1,687
22
Essay, 2 pages (500 words)

The usage of prolyl oligopeptide

Advertising We'll write a high-quality original custom paper on The usage of prolyl oligopeptide just for you with a 15% discount for the 1st order Use a Discount Use a Discount

Prolyl oligopeptidase or prolyl endopeptidase (EC 3. 4. 21. 26) is a post-proline cleaving enzyme that belongs to the family of serine proteases. It is also abbreviated as PO, PE, PEP, POP, or PREP (herein referred as POP) (Polgar, 2002). POP is primarily expressed in the hippocampus, hypothalamus, cortex, amygdala, and striatum regions of the human brain. Earlier, POP was discovered as an oxytocin cleaving enzyme and later demonstrated to be a peptidase that cleaved short peptides at the carboxyl side of proline with a high specificity (Walter et al., 1971; Polgar and Szeltner, 2008).

It has been demonstrated that POP serves an important role in the brain function as it cleaves several neuropeptides and also in the maturation of peptide hormones as well as recognize several neuroactive peptides as its substrates including oxytocin, bradykinin, angiotensins I and II, substance P, arginine vasopressin, and thyrotropin releasing hormone (Polgar and Szeltner, 2008. In addition to its peptidase activity, POP is capable of modulating the function of several proteins such as α-tubulin (Schulz et al., 2005), GAP-43 (Di Daniel et al., 2009), and α-synuclein (Lambeir, 2011a) through protein-protein interactions. Furthermore, numerous inhibitors against POP were proposed that are effective in several aspects of the central nervous system, including learning, memory and mood-related behaviors (Männistö et al., 2007; Lawandi et al., 2010; Lambeir, 2011b).

Besides its suggested role in eating and mood disorders, hypertension and cell-cycle progression, POP is related to the pathological process of neurodegeneration in Parkinson’s, Alzheimer’s, and Huntington’s disease (Hannula et al., 2013). Numerous POP inhibitors possessing anti-amnesic, cognition-enhancing and neuroprotective properties have been reported by several academic research groups (Lawandi et al., 2010; LГіpez et al., 2011; LГіpez et al., 2013). Early efforts included the development of substrate-like peptidomimetic compounds that were based on the systematic modification of the prototypical POP inhibitor N-benzyloxycarbonyl prolyl-prolinal (ZPP) (Yoshimoto et al., 1985).

Over the past 30 years, several POP inhibitors have been patented and entered the early phases of clinical trials [11]. Despite the development of potent inhibitors of POP having nanomolar activities, they failed in the clinical trials and none are currently in the market for human therapy (LГіpez et al., 2011). The most common reason for failure is their unfavorable pharmacokinetic properties and inability to cross the blood-brain barrier (BBB) (LГіpez et al., 2013).

Hence, the exploration of new scaffolds and potent inhibitors which have good pharmacokinetic, pharmacodynamic and toxic properties becomes critical. Consistent effort have been made to identify potential inhibitors against POP through in silico studies highlight the need of POP inhibitors along with the contribution of in silico research to therapeutics (Haffner et al., 2008; Lawandi et al., 2009; De Cesco et al., 2012; Mariaule et al., 2015; De Almeida et al., 2016; Kumar et al., 2017).

Therefore, computer-aided drug discovery strategies offer promising choice to the identification of new hit compounds, their optimization into potential hits with improved absorption, distribution, metabolism, excretion and toxicity profile and avoid adverse effects, cost, and time with limited resources (Kapetanovic, 2008; Macalino et al., 2015).

Thank's for Your Vote!
The usage of prolyl oligopeptide. Page 1
The usage of prolyl oligopeptide. Page 2
The usage of prolyl oligopeptide. Page 3
The usage of prolyl oligopeptide. Page 4

This work, titled "The usage of prolyl oligopeptide" was written and willingly shared by a fellow student. This sample can be utilized as a research and reference resource to aid in the writing of your own work. Any use of the work that does not include an appropriate citation is banned.

If you are the owner of this work and don’t want it to be published on AssignBuster, request its removal.

Request Removal

Cite this Essay

References

AssignBuster. (2021) 'The usage of prolyl oligopeptide'. 31 December.

Reference

AssignBuster. (2021, December 31). The usage of prolyl oligopeptide. Retrieved from https://assignbuster.com/the-usage-of-prolyl-oligopeptide/

References

AssignBuster. 2021. "The usage of prolyl oligopeptide." December 31, 2021. https://assignbuster.com/the-usage-of-prolyl-oligopeptide/.

1. AssignBuster. "The usage of prolyl oligopeptide." December 31, 2021. https://assignbuster.com/the-usage-of-prolyl-oligopeptide/.


Bibliography


AssignBuster. "The usage of prolyl oligopeptide." December 31, 2021. https://assignbuster.com/the-usage-of-prolyl-oligopeptide/.

Work Cited

"The usage of prolyl oligopeptide." AssignBuster, 31 Dec. 2021, assignbuster.com/the-usage-of-prolyl-oligopeptide/.

Get in Touch

Please, let us know if you have any ideas on improving The usage of prolyl oligopeptide, or our service. We will be happy to hear what you think: [email protected]