Table 12.

Adipose-Targeting Peptides

Isolation method and cell typea	Peptide Sequenceb,c	Receptor Identified	Applications and Notes
In vitro panning against mouse preadipocyte 3T3-L1 cells	CWLGEWLGC413 (mPep)	α5β1	Therapeutic Applications: Peptide-D(KLAKLAK)2 killed mouse 3T3-L1 preadipocytes that were induced toward adipocyte differentiation in vitro. Oligonucleotide Delivery: When the peptide was displayed on a chimeric prokaryotic-eukaryotic AAVP vector carrying the Ucp 1 gene, it transduced 3T3-L1 preadipocytes, preventing them from differentiating into adipocytes.
Ex vivo panning against adipose stromal cells isolated from white adipose tissue after patient liposuction	CMLAGWIPC413 (hPep)	α5β1	Functional Peptide Activity: Free peptide increased cell migration of human adipose stem cells in vitro.
In vivo panning against white fat in obese leptin-deficient Lepob/ob mice using a T7 phage peptide library	CKGGRAKDC414 (binds white fat vasculature)	Prohibitin414,416,417	Therapeutic Applications: Subcutaneous injection of peptide-GG-D(KLAKLAK)2 into obese mice414,418 or rats418 reversed obesity and reduced white fat mass. Injection of a peptide-BVT.2733 (an 11β-HSD1 inhibitor) conjugate into obese mice reversed obesity, reduced adipose tissue mass and size, and decreased plasma glucose tolerance.419 Subcutaneous injection of peptide-GG-D(KLAKLAK)2 into obese rhesus macaques monkeys decreased white fat mass, total body weight, BMI, abdominal circumference, and insulin resistance.415 Note: The peptide also targets to prohibitin-positive tumors.472
In vivo panning (T7 library) against white adipose tissue in mice followed by FACS to isolate adipose stromal cells	CSWKYWFGEC412 (WAT7)	Truncated decorin lacking glycanation site (ΔDCN)

^aAll libraries are pIII phage libraries unless otherwise noted.

^bCysteine residues that form disulfide bonds are indicated in bold.

^cCommon peptide names that have been used in the literature are indicated in parentheses next to the peptide sequence.