| 摘要 |
The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. |
| 主权项 |
1. An immunogenic composition comprising:
(a) a glycan conjugate including a carrier and one or more glycans, and optionally (b) an adjuvant; wherein each of the one or more glycans is conjugated with the carrier through a linker having the formula (III):wherein:
X1 is —OR or —SR, wherein R is an oxygen or sulfur protecting group, optionally substituted C1-10 alkyl, optionally substituted aryl, optionally substituted acyl, or optionally substituted imidoyl; each instance of R1, R2, R3, R4, R5, R6 and L is independently selected from hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted heterocyclyl, optionally substituted aryl, —N3, —NO2, —N(RB)2, —N(RA)C(O)RA, —ORA, —OC(O)RA, —SRA, —C(O)N(RB)2, —CN, —C(O)RA, —C(O)ORA, —S(O)RA, —SO2RA, —SO2N(RB)2, and —NHSO2RB; each instance of RA is independently selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted heterocyclyl, and optionally substituted aryl; each instance of RB is independently selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted heterocyclyl, and optionally substituted aryl;and
provided the glycan conjugate is not of the formula (III-a) and (III-b): |
