Topics: Antibodies, Antinuclear; Drug Design; Humans; Inhibitory Concentration 50; Kidney; Lupus Erythematosus, Systemic; Peptidomimetics; Polyamines; Quinolines; Saquinavir; Structure-Activity Relationship

2017