Wasilko David J, Lee S Edward, Stutzman-Engwall Kim J, Reitz Beverly A, Emmons Thomas L, Mathis Karl J, Bienkowski Michael J, Tomasselli Alfredo G, Fischer H David
Pfizer Inc., Global Research and Development Groton/New London Laboratories, Eastern Point Road, Groton, CT 06340, USA.
Protein Expr Purif. 2009 Jun;65(2):122-32. doi: 10.1016/j.pep.2009.01.002. Epub 2009 Jan 11.
Compounds capable of stimulating soluble guanylate cyclase (sGC) activity might become important new tools to treat hypertension. While rational design of these drugs would be aided by elucidation of the sGC three-dimensional structure and molecular mechanism of activation, such efforts also require quantities of high quality enzyme that are challenging to produce. We implemented the titerless infected-cells preservation and scale-up (TIPS) methodology to express the heterodimeric sGC. In the TIPS method, small-scale insect cell cultures were first incubated with a recombinant baculovirus which replicated in the cells. The baculovirus-infected insect cells (BIIC) were harvested and frozen prior to cell lysis and the subsequent escape of the newly replicated virus into the culture supernatant. Thawed BIIC stocks were ultimately used for subsequent scale up. As little as 1 mL of BIIC was needed to infect a 100-L insect cell culture, in contrast to the usual 1L of high-titer, virus stock supernatants. The TIPS method eliminates the need and protracted time for titering virus supernatants, and provides stable, concentrated storage of recombinant baculovirus in the form of infected cells. The latter is particularly advantageous for virus stocks which are unstable, such as those for sGC, and provides a highly efficient alternative for baculovirus storage and expression. The TIPS process enabled efficient scale up to 100-L batches, each producing about 200mg of active sGC. Careful adjustment of expression culture conditions over the course of several 100-L runs provided uniform starting titers, specific activity, and composition of contaminating proteins that facilitated development of a process that reproducibly yielded highly active, purified sGC.
能够刺激可溶性鸟苷酸环化酶(sGC)活性的化合物可能会成为治疗高血压的重要新工具。虽然阐明sGC的三维结构和激活分子机制有助于这些药物的合理设计,但此类研究还需要大量高质量的酶,而这在生产上具有挑战性。我们采用无滴度感染细胞保存和放大(TIPS)方法来表达异二聚体sGC。在TIPS方法中,首先将小规模昆虫细胞培养物与在细胞中复制的重组杆状病毒一起孵育。在细胞裂解以及新复制的病毒随后逸出到培养上清液之前,收获并冷冻杆状病毒感染的昆虫细胞(BIIC)。最终将解冻的BIIC储备用于后续放大培养。与通常需要1升高滴度病毒储备上清液相比,感染100升昆虫细胞培养物只需1毫升BIIC。TIPS方法消除了对病毒上清液进行滴度测定的需求和漫长时间,并以感染细胞的形式提供重组杆状病毒的稳定、浓缩储存。对于不稳定的病毒储备(如sGC的病毒储备),后者特别有利,并为杆状病毒的储存和表达提供了一种高效替代方法。TIPS工艺能够高效放大至100升批次,每批可产生约200毫克活性sGC。在几次100升培养过程中仔细调整表达培养条件,可提供均匀的起始滴度、比活性和污染蛋白组成,这有助于开发一种可重复产生高活性、纯化sGC的工艺。