PMID- 34867411
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20211207
IS  - 1663-9812 (Print)
IS  - 1663-9812 (Electronic)
IS  - 1663-9812 (Linking)
VI  - 12
DP  - 2021
TI  - Lipidized Prolactin-Releasing Peptide as a New Potential Tool to Treat Obesity 
      and Type 2 Diabetes Mellitus: Preclinical Studies in Rodent Models.
PG  - 779962
LID - 10.3389/fphar.2021.779962 [doi]
LID - 779962
AB  - Obesity and type 2 diabetes mellitus (T2DM) are preconditions for the development 
      of metabolic syndrome, which is reaching pandemic levels worldwide, but there are 
      still only a few anti-obesity drugs available. One of the promising tools for the 
      treatment of obesity and related metabolic complications is anorexigenic 
      peptides, such as prolactin-releasing peptide (PrRP). PrRP is a centrally acting 
      neuropeptide involved in food intake and body weight (BW) regulation. In its 
      natural form, it has limitations for peripheral administration; thus, we designed 
      analogs of PrRP lipidized at the N-terminal region that showed high binding 
      affinities, increased stability and central anorexigenic effects after peripheral 
      administration. In this review, we summarize the preclinical results of our 
      chronic studies on the pharmacological role of the two most potent palmitoylated 
      PrRP31 analogs in various mouse and rat models of obesity, glucose intolerance, 
      and insulin resistance. We used mice and rats with diet-induced obesity fed a 
      high-fat diet, which is considered to simulate the most common form of human 
      obesity, or rodent models with leptin deficiency or disrupted leptin signaling in 
      which long-term food intake regulation by leptin is distorted. The rodent models 
      described in this review are models of metabolic syndrome with different 
      severities, such as obesity or morbid obesity, prediabetes or diabetes and 
      hypertension. We found that the effects of palmitoylated PrRP31 on food intake 
      and BW but not on glucose intolerance require intact leptin signaling. Thus, 
      palmitoylated PrRP31 analogs have potential as therapeutics for obesity and 
      related metabolic complications.
CI  - Copyright (c) 2021 Mrazikova, Neprasova, Mengr, Popelova, Strnadova, Hola, Zelezna, 
      Kunes and Maletinska.
FAU - Mrazikova, Lucia
AU  - Mrazikova L
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Neprasova, Barbora
AU  - Neprasova B
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
AD  - Institute of Physiology, Czech Academy of Sciences, Prague, Czech.
FAU - Mengr, Anna
AU  - Mengr A
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Popelova, Andrea
AU  - Popelova A
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Strnadova, Veronika
AU  - Strnadova V
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Hola, Lucie
AU  - Hola L
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Zelezna, Blanka
AU  - Zelezna B
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
FAU - Kunes, Jaroslav
AU  - Kunes J
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
AD  - Institute of Physiology, Czech Academy of Sciences, Prague, Czech.
FAU - Maletinska, Lenka
AU  - Maletinska L
AD  - Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, 
      Prague, Czech.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20211118
PL  - Switzerland
TA  - Front Pharmacol
JT  - Frontiers in pharmacology
JID - 101548923
PMC - PMC8637538
OTO - NOTNLM
OT  - leptin resistance
OT  - obesity
OT  - prolactin-releasing peptide
OT  - rodent models
OT  - type 2 diabetes
COIS- The authors declare that the research was conducted in the absence of any 
      commercial or financial relationships that could be construed as a potential 
      conflict of interest.
EDAT- 2021/12/07 06:00
MHDA- 2021/12/07 06:01
PMCR- 2021/11/18
CRDT- 2021/12/06 09:04
PHST- 2021/09/27 00:00 [received]
PHST- 2021/11/01 00:00 [accepted]
PHST- 2021/12/06 09:04 [entrez]
PHST- 2021/12/07 06:00 [pubmed]
PHST- 2021/12/07 06:01 [medline]
PHST- 2021/11/18 00:00 [pmc-release]
AID - 779962 [pii]
AID - 10.3389/fphar.2021.779962 [doi]
PST - epublish
SO  - Front Pharmacol. 2021 Nov 18;12:779962. doi: 10.3389/fphar.2021.779962. 
      eCollection 2021.