Novel growth hormone conjugates comprising a growth hormone compound (GH) and a growth hormone binding protein (GHBP) are disclosed. The invention also encompasses a novel derivatization method for producing stable, long-lasting conjugate (hGH-GHBP) by site specific conjugation. The novel GH-GHBP conjugates have an extended half-life in circulation that facilitates therapeutic use of the protein. The GH-GHBP conjugates exhibit pharmacological properties such as increased functional in vivo half-life, improved renal filtration, improved protease protection and albumin binding.
Carbohydrate-based drug delivery polymers and conjugates thereof
申请人:NEKTAR THERAPEUTICS
公开号:US09173951B2
公开(公告)日:2015-11-03
Provided herein are water-soluble carbohydrate polymers which are monoderivatized at their reducing terminus, such that the carbohydrate polymers can be selectively conjugated at a single location. Also provided are methods of preparation and conjugation of the monoderivatized carbohydrate polymers.
THERAPEUTIC PROTEINS WITH INCREASED HALF-LIFE AND METHODS OF PREPARING SAME
申请人:Baxalta Incorporated
公开号:US20180318432A1
公开(公告)日:2018-11-08
The present disclosure relates to materials and methods of conjugating a water soluble polymer to a therapeutic protein.
本公开涉及将水溶性聚合物与治疗性蛋白质结合的材料和方法。
BLOOD COAGULATION PROTEIN CONJUGATES
申请人:BAXALTA INCORPORATED
公开号:US20160120994A1
公开(公告)日:2016-05-05
The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a blood coagulation protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer. In one embodiment of the invention the conjugation is carried out in the presence of the nucleophilic catalyst aniline. In addition the generated oxime linkage can be stabilized by reduction with NaCNBH
3
to form an alkoxyamine linkage.
A newapproach for tethering of bioactive molecules via arginine is proposed and validated on collagen 2D matrices. The method involves the introduction of a methyl ketone on arginine side-chains, followed by reaction with model alkoxyamino derivatives.