Small molecule antagonists of α4 integrins: novel drugs for asthma

Bibliography

• LOBB RR, HEMLER ME: The pathophysiologic role of a4 integrins in vivo. J. Clin. Invest. (1994) 94:1722–1728.
   PubMed Web of Science ®Google Scholar
• BAYLESS KJ, MEININGER GA, SCHOLTZ JM, DAVIS GE: Osteopontin is a ligand for the a481 integrin. J. Cell Sci. (1998) 111:1165–1174.
   PubMed Web of Science ®Google Scholar
• •This paper suggests that the phosphoprotein osteopontin, highly expressed at inflammatory sites, may be a novel extracellular ligand for integrin VLA-4.
   Google Scholar
• MURRY CE, GIACHELLI CM, SCHWARTZ SM, VRACKO R: Macrophages express osteopontin during repair of myocardial necrosis. Am. J. Pathol (1994) 145:1450–1462.
   PubMed Web of Science ®Google Scholar
• LOBB RR: Adhesion molecule antagonists in animal models of asthma. Adhesion Molecules in Allergic Disease, (Bochner B, Ed.) Marcel Dekker, Inc., NY: 393–405.
   Google Scholar
• HENDERSON WR Jr., CHI EY, ALBERT RK et al.: Blockade of CD49d (a4 integrin) on intrapulmonary but not circulating leukocytes inhibits airway inflammation and hyperresponsiveness in a mouse model of asthma. J. Clin. Invest. (1997) 100:3083–3092.
   Google Scholar
• ••A careful comparison of local and systemic delivery of mAbto a4 integrins in a murine model of asthma shows conclu-sively that local delivery is more efficacious, and identifies a novel a4-expressing CD11c+ cell within the lung parenchyma as the possible therapeutic target.
   Google Scholar
• HOJO M, MAGHNI K, ISSEKUTZ TB, MARTIN JG: Involve-ment of a-4 integrins in allergic airway responses and mast cell degranulation in vivo. Am. J. Respir. Grit Care Med. (1998) 158:1127–1133.
   PubMed Web of Science ®Google Scholar
• STAMATIOU P, HAMID Q, TAHA R et al: 5-0xo-ETEinduces pulmonary eosinophilia in an integrin-dependent manner in brown Norway rats. J. Clin. Invest. (1998) 102:2165–2172.
   PubMed Web of Science ®Google Scholar
• SCHNEIDER T, ISSEKUTZ TB, ISSEKUTZ AC: The role ofalpha4 (CD49d) and beta2 (CD18) integrins in eosino-phil and neutrophil migration to allergic lung inflam-mation in the brown Norway rat. Am. J. Respir. Cell Mol Biol. (1999) 20:448–457.
   PubMed Web of Science ®Google Scholar
• KUBES P, NIU X-F, SMITH CW, KEHRLI ME Jr., REINHARDTPH, WOODMAN RC: A novel 81-dependent adhesion pathway on neutrophils: A mechanism invoked by dihydrocytochalasin B or endothelial transmigration. FASEB J. (1995) 9:1103–1111.
   Google Scholar
• REINHARDT PH, ELLIOTT JF, KUBES P: Neutrophils canadhere via a481-integrin under flow conditions. Blood (1997) 89:3837–3846.
   PubMed Web of Science ®Google Scholar
• REINHARDT PH, WARD CA, GILES WR, KUBES P: Emigrated rat neutrophils adhere to cardiac myocytes via a4 integrin. Circ. Res. (1997) 81:196–201.
   PubMed Web of Science ®Google Scholar
• REINHARDT PH, KUBES P: Differential leukocyterecruitment from whole blood via endothelial adhesion molecules under shear conditions. Blood (1998) 92:4691–4699.
   PubMed Web of Science ®Google Scholar
• •This paper shows that a subset of PMN in human whole blood can adhere to VCAM1 under flow conditions in an a4-integrin dependent fashion.
   Google Scholar
• WENZEL SE, SZEFLER SJ, LEUNG DY, SLOAN SI, REX MD, MARTIN RJ: Bronchoscopic evaluation of severe asthma. Amer. J. Respir. Crit. Care Med. (1997) 156:737–743.
   PubMed Web of Science ®Google Scholar
• FAHY JV, KIM KW, LIU J, BOUSHEY HA: Respiratory pathophysiologic responses - prominent neutrophilic inflammation in sputum from subjects with asthma exacerbation. J. Allergy Clin. Immunol (1995) 95:843–852.
   PubMed Web of Science ®Google Scholar
• JAKUBOWSKI A, ROSA MD, BIXLER S, LOBB R, BURKLY LC: Vascular cell adhesion molecule (VCAM)-Ig fusion protein defines distinct affinity states of the very late antigen-4 (VLA-4) receptor. Cell Ad. Commun. (1995) 3:131–142.
   PubMed Web of Science ®Google Scholar
• LOBB RR, ANTOGNETTI G, PEPINSKY RB, BURKLY LC,LEONE DR, WHITTY A. A direct binding assay for the vascular cell adhesion molecule-1 (VCAM-1) interac-tion with a4 integrins. Cell Ad. Commun. (1995) 3:385–397.
   Google Scholar
• KUIJPERS TW, MUL EP, BLOM M et al.: Freezing adhesion molecules in a state of high-avidity binding blocks eosinophil migration. J. Exp. Med. (1993) 178:279–284.
   PubMed Web of Science ®Google Scholar
• ALON R, KASSNER PD, CARR MW, FINGER EB, HEMLER ME, SPRINGER TA: The integrin VLA-4 supports tethering and rolling in flow on VCAM-1. J. Cell Biol. (1995) 128:1243–1253.
   PubMed Web of Science ®Google Scholar
• CHEN C, MOBLEY JL, DWIR 0 et al.: High affinity very late antigen-4 subsets expressed on T cells are mandatory for spontaneous adhesion strengthening but not for rolling on VCAM-1 in shear flow. J. Immunol (1999) 162:1084–1095.
   Google Scholar
• •This paper provides the first good evidence for a small sub-population of high affinity VLA4 integrins on the surface of Jurkat T-cells and human PBL.
   Google Scholar
• BRISKIN M, WINSOR-HINES D, SHYJAN A et al.: Human mucosal addressin cell adhesion molecule-1 is prefer-entially expressed in intestinal tract and associated lymphoid tissue. Amer. J. Pathol (1997) 151:97–110.
   PubMed Web of Science ®Google Scholar
• ERLE DJ, BRISKIN MJ, BUTCHER EC, GARCIA-PARDO A, LAZAROVITS Al, TIDSWELL M: Expression and function of the MAdCAM-1 receptor, integrin a4p7, on human leukocytes. J. Immunol. (1994) 153:517–528.
   PubMed Web of Science ®Google Scholar
• GRAYSON MH, VAN DER VIEREN M, STERBINSKY SA eta].: ac1132 integrin is expressed on human eosinophils and functions as an alternative ligand for vascular cell adhesion molecule 1 (VCAM-1). J. Exp. Med. (1998) 188:2187–2191.
   Google Scholar
• •This paper shows that VCAM1 can bind to the novel 132 integrin ad132. This is the first example of an I-domain containing 132 integrin binding VCAM1.
   Google Scholar
• TAOOKA Y, CHEN J, YEDNOCK T, SHEPPARD D: The integrin a9B1 mediates adhesion to activated endothe-lial cells and transendothelial neutrophil migration through interaction with vascular cell adhesion molecule-1. J. Cell Biol. (1999) 145:413–420.
   PubMed Web of Science ®Google Scholar
• ••This paper shows that the integrin a9131, closely related toa4131, is expressed on human PMN and binds VCAM1.
   Google Scholar
• VAN DER VIEREN M, TRONG HL, WOOD CL et al.: A novel leukointegrin, adb02, binds preferentially to ICAM-3. Immunity (1995) 3:683–690.
   Google Scholar
• PALMER EL, RUEGG C, FERRANDO R, PYTELA R, SHEPPARD D Sequence and tissue distribution of the integrin a9 subunit, a novel partner of pl that is widely distributed in epithelia and muscle. J. Cell Biol. (1993) 123:1289–1297.
   PubMed Web of Science ®Google Scholar
• LIN K-C, CASTRO AC: Very late antigen 4 (VLA4) antago-nists as anti-inflammatory agents. Curr. Op. Chem. Biol. (1998) 2:453–457.
   PubMed Web of Science ®Google Scholar
• LIN K-C, ATEEQ HS, HSIUNG SH et al: Selective, tight-binding inhibitors of integrin a4131 that inhibit allergic airway responses. J. Med. Chem. (1999) 42:920–934.
   PubMed Web of Science ®Google Scholar
• ••This paper reports on selective high affinity tight-bindinginhibitors of a4131 that are as effective in a sheep model of allergen-induced airways responses as a blocking a4-monoclonal antibody.
   Google Scholar
• CHEN LL, WHITTY A, LOBB RR, ADAMS SP, PEPINSKY RB: Multiple activation states of integrin a4131 detected through their different affinities for a small molecule ligand. J. Biol. Chem. (1999) 274:13167–13175.
   PubMed Web of Science ®Google Scholar
• ••In this paper, a high affinity small molecule ligand for a4131is used to directly identify a continuum of discrete a4131 affinity states defined by a range of receptor activation conditions.
   Google Scholar
• CARDARELLI PM, COBB RR, NOWLIN DM et al: Cyclic RGD peptide inhibits alpha 4 beta 1 interaction with connecting segment 1 and vascular cell adhesion molecule. J. Biol. Chem. (1994) 269:18668–18673.
   PubMed Web of Science ®Google Scholar
• VANDERSLICE P, REN K, REVELLE JK et al: A cyclic hexapeptide is a potent antagonist of alpha 4 integrins. j Immunol (1997) 158: 1710-1718.
   Google Scholar
• JACKSON DY, QUAN C, ARTIS DR et al.: Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents. J. Med. Chem. (1997) 40:3359–3368.
   PubMed Web of Science ®Google Scholar
• •This paper documents high affinity a4131 inhibitors based on a constrained cyclic tetra-peptide scaffold.
   Google Scholar
• HAMANN A, ANDREW DP, JABLONSKI-WESTRICH D, HOLZMANN B, BUTCHER EC: Role of alpha 4-integrins in lymphocyte homing to mucosal tissues in vivo. J. Immunol (1994) 152:3282–3293.
   PubMed Web of Science ®Google Scholar
• SOUERS AJ, VIRGILIO AA, SCHURER SS, ELLMAN JA: Novelinhibitors of a4131 integrin receptor interactions through library synthesis and screening. Bioorg. &Med. Chem. Lett. (1998) 8:2297–2302.
   PubMed Web of Science ®Google Scholar
• ABRAHAM WM, AHMED A, SIELCZAK MW, NARITA M, ARRHENIUS T, ELICES MJ: Blockade of late-phase airway responses and airway hyperresponsiveness in allergic sheep with a small-molecule peptide inhibitor of VLA-4. Am. J. Respir. Grit. Care Med. (1997) 156:696–703.
   PubMed Web of Science ®Google Scholar
• ABRAHAM WM, GILL A, AHMED A etal.: A small moleculetight binding inhibitor of the integrin a41, BIO-1211, blocks antigen-induced late airway responses (LAR), airway hyperresponsiveness (AHR), and inflamma-tion in sheep. Am. J. Respir. CriL Care Med. (1999) 159:A326.
   Google Scholar
• MAO Y, ORIORDAN TG, SABATER J et al: A small molecule inhibitor of very late antigen-4 (VLA-4) can block and reverse the antigen induced impairment of mucociliary clearance (MCC) in ovine airways. Am. J. Respir. Grit. Care Med. (1999) 159:A472.
   Web of Science ®Google Scholar